A Comparative Study on the Lysosomal Cation Channel TMEM175 Using Automated Whole-Cell Patch-Clamp, Lysosomal Patch-Clamp, and Solid Supported Membrane-Based Electrophysiology: Functional Characterization and High-Throughput Screening Assay Development.

The lysosomal cation channel TMEM175 is a Parkinson's disease-related protein and a promising drug target. Unlike whole-cell automated patch-clamp (APC), lysosomal patch-clamp (LPC) facilitates physiological conditions, but is not yet suitable for high-throughput screening (HTS) applications. Here, we apply solid supported membrane-based electrophysiology (SSME), which enables both direct access to lysosomes and high-throughput electrophysiological recordings. In SSME, ion translocation mediated by TMEM175 is stimulated using a concentration gradient at a resting potential of 0 mV. The concentration-dependent K+ response exhibited an I/c curve with two distinct slopes, indicating the existence of two conducting states. We measured H+ fluxes with a permeability ratio of PH/PK = 48,500, which matches literature findings from patch-clamp studies, validating the SSME approach. Additionally, TMEM175 displayed a high pH dependence. Decreasing cytosolic pH inhibited both K+ and H+ conductivity of TMEM175. Conversely, lysosomal pH and pH gradients did not have major effects on TMEM175. Finally, we developed HTS assays for drug screening and evaluated tool compounds (4-AP, Zn as inhibitors; DCPIB, arachidonic acid, SC-79 as enhancers) using SSME and APC. Additionally, we recorded EC50 data for eight blinded TMEM175 enhancers and compared the results across all three assay technologies, including LPC, discussing their advantages and disadvantages.

Solid-Supported Membrane (SSM)-Based Electrophysiology Assays Using Surface Electrogenic Event Reader Technology (SURFE²R) in Early Drug Discovery.

This article presents detailed descriptions of procedures and troubleshooting tips for solid-supported membrane (SSM)-based electrophysiology assays (SURFE²R) to measure electrogenic solute carrier transporter proteins (SLCs) and assess the effects of compounds that modulate their activity. SURFE²R allows the use of the standard 96-well format, making it an ideal platform for tertiary assays in a drug-discovery campaign. The assays are performed with cell-line-derived membrane fractions or proteoliposomes containing the transporter of interest. Three main protocols are described for the isolation of membrane fractions from cell culture and the generation of proteoliposomes containing the transporter of interest. Additionally, detailed protocols for SURFE²R single concentration and dose-response experiments are included to measure the potencies of test compounds in stimulating or inhibiting transporter function (EC50 or IC50 values, respectively) and kinetic functional assays to calculate apparent affinity (kM ) and maximal velocity (Vmax ) of substrate uptake. © 2023 Sanofi. Current Protocols published by Wiley Periodicals LLC. PROTOCOL GROUP 1: Sample preparation for SSM-based electrophysiology assays Support Protocol 1: Production of cell batches Support Protocol 2: Simple isolation of cell membranes Alternate Protocol 1: Isolation of cell membranes with sucrose gradient pre-purification Support Protocol 3: Production and isolation of liposomes Support Protocol 4: Preparation of sensor with isolated cell membranes Alternate Protocol 2: Preparation of sensor with isolated proteoliposomes PROTOCOL GROUP 2: Determination of assay parameters for SSM-based electrophysiology assay Support Protocol 5: Assay with stable buffer Alternate Protocol 3: Assay with ion gradient Support Protocol 6: Determination of membrane/liposome concentration Support Protocol 7: Determination of substrate dependency kM PROTOCOL GROUP 3: Determination of advanced assay parameters for SSM-based electrophysiology assays Support Protocol 8: Assessment of ion concentration dependency Support Protocol 9: Assessment of pH dependency Support Protocol 10: Assessment of DMSO dependency Support Protocol 11: Assessment of signal stability with multiple activations PROTOCOL GROUP 4: Compound testing through SSM-based electrophysiology assays using SURFE²R apparatus Support Protocol 12: Assessment of signal specificity of a published inhibitor or unknown compound(s) Support Protocol 13: Compound wash-out Support Protocol 14: Statistical analysis.

SSM-based electrophysiology, a label-free real-time method reveals sugar binding & transport events in SGLT1.

Here, we present a solid-supported membrane (SSM)-based electrophysiological approach to study sugar binding and Na+/glucose cotransport by SGLT1 in membrane vesicles. SSM-based electrophysiology delivers a cumulative real-time current readout from numerous SGLT1 proteins simultaneously using a gold-coated sensor chip. In contrast to conventional techniques, which mainly operate with voltage steps, currents are triggered by sugar or sodium addition. Sugar concentration jumps in the presence of sodium lead to transport currents between 5 and 10 nA. Remarkably, in the absence of sodium (i.e. no transport), we observed fast pre-steady-state (PSS) currents with time constants between 3 and 10 ms. These PSS currents mainly originate from sugar binding. Sodium binding does not induce PSS currents. Due to high time resolution, PSS currents were distinguished from transport and eventually correlated with conformational transitions within the sugar translocation pathway. In addition, we analyzed the impact of driving forces on transport and binding currents, showing that membrane voltage and sodium concentration gradients lead to an increased transport rate without affecting sugar binding kinetics. We also compared Na+/sugar efflux with physiologically relevant influx and found similar transport rates, but lower affinity in efflux mode. SSM-based electrophysiology is a powerful technique, which overcomes bottlenecks for transport measurements observed in other techniques such as the requirement of labels or the lack of real-time data. Rapid solution exchange enables the observation of substrate-induced electrogenic events like conformational transitions, opening novel perspectives for in-depth functional studies of SGLT1 and other transporters.

