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1.
Front Physiol ; 13: 981108, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36246108

RESUMEN

Previous studies reported that both a more compliant quadriceps tendon and a stiffer Achilles tendon are associated with better running economy. While tendon stiffness can be decreased by a single bout of proprioceptive neuromuscular facilitation (PNF), post-stretching dynamic activities (PSA) can counteract the potential stretch-induced force loss. Thus, the purpose of this study was to investigate if a single, moderate duration, (4 × 15 s), bout of PNF stretching of either the quadriceps or triceps surae muscles followed each by PSA, causes either an improvement or impairment in running economy. Eighteen trained male runners/triathletes visited the laboratory five times. The first two visits were to familiarize the participants and to test for maximal oxygen consumption (VO2max) respectively. The further three appointments were randomly assigned to either 1.) quadriceps PNF stretching + PSA or 2.) triceps surae PNF stretching + PSA or 3.) no stretching + PSA. Following the interventions, participants performed a 15-min run on the treadmill with a speed reflecting a velocity of 70% VO2max to assess oxygen consumption (i.e., running economy) and running biomechanics. Our results showed neither a difference in oxygen consumption (p = 0.15) nor a change in any variable of the running biomechanics (p > 0.33) during the steady-state (i.e., last 5 min) of the 15-min run. Athletes can perform moderate duration PNF stretching of the quadriceps or triceps surae + PSA prior to a running event, without affecting running economy. Future studies should emphasize long-term training effects on tendon stiffness adaptations and running economy.

2.
Ageing Res Rev ; 67: 101265, 2021 05.
Artículo en Inglés | MEDLINE | ID: mdl-33571702

RESUMEN

This systematic review and meta-analysis aimed to examine the effects of home-based exercise programmes on measures of physical-fitness in healthy older adults. Seventeen randomized-controlled trials were included with a total of 1,477 participants. Results indicated small effects of home-based training on muscle strength (between-study standardised-mean-difference [SMD] = 0.30), muscle power (SMD = 0.43), muscular endurance (SMD = 0.28), and balance (SMD = 0.28). We found no statistically significant effects for single-mode strength vs. multimodal training (e.g., combined balance, strength, and flexibility exercises) on measures of muscle strength and balance. Single-mode strength training had moderate effects on muscle strength (SMD = 0.51) and balance (SMD = 0.65) while multimodal training had no statistically significant effects on muscle strength and balance. Irrespective of the training type, >3 weekly sessions produced larger effects on muscle strength (SMD = 0.45) and balance (SMD = 0.37) compared with ≤3 weekly sessions (muscle strength: SMD = 0.28; balance: SMD = 0.24). For session-duration, only ≤30 min per-session produced small effects on muscle strength (SMD = 0.35) and balance (SMD = 0.34). No statistically significant differences were observed between all independently-computed single-training factors. Home-based exercise appears effective to improve components of health- (i.e., muscle strength and muscular endurance) and skill-related (i.e., muscle power, balance) physical-fitness. Therefore, in times of restricted physical activity due to pandemics, home-based exercises constitute an alternative to counteract physical inactivity and preserve/improve the health and fitness of healthy older adults aged 65-to-83 years.


Asunto(s)
COVID-19 , Entrenamiento de Fuerza , Anciano , Anciano de 80 o más Años , Terapia por Ejercicio , Humanos , Fuerza Muscular , Aptitud Física , SARS-CoV-2
3.
Eur Rev Med Pharmacol Sci ; 25(24): 7847-7857, 2021 12.
Artículo en Inglés | MEDLINE | ID: mdl-34982447