Atuação profissional nos esportes de aventura: estudo de caso com uma treinadora de surfe / Professional work performance in adventure sports: case study with a surf coach

RESUMO O objetivo do estudo foi analisar o contexto de atuação profissional de uma treinadora de surfe da cidade de Florianópolis, Santa Catarina. Adotaram-se procedimentos de pesquisa qualitativa e estudo de caso, por meio da combinação de técnicas de observação participante e entrevista semiestruturada. Foi utilizada a técnica de Análise Temática para a análise dos dados. Verificou-se que o contexto de atuação profissional da treinadora investigada compreende um sistema amplo e complexo, marcado pela sua participação em diversas atividades e interações sociais, com o envolvimento pleno em seu local de atuação profissional. A intervenção pedagógica da treinadora para o ensino/treino do surfe é condicionado pela sazonalidade, pelas condições do ambiente de prática desta modalidade, assim como pelo tipo de orientação esportiva, com o propósito pessoal de transmitir o seu estilo de vida ligado ao surfe.

ABSTRACT The purpose of the study was to analyze the context of professional work performance of a surf coach from Florianópolis city, Santa Catarina. Qualitative research and case study procedures were adopted conbining participant observation and semi-structured interviews. Thematic Analysis was used for data analysis. It was verified that the coach's context of professional work performance comprises a broad and complex system, marked by her participation in various activities and social interactions, with full participation in her place of professional work. The coach's pedagogical intervention for teaching/coaching surfing is conditioned by seasonality, the environmental conditions to practice this sport, and the focus of sports instruction. Essentialy, the coach's personal goal is to share her surfing lifestyle.

A Solid Supported Membrane-Based Technology for Electrophysical Screening of B0AT1-Modulating Compounds.

Classical high-throughput screening (HTS) technologies for the analysis of ionic currents across biological membranes can be performed using fluorescence-based, radioactive, and mass spectrometry (MS)-based uptake assays. These assays provide rapid results for pharmacological HTS, but the underlying, indirect analytical character of these assays can be linked to high false-positive hit rates. Thus, orthogonal and secondary assays using more biological target-based technologies are indispensable for further compound validation and optimization. Direct assay technologies for transporter proteins are electrophysiology-based, but are also complex, time-consuming, and not well applicable for automated profiling purposes. In contrast to conventional patch clamp systems, solid supported membrane (SSM)-based electrophysiology is a sensitive, membrane-based method for transporter analysis, and current technical developments target the demand for automated, accelerated, and sensitive assays for transporter-directed compound screening. In this study, the suitability of the SSM-based technique for pharmacological compound identification and optimization was evaluated performing cell-free SSM-based measurements with the electrogenic amino acid transporter B0AT1 (SLC6A19). Electrophysiological characterization of leucine-induced currents demonstrated that the observed signals were specific to B0AT1. Moreover, B0AT1-dependent responses were successfully inhibited using an established in-house tool compound. Evaluation of current stability and data reproducibility verified the robustness and reliability of the applied assay. Active compounds from primary screens of large compound libraries were validated, and false-positive hits were identified. These results clearly demonstrate the suitability of the SSM-based technique as a direct electrophysiological method for rapid and automated identification of small molecules that can inhibit B0AT1 activity.

Evidências psicológicas do surfe: efeitos terapêuticos e demandas assistenciais / Psychological evidences of surf: therapeutic effects and assistance demands / Evidencias psicológicas del surf: efectos terapéuticos y demandas de asistencia

O presente trabalho caracteriza-se como um estudo de revisão sistemática sobre pesquisas que tenham utilizado medidas psicológicas para avaliar atletas e praticantes de surfe. Foram utilizados os descritores "Surf" AND "Sport" e "Surf" AND "Psychology" e após aplicação dos critérios de exclusão, obteve-se uma amostra final de 28 artigos. Foram identificados estudos diversificados explorando aspectos psicológicos diferenciados nesse contexto, como questões de gênero, processos psicossociais, produção da subjetividade, efeitos terapêuticos e aspectos psicológicos concernentes ao universo da competição. Os resultados foram discutidos em categorias temáticas específicas, dentre as quais, destacam-se o estudo de processos psicológicos diretamente associados à prática do surfe; produções sobre o potencial terapêutico desencadeado pela prática do surfe; e também algumas evidências sobre efeitos adversos, principalmente no contexto competitivo. As evidências reforçaram a importância da assistência psicológica aos atletas de alto rendimento para promoção e manutenção da saúde mental, bem como para melhorias no desempenho esportivo. No lazer e em projetos específicos, o potencial terapêutico do surfe também se apresenta como um campo promissor.

The present work is characterized as a systematic review of researches that have used psychological measures to evaluate surf athletes and practitioners. The descriptors used were "Surf" AND "Psychology" and "Surf" AND "Sport" and after applying inclusion and exclusion criteria, was obtained a final sample of 28 articles. Diversified studies were found exploring different psychological aspects in this field, such gender issues, psychosocial processes, subjectivity development, therapeutic effects and psychological aspects concerning the competitive context. The results were discussed in specific categories, as those directly associated with the surf practice; works about the therapeutic potential triggered by the surfing practice; and also some evidences about some adverse effects, especially in the competition context. The evidences reinforce the relevance of psychological assistance to high-performance athletes to promotion and maintenance of the mental health, as well to improvements in surf performance. In leisure activities and specific projects, the therapeutic potential of surfing also appears as a promising field.

El presente trabajo se caracteriza como un estudio de revisión sistemática sobre investigaciones que han utilizado medidas psicológicas para evaluar atletas y practicantes de surf. Se utilizaron de los descriptores "Surf" AND "Psychology" y "Surf" AND "sport", después aplicar los criterios de inclusión y exclusión, se tienes una muestra final de 28 artículos. Fueron encontrados estudios explorando diferentes aspectos psicológicos en este campo, como temas de género, procesos psicosociales, desarrollo de la subjetividad, efectos terapéuticos y aspectos psicológicos relacionados con el contexto competitivo. Los resultados fueron discutidos en categorías específicas, como los directamente relacionados con la práctica del surf; trabajos sobre el potencial terapéutico desencadenados por la práctica del surf; y también algunas evidencias sobre efectos adversos, especialmente en el contexto competitivo. Las evidencias refuerzan la relevancia de asistencia psicológica a los atletas de alto rendimiento para promover y mantener la salud mental, así como para mejorar el rendimiento del surf. En las actividades de ocio y proyectos específicos, el potencial terapéutico del surf también aparece como un campo prometedor.

Amateur surfing on the south coast of são paulo: lifestyle and work as factors for practice engagement / O surfe amador no litoral sul de são paulo: estilo de vida e trabalho como fatores de aderência à prática

ABSTRACT The present study addresses correlations between lifestyle and engagement in physical activity, in addition to discussing the conditions that make it possible for amateurs to continue with a complex practice such as surfing for a long time. To this end, we interviewed eleven surfers with more than ten years of uninterrupted practice on the south coast of São Paulo. Using content analysis, it was possible to find that their permanence is less influenced by matters of gender, age and marital status (usually prioritized in the literature on the topic) than by employment conditions. It is argued that engagement in surfing is linked to the lifestyle and ideals of youth, while the conditions that lead amateurs to keep this practice involve family and employment relationships, the stability of which provides security to routine and modulates the games between social and nature times. Thus, mature surfers narrate a way of living that values prudent attitudes as a means for re-signifying surfing in their lives, pointing to a transformation of the surf culture. It is considered that the relationships between permanence in practice and job stability are worth investigating in further studies.

RESUMO No presente estudo, tratamos das relações entre estilo de vida e aderência à atividade física e discutimos as condições que possibilitam a longa permanência de amadores numa prática complexa como o surfe. Para tanto, entrevistamos onze surfistas com mais de dez anos de prática ininterrupta no litoral sul de São Paulo. Por meio de uma análise de conteúdo, foi possível constatar que a sua permanência é menos influenciada por questões de gênero, idade e estado civil (geralmente priorizada na literatura sobre o tema) do que condições empregatícias. Discute-se que adesão ao surfe é vinculada ao estilo de vida e aos ideais de juventude, ao passo que as condições de continuidade da prática dos amadores envolvem a família e os vínculos de emprego, cuja estabilidade dá segurança à rotina e modula os jogos entre os tempos sociais e da natureza. Assim, os surfistas maduros narram um modo de viver que valoriza atitudes prudentes como uma forma de ressignificação do surfe em suas vidas, apontando para uma transformação da cultura do surfe. Considera-se que as relações entre permanência na prática e estabilidade do emprego merecem ser investigadas em estudos futuros.

A esportivização do surfe: reflexões a luz de Pierre Bourdieu / The sportivization of surf: reflections in the light of Pierre Bourdieu / La esportivización del surf: reflexiones a la luz de Pierre Bourdieu

Pierre Bourdieu é uma referência importante para a pesquisa sociocultural do esporte e de práticas corporais. O presente trabalho, de cunho teórico conceitual, tem como objetivo analisar o processo de esportivização do surfe e identificar algumas vias para a construção de objetos de pesquisa sociocultural do surfe, a partir dos conceitos bourdieusianos de campo social e habitus. Para tanto, aspectos da constituição do surfe como esporte moderno são analisados. A análise também focaliza disputas especificas pelo capital e pela inserção brasileira no cenário internacional, na interface com questões relacionadas ao esporte espetáculo e sua relação com o mercado consumidor. Evidenciam-se contradições relacionadas à profissionalização do esporte, a interesses comerciais e aos ideais de liberdade e prazer presentes no surfe.

Pierre Bourdieu is an important theoretical reference for the sociocultural research of sport. The purpose of this article is to analyze the process of sportivization of surfing and to identify from Bourdieu's perspective some socio cultural dimensions for advance surf research, based on the concepts as social field and habitus. We discuss the process of constitution the surf as a modern sport. The analysis also evidences disputes over capital and the Brazilian insertion in the international competition scenario, as well as issues related to sport spectacle and its relationship with the consumer market. There are contradictions related to the professionalization of sport, commercial interests and the ideals of freedom and pleasure present in surfing.