RESUMEN

OBJECTIVE: The Islamic Republic of Iran has displayed one of the highest rates of COVID-19 infection in the world and the highest rate of mortality in the Middle East. Iran has used a stringent package of preventive health measures to mitigate the spread of infection, which however has negatively affected individuals' physical and psychological health. This study aimed at examining whether physical-activity (PA) behavior, anxiety, well-being, and sleep-quality changed in response to the COVID-19-related public health restrictions enforced in Iran. PATIENTS AND METHODS: An online questionnaire was disseminated to adults residing in Iran from November 17, 2020, to February 13, 2021 (~88 days), during Iran's strictest public health restrictions. Main outcome measures included Godin-Shephard Leisure-Time Exercise Questionnaire, General Anxiety Disorder-7, Mental Health Continuum-Short Form, and Pittsburgh Sleep Quality Index. RESULTS: A total of 3,323 adults (mean age 30±11 years, 54.3% female) participated in the survey. Firstly, the restrictions generally reduced PA behavior: (a) among inactive participants (IPs), 60.6% became less active vs. 5.1% who became more active; and (b) among active participants (APs), 49.9% became less active vs. 22.8% who became more active. Secondly, PA behavior was associated with higher well-being and sleep quality during the restrictions: (a) APs reported higher (or lower) levels of well-being and sleep quality (or anxiety) than did IPs; and (b) among IPs as well as among APs, the more active the participants, the greater (or lower) the levels of well-being and sleep quality (or anxiety). CONCLUSIONS: This study showed the beneficial role of PA behavior for well-being, anxiety, and sleep quality during the COVID-19 restrictions, whereas such restrictions appeared to decrease PA participation. Active lifestyle should be then encouraged during the COVID-19 outbreak while taking precautions.


Asunto(s)
Ansiedad/epidemiología , COVID-19/prevención & control , Ejercicio Físico/estadística & datos numéricos , Cuarentena/normas , Calidad del Sueño , Adolescente , Adulto , Ansiedad/diagnóstico , COVID-19/epidemiología , COVID-19/transmisión , Femenino , Humanos , Irán/epidemiología , Masculino , Pandemias/prevención & control , Cuarentena/estadística & datos numéricos , Autoinforme/estadística & datos numéricos , Adulto Joven
5.
Eur J Appl Physiol ; 119(11-12): 2745-2755, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31696316

RESUMEN

PURPOSE: Transcutaneous electrical nerve stimulation (TENS) can reduce acute and chronic pain. Unilateral fatigue can produce discomfort in the affected limb and force and activation deficits in contralateral non-exercised muscles. TENS-induced local pain analgesia effects on non-local fatigue performance are unknown. Hence, the aim of the study was to determine if TENS-induced pain suppression would augment force output during a fatiguing protocol in the treated and contralateral muscles. METHODS: Three experiments were integrated for this article. Following pre-tests, each experiment involved 20 min of TENS, sham, or a control condition on the dominant quadriceps. Then either the TENS-treated quadriceps (TENS_Treated) or the contralateral quadriceps (TENS_Contra) was tested. In a third experiment, the TENS and sham conditions involved two\; 100-s isometric maximal voluntary contractions (MVC) (30-s recovery) followed by testing of the contralateral quadriceps (TENS_Contra-Fatigue). Testing involved single knee extensors (KE) MVCs (pre- and post-test) and a post-test 30% MVC to task failure. RESULTS: The TENS-treated study induced greater (p = 0.03; 11.0%) time to KE (treated leg) failure versus control. The TENS_Contra-Fatigue induced significant (p = 0.04; 11.7%) and near-significant (p = 0.1; 7.1%) greater time to contralateral KE failure versus sham and control, respectively. There was a 14.5% (p = 0.02) higher fatigue index with the TENS (36.2 ± 10.1%) versus sham (31.6 ± 10.6%) conditions in the second fatigue intervention set (treated leg). There was no significant post-fatigue KE fatigue interaction with the TENS_Contra. CONCLUSIONS: Unilateral TENS application to the dominant KE prolonged time to failure in the treated and contralateral KE suggesting a global pain modulatory response.