Pierre Bourdieu es una referencia importante para la investigación sociocultural del deporte. El presente trabajo, de cuño teórico conceptual, tiene como objetivo analizar el proceso de esportivización del surf y identificar algunas vías para la construcción de objetos de investigación sociocultural del surf, a partir de los conceptos de campo social y habitus. Discutiremos aspectos de la constitución del surf como deporte moderno, así como se identifican disputas por el capital y la inserción brasileña en el escenario internacional competitivo, en la interfaz con cuestiones relacionadas al deporte espectáculo y su relación con el mercado consumidor. Se evidencian contradicciones relacionadas con la profesionalización del deporte, los intereses comerciales y los ideales de libertad y placer presentes en el surf.

Functional Characterization of SLC Transporters Using Solid Supported Membranes.

Here, we present a protocol for the functional characterization of the H+-coupled human peptide transporter PepT1 and sufficient notes to transfer the protocol to the Na+-coupled sugar transporter SGLT1, the organic cation transporter OCT2, the Na+/Ca2+ exchanger NCX, and the neuronal glutamate transporter EAAT3.The assay was developed for the commercially available SURFE2R N1 instrument (Nanion Technologies GmbH) which applies solid supported membrane (SSM)-based electrophysiology. This technique is widely used for the functional characterization of membrane transporters with more than 100 different transporters characterized so far. The technique is cost-effective, easy to use, and capable of high-throughput measurements.SSM-based electrophysiology utilizes SSM-coated gold sensors to physically adsorb membrane vesicles containing the protein of interest. A fast solution exchange provides the substrate and activates transport. For the measurement of PepT1 activity, we applied a peptide concentration jump to activate H+/peptide symport. Proton influx charges the sensor. A capacitive current is measured reflecting the transport activity of PepT1 . Multiple measurements on the same sensor allow for comparison of transport activity under different conditions. Here, we determine EC50 for PepT1-mediated glycylglycine transport and perform an inhibition experiment using the specific peptide inhibitor Lys[Z(NO2)]-Val.

Assessing non-uniform stiffening of the achilles tendon noninvasively using surface wave.

Currently, noninvasive cost-effective techniques capable of quantifying non-uniform degradation of tendon's mechanical and structural properties associated with localized tendon injuries are not readily available. This study demonstrates the applicability of a simple surface-wave elastography (SURF-E) method for assessing the stiffness of the Achilles Tendon by measuring the propagation velocity of surface waves along the tendon in a much broader range of values than currently available Ultrasound-based or MRI-based elastography methods do. Results from this study confirm the non-uniform stiffening of the AT during passive ankle dorsiflexions.

A experiência vivida de surfar: um estudo fenomenológico / The lived experience of surfing: a phenomenological study / La experiencia vivida de surfear: un estudio fenomenológico

O surfe é uma atividade amplamente praticada, que se constitui em deslizar na parede de uma onda sobre uma prancha. Entretanto, nota-se que a vivência com essa prática vai além de suas técnicas. O objetivo deste estudo foi compreender como é a experiência vivida de surfar por meio das percepções dos próprios praticantes. A metodologia de inspiração fenomenológica foi utilizada como meio de acesso a essas vivências, com o auxílio de entrevistas abertas, norteadas por pergunta disparadora. Foram entrevistados 8 participantes, todos amadores, que relataram experiências vividas apresentadas em 3 movimentos: antes de entrar no mar, vivenciando o mar com uma prancha e saída do mar. Nestes, evidenciou-se a necessidade de preparação para a prática, percepções mistas de medo, coragem, prazer e contemplação durante a experiência e a demonstração do quanto essa vivência extrapola os limites da praia para suas vidas pessoais. A partir dos resultados do presente estudo, entende-se que essa prática se apresenta de modo peculiar, e exige do profissional que se proponha a trabalhar com o surfe uma reflexão sobre os aspectos que o envolvem. Defende-se aqui uma psicologia do esporte que seja sensível às experiências vividas de seus praticantes para, posteriormente, ocupar-se de regras e técnicas.

Surfing is a widely practiced activity based on sliding up or down the wall of a wave on a surfboard. However, this study established that the experience with this practice goes beyond this technique. The aim of this study was to understand the lived experience of surfing based on practitioners' perceptions. The methodology was based on a phenomenologically inspired assumption and was used as a way to access these experiences with the support of open interviews guided by a trigger question. Eight participants were interviewed, and they reported the lived experience of surfing based on three moments: before entering the sea, experiencing the sea with a board and out of the sea. What came to light was the preparation for this practice, mixed perceptions of fear, courage, pleasure and contemplation during the experience and the descriptions of how much this experience goes beyond the limits of the beach and how it touches their personal lives. From these results, we understand this is a singular activity that requires reflection by those who intend to work with it. We claim that sport psychology must include the lived experiences of the practitioners in order to later focus on rules and techniques.

El surf es una actividad ampliamente practicada, que consiste en deslizar en la pared de una ola sobre una plancha de surf. Sin embargo, la vivencia con esta practica va mucho más allá de sus técnicas. El objetivo de este estudio fue comprender como es la experiencia de surfear con base en las percepciones de los propios practicantes. La metodología de inspiración fenomenológica fue utilizada como medio de acceso a esas vivencias, junto con el auxilio de entrevistas abiertas, guiadas por una pregunta disparadora. Fueron entrevistados 8 participantes amateurs, los cuales relataron experiencias vividas en 3 movimientos: antes de entrar en el mar, vivenciando el mar con una plancha y la salida del mar. Evidenciando, así, la necesidad de la preparación para la practica, percepciones de miedo, coraje, placer y contemplación durante la experiencia y la demostración del cuanto esa vivencia extrapola los limites de la playa para sus vidas personales. A partir de los resultados del presente estudio, se entiende que esa modalidad se presenta de forma peculiar, y exige del profesional que se propone a trabajar con el surf una reflexión sobre los aspectos que están implicados. Se defiende aquí una psicología del deporte quesea sensible, inicialmente, a las experiencias vividas de sus practicantes para así, después, ocuparse de reglas y técnicas.

SSM-Based Electrophysiology for Transporter Research.

Functional characterization of transport proteins using conventional electrophysiology can be challenging, especially for low turnover transporters or transporters from bacteria and intracellular compartments. Solid-supported membrane (SSM)-based electrophysiology is a sensitive and cell-free assay technique for the characterization of electrogenic membrane proteins. Purified proteins reconstituted into proteoliposomes or membrane vesicles from cell culture or native tissues are adsorbed to the sensor holding an SSM. A substrate or a ligand is applied via rapid solution exchange. The electrogenic transporter activity charges the sensor, which is recorded as a transient current. The high stability of the SSM allows cumulative measurements on the same sensor using different experimental conditions. This allows the determination of kinetic properties including EC50, IC50, Km, KD, and rate constants of electrogenic reactions. About 100 different transporters have been measured so far using this technique, among them symporters, exchangers, uniporters, ATP-, redox-, and light-driven ion pumps, as well as receptors and ion channels. Different instruments apply this technique: the laboratory setups use a closed flow-through arrangement, while the commercially available SURFE2R N1 resembles a pipetting robot. For drug screening purposes high-throughput systems, such as the SURFE2R 96SE enable the simultaneous measurement of up to 96 sensors.

Um novo barato: surfe e contracultura no Rio de Janeiro dos anos 1970 / Surfing and counter-culture in the 1970s Rio de Janeiro / Surf y contracultura en Río de Janeiro durante la década de 1970

Resumo Este estudo, uma pesquisa histórica, tem por objetivo discutir os encontros que houve no Rio de Janeiro dos anos 1970 de praticantes do surfe e ideias ligadas à contracultura. Para alcance desse objetivo, usamos como fontes depoimentos de surfistas cariocas publicados em livros e periódicos. Pensamos que essa investigação nos permite dar um passo no sentido de melhor entender a relação entre a prática esportiva e o contexto sociocultural. Permite até perceber como os sentidos e significados de um esporte vão mudando no decorrer do tempo. Além disso, esperamos lançar alguns olhares sobre a própria noção de contracultura, se considerarmos que sua interpretação e manifestação foram múltiplas e diversas.

Abstract This study aims to discuss, in the 1970s Rio de Janeiro, the meetings that took place between practitioners of surfeing and ideas related to the counterculture. To reach this aim, we used as sources statements of locals surfers published in books and periodicals. We think that this research allows us to take a step towards better understanding the relationship between sports and sociocultural context, including the giving opportunity to see how the meanings of a sport are changing over time. Furthermore, we hope to shed some light on the notion of counterculture, considering that its interpretation was multiple and diverse.

Resumen Este estudio tiene el objetivo de analizar los encuentros entre practicantes de surf y las ideas relacionadas con la contracultura en la ciudad de Río de Janeiro durante la década de 1970. Para alcanzar este objetivo, hemos utilizado como fuentes las declaraciones de surfistas locales que se publicaron en libros y periódicos. Creemos que esta investigación nos permite dar un paso hacia una mejor comprensión de la relación entre el deporte y el contexto sociocultural, incluyendo la posibilidad de comprobar cómo el concepto que hay detrás de un deporte cambia con el tiempo. Asimismo, esperamos lanzar algunas miradas sobre la propia noción de contracultura al considerar que su interpretación y manifestación son múltiples y diversas.

Functional analysis of Torpedo californica nicotinic acetylcholine receptors in multiple activation states by SSM-based electrophysiology.

Organophosphorus compounds (OPC), i.e. nerve agents or pesticides, are highly toxic due to their strong inhibition potency against acetylcholinesterase (AChE). Inhibited AChE results in accumulation of acetylcholine in the synaptic cleft and thus the desensitisation of the nicotinic acetylcholine receptor (nAChR) in the postsynaptic membrane is provoked. Direct targeting of nAChR to reduce receptor desensitisation might be an alternative therapeutic approach. For drug discovery, functional properties of potent therapeutic candidates need to be investigated in addition to affinity properties. Solid supported membrane (SSM)-based electrophysiology is useful for functional characterisation of ligand-gated ion channels like nAChRs, as charge translocations via capacitive coupling of the supporting membrane can be measured. By varying the agonist (carbamoylcholine) concentration, different functional states of the nAChR were initiated. Using plasma membrane preparations obtained from Torpedo californica electric organ, functional properties of selected nAChR ligands and non-oxime bispyridinium compounds were investigated. Depending on overall-size, the bispyridinium compounds enhanced or inhibited cholinergic signals induced by 100 µM carbamoylcholine. Applying excessive concentrations of the agonist carbamoylcholine provoked desensitisation of the nAChRs, whereas addition of bispyridinium compounds bearing short alkyl linkers exhibited functional recovery of previously desensitised nAChRs. The results suggest that these non-oxime bispyridinium compounds possibly interacted with nAChR subtypes in a manner of a positive allosteric modulator (PAM). The described newly developed functional assay is a valuable tool for the assessment of functional properties of potential compounds such as nAChR modulating ligands, which might be a promising approach in the therapeutically treatment of OPC-poisonings.