Asunto(s)
Contracción Isométrica/fisiología , Articulación de la Rodilla/fisiología , Rodilla/fisiopatología , Fatiga Muscular/fisiología , Adulto , Electromiografía/métodos , Femenino , Humanos , Masculino , Fuerza Muscular/fisiología , Músculo Cuádriceps/fisiología , Estimulación Eléctrica Transcutánea del Nervio/métodos , Adulto Joven
6.
HLA ; 91(3): 175-186, 2018 03.
Artículo en Inglés | MEDLINE | ID: mdl-29327506

RESUMEN

Next generation DNA sequencing is used to determine the HLA-A, -B, -C, -DRB1, and -DQB1 assignments of 1472 unrelated volunteers for the unrelated donor registry in Argentina. The analysis characterized all HLA exons and introns for class I alleles; at least exons 2, 3 for HLA-DRB1; and exons 2 to 6 for HLA-DQB1. Of the distinct alleles present, there are 330 class I and 98 class II. The majority (~98%) of the cumulative allele frequency at each locus is contributed by alleles that appear at a frequency of at least 1 in 1000. Fourteen (18.2%) of the 77 novel class I and II alleles carry nonsynonymous variation within their exons; 52 (75.4%) class I novel alleles carry only single, apparently random, nucleotide variation within their introns/untranslated regions. Alleles encoding protein variation not usually detected by typing focused only on the exons encoding the antigen recognition domain are 1.0% of the class I assignments and 7.3% of the class II assignments (predominantly DQB1*02:02:01, DQB1*03:19:01, and DRB1*14:54:01). Updates to the common and well documented list of alleles include 10 alleles previously thought to be uncommon but that are found at least 30 times. Five locus haplotypes estimated using the expectation-maximization algorithm as present 3 or more times total 187. While the known HLA diversity continues to increase, the conservation of known allele sequences is remarkable. Overall, the HLA diversity observed in the Argentinian population reflects its European and Native American ancestry.


Asunto(s)
Variación Genética , Antígenos HLA/genética , Secuenciación de Nucleótidos de Alto Rendimiento/métodos , Sistema de Registros , Alelos , Argentina , Secuencia de Bases , Exones/genética , Frecuencia de los Genes/genética , Sitios Genéticos , Haplotipos/genética , Humanos , Intrones/genética
7.
Scand J Med Sci Sports ; 28(2): 407-417, 2018 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-28628245

RESUMEN

The aims of this study were to compare both eccentric- and concentric-phase adaptations in highly trained handball players to 4 weeks of twice-weekly rebound bench press throw training with varying loads (30%, 50% and 70% of one-repetition maximum [1-RM]) using either known (KL) or unknown (UL) loads and to examine the relationship between changes in eccentric- and concentric-phase performance. Twenty-eight junior team handball players were divided into two experimental groups (KL or UL) and a control group. KL subjects were told the load prior each repetition, while UL were blinded. For each repetition, the load was dropped and then a rebound bench press at maximum velocity was immediately performed. Both concentric and eccentric velocity as well as eccentric kinetic energy and musculo-articular stiffness prior to the eccentric-concentric transition were measured. Results showed similar increases in both eccentric velocity and kinetic energy under the 30% 1-RM but greater improvements under 50% and 70% 1-RM loads for UL than KL. UL increased stiffness under all loads (with greater magnitude of changes). KL improved concentric velocity only under the 30% 1-RM load while UL also improved under 50% and 70% 1-RM loads. Improvements in concentric movement velocity were moderately explained by changes in eccentric velocity (R2 =.23-.62). Thus, UL led to greater improvements in concentric velocity, and the improvement is potentially explained by increases in the speed (as well as stiffness and kinetic energy) of the eccentric phase. Unknown load training appears to have significant practical use for the improvement of multijoint stretch-shortening cycle movements.


Asunto(s)
Adaptación Fisiológica , Contracción Muscular , Músculo Esquelético/fisiología , Entrenamiento de Fuerza , Adolescente , Atletas , Humanos , Masculino
8.
Scand J Med Sci Sports ; 27(10): 1090-1098, 2017 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-27460831