Nova proposta de teste incremental de remada na avaliação aeróbia de surfistas / A new proposed incremental surfing paddle test to assess aerobic fitness in surfers

Os objetivos desse estudo foram: 1) verificar as respostas do lactato sanguíneo e da frequência cardíaca (FC) durante um protocolo de campo específico de remada no surfe; 2) correlacionar os índices de capacidade e potência aeróbia determinados nesse protocolo específico com o tempo de prática da modalidade e variáveis antropométricas. Participaram deste estudo nove sujeitos (24 ± 4,5 anos; 72,2 ± 6,7 kg; 178,4 ± 4,8 cm) que foram submetidos a um teste progressivo intermitente de remada sobre a sua própria prancha de surfe, do tipo vai e vêm, com velocidades iniciais entre 1-1,1 m/s e incrementos de 0,05 m/s a cada 3 min até a exaustão voluntária. Uma resposta linear e exponencial foram observadas para a FC e o lactato sanguíneo, respectivamente, durante o protocolo incremental. Este comportamento foi semelhante ao demonstrado durante protocolos incrementais com objetivo de avaliar a capacidade e a potência aeróbia realizados em outras modalidades cíclicas. Além disso, foram encontradas correlações significantes entre o pico de velocidade (PV) e a velocidade correspondente ao início do acúmulo de lactato no sangue (vOBLA) (r = 0,87, p = 0,005) e do PV com tempo de prática de surfe (r = 0,70, p = 0,03). No entanto, não foram encontradas correlações significativas entre PV e vOBLA com nenhuma das variáveis antropométricas mensuradas. Assim, podemos concluir que o protocolo incremental específico de remada no surfe utilizado no presente estudo poderia ser uma ferramenta útil na determinação de índices relacionados à capacidade (vOBLA) e potência (PV) aeróbia de surfistas.

The aim of this study were: 1) to analyse heart rate (HR) and blood lactate (La) responses during a protocol of intermittent surfing paddle on board; 2) to correlate the aerobic capacity and power indexes determined from this specific protocol with the experience in surfing practice and anthropometric variables. Participated in the study nine subjects (24 ± 4.5 years; 72.2 ± 6.7 kg; 178.4 ± 4.8 cm) were submitted to an intermittent incremental shuttle paddle test on the surfboard, with initial velocity between 1 to 1.1 m/s and increments from 0.05 m/s for each 3 min until volitional exhaustion. During the incremental protocol, linear and exponential responses were observed for HR and La, respectively. These responses were similar to those demonstrated during incremental protocols in cyclic exercise modes aiming to assess the aerobic power and capacity. They were found significant correlations between the peak velocity (PV) and velocity at the Onset Blood Lactate Accumulation (vOBLA) (r = 0.87) and between the PV and experience in surfing practice (r = 0.7). However, they were found no significant correlations between PV and vOBLA with anthropometrics variables and weekly training volume. Thus, we conclude that the specific protocol of intermittent surfing paddle could be a useful tool to determine indices related with aerobic power (PV) and capacity (OBLA) of surfers.

Territorial disputes, identity conflicts, and violence in surfing / Disputas territoriais, conflitos de identidade e violência no surfe / Disputas territoriales, conflictos de identidad y la violencia en el surf

Aggressive manifestations of localism are a current concern among surfers and are becoming well known as a result of specialized media. The objective of this paper was to investigate this phenomenon through the examination of a specific case and empirical fieldwork that was conducted for an ethnography of São Paulo surfers. The data were obtained via participant observations and open interviews. The results indicate that conflicts generally begin as disputes over the best waves. Surfing has a general rule of "wave priority criteria," based on spatial positioning. However, this universal rule may be intentionally broken depending on surfers' sociability. Ethnic and class differences based on historical processes can exist in oppositional relationships among surfers and are manifested by categories of accusation or identity (in São Paulo's case, local, haole, roots, prego, and playboy). However, this category attribution is contextual and interchangeable because surfers circulate between groups and beaches while searching for waves.

Manifestações agressivas de localismo são preocupações entre surfistas e se tornam conhecidas pela mídia especializada. O objetivo deste trabalho foi investigar este fenômeno a partir de um caso específico por meio de pesquisa de campo conduzida para a etnografia entre surfistas da cidade de São Paulo. Os dados foram obtidos por observação participante e entrevistas abertas. Os resultados mostram que os conflitos geralmente começam com disputas pelas melhores ondas. O surfe institui uma regra geral de acordo com "critérios de prioridade pela onda" baseada no posicionamento espacial. No entanto, esta regra pode ser desobedecida propositalmente, de acordo com a sociabilidade dos surfistas. Diferenças étnicas e de classe baseadas em processos históricos aparecem como relações de oposição reveladas por categorias de acusação ou identidade (no caso de São Paulo: local, haole, roots, prego e playboy). Entretanto, como os surfistas circulam entre grupos e praias a procura de ondas sua atribuição é contextual e intercambiável.

Manifestaciones agresivas de localismo son una preocupación actual entre los surferos y se están convirtiendo en conocida en los medios especializados. El objetivo de este trabajo fue investigar este fenómeno a través de um caso específico y investigación de campo para la etnografía entre surferos de São Paulo. Los datos fueron obtenidos a través de observación participante y entrevistas abiertas. Los resultados muestran que los conflictos generalmente comienzan por disputas de las mejores olas. El surf tiene una regla general de acuerdo a "criterios de prioridad por la ola" baseados en posicionamento técnico. Sin embargo, esta regla universal puede ser desobedecida a propósito dependiendo de la sociabilidad de los surferos. Diferencias étnicas y de clase sobre la base de los procesos históricos aparecem en relaciones de oposición reveladas por categorías de acusación o de identidad (en el caso de São Paulo: local, haole, roots, prego y playboy). Sin embargo, como los surferos circulan entre grupos e playas en busca de las olas su atribución es contextual e intercambiable.

Qualidade de vida relacionada à prática de atividade física de surfistas / Quality of life related to the practical of physical activity in surfers

Este estudo de corte transversal objetivou investigar a qualidade de vida (QV) relacionada à prática de atividade física de surfistas. A amostragem por conveniência foi de 202 surfistas com média de idade de 25,9±7,5 anos. Optou-se por um questionário autoaplicável. A maioria dos surfistas são solteiros (82%), com ensino médio completo (64%), do estrato econômico B (61%), realizam atividade física regularmente e são considerados muito ativos (83,2%). A QV foi considerada de boa a muito boa, variando de 59,8% a 77%. O domínio social obteve maior escore e o físico o menor. Houve uma fraca associação entre os domínios da QV e os componentes da atividade física (r=-0,105 - r=0,114) não havendo significância, ou seja, a QV, no presente estudo, não foi influenciada pela prática de atividade física. Provavelmente, outros hábitos dos surfistas investigados contribuem de forma mais significativa para o fenômeno QV pesquisado.

The present study aimed at investigating the quality of life (QL) of surfers in regards to their engagement with regular physical activity. The convenience sample was composed of 202 surfers, with mean age of 25,9±7,5 years. The survey method chosen for this research was a self-completion questionnaire. The majority of surfers from our sample are single (82%), have completed secondary school (64%), are economically situated in „B‟ class (61%), are engaged in physical activities regularly and are considered very physically active (83.2%). The QL was considered good to very good, varying from 59.8% to 77%. The social domain received the highest score and the physical the lowest. There was a weak association between the QL domains and the physical activity components (r=-0,105 - r=0,114), with no significance found between the two. This result indicated that the QL, in the present study, was not influenced by the practice of physical activities. Possibly, for the sampled surfers, other habits contribute more significantly to their QL.

"Do outside": corpo e natureza, medo e gênero no surfe universitário paulistano / \"From the outside\": body and nature, fear and gender in surfing

Ao objetivo primeiro desta pesquisa, descrever as dinâmicas do surfe e os significados de sua prática, em especial a relação ser humano/natureza estabelecida por meio do esporte, somaram-se outros objetivos: problematizar a aproximação do pesquisador de seu campo de investigação, a possibilidade de um pesquisador realizar uma investigação através de seu próprio corpo e discutir a questão de gênero no surfe. Sobre o objetivo primeiro desta pesquisa, vivendo e descrevendo as dinâmicas do surfe encontrou-se os significados da relação do surfista com o mar nas sensações corporais experimentadas nas técnicas do remar, sentar, dar o joelhinho e dropar a onda. Que ser capaz de passar a rebentação é associado a um retorno bem sucedido à comunhão do homem com a natureza, sendo as cores, formas e sensações do "outside" o privilégio daquele que vence as dificuldades do tornar-se e ser surfista. Mas, que estas sensações são tidas como possibilidades de corpos corajosos e hábeis, "a priori", entendidos como corpos masculinos. O surfe como campo em que o feminino é visto ainda como exceção dá a pensar que os esportes na natureza e a educação ao ar livre, embora tenham potencial de promover novas condutas políticas e a virtuosa sensibilidade ambiental, não estão livres de reproduzir outros padrões de dominação.

The main goal of this research is to describe the dynamics of surfing and its meanings, mainly the human/nature relation established through the sport. Meanwhile, other goals were added: discussing the approach to the field by the researcher, the possibility this researcher could investigate through her own body and the gender matter in the sport. About the main aim of the research, living and experiencing the sport itself, meaning, to the relation between the surfer and the sea, was found in the body sensations experienced through techniques such as paddling, sitting, duck diving and dropping a wave. Being able to go out is associated to a successful return to man's communion with nature, making outside's colors, shapes and sensations the privilege of whoever transposes the challenges and difficulties of becoming and being a surfer. However, these sensations are held as being only possible for courageous and agile bodies, at first, understood as male ones. Surfing as a field where the feminine is still the exception, allows the thinking that, even though nature sports and outdoor education have the potential to promote new political conducts and environmental sensitivity virtues, they are not free from reproducing other domination standards.

Novos sonhos de verão sem fim: surfe, mulheres e outros modos de representação / New endless summer dreams: surf, women and others representations / Nuevos sueños de verano sin fin: surf, mujeres y otros modos de representación

Este artigo pretende analisar a maneira que o filme Blue Cruch (2002) - no Brasil A onda dos sonhos - captura, representa e difunde sentidos sobre o surfe. O fundamento da iniciativa é o de que filmes como esse, captam o que a prática de esportes simboliza, atribuindo-lhes assim significados que podem ser interpretados a partir deles mesmos. Nesse caso, três elementos do seu enredo foram tomados como eixo de análise: i) o modo de representação da mulher; ii) a crescente comodificação como forma de se relacionar com esta modalidade; iii) a tendência realística-documental dos filmes de surfe. São dimensões que dramatizam dinâmicas culturais desta modalidade, encerrando uma ambivalência que traduz as disputas, clivagens e tensões próprias a qualquer prática cultural.

This article intends to analyze the way that the film Blue Crush (2002) captures, represents and spreads out senses on surf. The premise of this reflection is that the films as themselves catch the practical of sports symbolize, attributing meanings that can be interpreted from that own contends. In this case, three elements of its plot had been taken as analysis axle: i) the way of representation of the woman; ii) the increasing commodification as form of relation with this modality; iii) the realistic-documentary trend of surf films. They are dimensions that they stage dynamic cultural of this modality, locking up an ambivalence that translates the proper disputes and tensions to any practical cultural.

Este artículo se prepone analizar la manera que la película Blue Crush (2002) captura, representa y hace la difusión de sentidos sobre el surf. El fundamento de la iniciativa es que películas como ésta, cogen el simbolismo del deportes, atribuyendo así significados a ellos que se puedan interpretar desde ellos mismos. En esto en caso, tres elementos hubiera sido tomada para su análisis: i) la representación de la mujer; ii) la comodificación cada vez mayor como forma de si se relacionar con esta modalidad; iii) La tendencia realista-documental de las películas de surf. Son dimensiones que dramatizan dinámicas culturales en esta modalidad y demarcan una ambivalencia que traduce los conflictos y las tensiones propria a las practicas culturales.

Consumo máximo de oxigênio em surfistas brasileiros profissionais / Peak oxygen uptake of brazilian professional surfers

O Surfe é um esporte muito popular em todo o mundo, mas há falta de informação dos efeitos fisiológicos induzidos pelo treinamento. Em geral, surfistas têm de remar para alcançar e pegar as ondas, essa fase pode durar de minutos há horas e provavelmente, a capacidade aeróbia dos músculos superiores do corpo pode ser alterada. O objetivo deste estudo foi medir o pico de VO2 de surfistas brasileiros profissionais. Para tal avaliação utilizou-se um ergômetro de alavanca de braço, com intuito de comparar a medida dos valores do pico de VO2 com os valores do VO2max próprios preditos para exercícios de membros inferiores calculados pela equação de Wasserman’s e verificar se o pico de VO2 nos braços pode ser afetado pelo treinamento. Foram estudados oito surfistas do sexo masculino (idade: 26 ± 6 anos, estatura: 175 ± 8 cm, peso corporal: 74 ± 9 kg). O pico de VO2 foi o maior VO2 obtido por um espirômetro de circuito aberto usando uma medição metabólica (V-max Series 229/Sensor Medics, USA) em um teste máximo. Valores medidos de pico de VO2 e preditos de VO2max de surfistas para membros inferiores foram de 3.42 ± 0.46 L.min-1 e 2.87 ± 0.22 L.min-1, respectivamente. Medidas dos valores do pico de VO2em exercício de braço foram significantemente melhores que os valores de VO2max preditos para exercício de perna (120%). Concluí-se que a prática do surfe pode ter um importante efeito induzido pelo treinamento na capacidade aeróbica dos músculos superiores do corpo de surfistas brasileiros profissionais.

Surfing is very popular sport all over the world. But there is lack of data of the physiological training-induced effects of surfing practice. In general, surfers must paddle to reach and catch the waves. And the paddling phase can last from several minutes to few hours. Probably, the aerobic capacity of the upper body muscles could be affected by the surfing practice. Our goals were to measure Brazilian professional surfer`s VO2peak. In an arm cranking ergometer, compare these measured VO2peak values to their own predicted VO2max values for legs exercise calculated by Wasserman`s equation and verify if the arms` VO2peak could be affected by the surfing training. We studied eight Brazilian professional male surfers (age: 26 ± 6 years, height: 175 ± 8 cm, weight: 73 ± 9 kg) that used to train only surfing at least 10 hours per week longer than 10 years. VO2peak was the highest VO2 obtained by an open circuit spirometer using a metabolic measurement cart (V-max Series 229/Sensor Medics, USA) in a maximal incremental test. Surfers` measured VO2peak and predicted VO2max for legs values were 3.42 ± 0.46 L.min-1 and 2.87 ± 0.22 L.min-1, respectively. Measured VO2peak values in arm exercise were significantly greater than predicted VO2max values for leg exercise (120%). We concluded that surfing practice could have an important training-induced effect on the aerobic capacity if the upper body muscles of Brazilian professional surfers.