RESUMEN

The purpose of this study was to examine whether drop height-induced changes in leg muscle activity during drop jumps (DJ) are additionally modulated by surface condition. Twenty-four healthy participants (23.7 ± 1.8 years) performed DJs on a force plate on stable, unstable, and highly unstable surfaces using different drop heights (i.e., 20 cm, 40 cm, 60 cm). Electromyographic (EMG) activity of soleus (SOL), gastrocnemius (GM), tibialis anterior (TA) muscles and coactivation of TA/SOL and TA/GM were analyzed for time intervals 100 ms prior to ground contact (preactivation) and 30-60 ms after ground contact [short latency response (SLR)]. Increasing drop heights resulted in progressively increased SOL and GM activity during preactivation and SLR (P < 0.01; 1.01 ≤ d ≤ 5.34) while TA/SOL coactivation decreased (P < 0.05; 0.51 ≤ d ≤ 3.01). Increasing surface instability produced decreased activities during preactivation (GM) and SLR (GM, SOL) (P < 0.05; 1.36 ≤ d ≤ 4.30). Coactivation increased during SLR (P < 0.05; 1.50 ≤ d ≤ 2.58). A significant drop height × surface interaction was observed for SOL during SLR. Lower SOL activity was found on unstable compared to stable surfaces for drop heights ≥40 cm (P < 0.05; 1.25 ≤ d ≤ 2.12). Findings revealed that instability-related changes in activity of selected leg muscles are minimally affected by drop height.


Asunto(s)
Rendimiento Atlético/fisiología , Músculo Esquelético/fisiología , Adulto , Fenómenos Biomecánicos , Electromiografía , Femenino , Humanos , Pierna , Masculino , Propiedades de Superficie , Soporte de Peso , Adulto Joven
9.
Scand J Med Sci Sports ; 26(11): 1301-1312, 2016 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-26633736

RESUMEN

Exercise-induced fatigue can change motor performance in non-exercised muscles. The objective was to investigate unilateral elbow flexion (EF) fatigue effects on the maximal voluntary force (MVC) and corticospinal excitability of contralateral non-exercised biceps brachii (BB). Transcranial magnetic, transmastoid electrical, and brachial plexus electrical stimulation were used to elicit motor evoked potentials (MEP), cervicomedullary motor evoked potentials (CMEP), and compound muscle action potentials in the contralateral non-exercised BB of 12 participants before and after (i) two bouts of 100-s unilateral EF (fatigue) or (ii) control. Three stimuli were evoked every 1.5 s during a series of 6-s isometric EF at 100%, 50%, and 5% of MVC. The non-exercised EF MVC force, electromyographic activity, and voluntary activation were not significantly different between fatigue and control. Non-exercised BB MEP and CMEP amplitudes during 100% MVCs demonstrated significantly higher (P = 0.03) and lower values (P = 0.01), respectively, after fatigue compared with control. There was no difference between the two conditions for MEP and CMEP amplitudes during 50% and 5% MVCs. Unilateral exercise-induced EF fatigue did not lead to cross-over central fatigue to the contralateral homologous muscle but enhanced the supraspinal responsiveness (MEP/CMEP) of the neural circuitries supplying central commands to non-exercised muscles at higher contraction intensity.


Asunto(s)
Potenciales de Acción/fisiología , Ejercicio Físico/fisiología , Lateralidad Funcional/fisiología , Fatiga Muscular/fisiología , Músculo Esquelético/fisiología , Tractos Piramidales/fisiología , Adulto , Brazo , Codo , Electromiografía , Potenciales Evocados Motores , Humanos , Masculino , Adulto Joven
10.
Scand J Med Sci Sports ; 26(1): 48-56, 2016 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25559249

RESUMEN

Cross-sectional studies revealed that inclusion of unstable elements in core-strengthening exercises produced increases in trunk muscle activity and thus potential extra stimuli to induce more pronounced performance enhancements in youth athletes. Thus, the purpose of the study was to investigate changes in neuromuscular and athletic performance following core strength training performed on unstable (CSTU) compared with stable surfaces (CSTS) in youth soccer players. Thirty-nine male elite soccer players (age: 17 ± 1 years) were assigned to two groups performing a progressive core strength-training program for 9 weeks (2-3 times/week) in addition to regular in-season soccer training. CSTS group conducted core exercises on stable (i.e., floor, bench) and CSTU group on unstable (e.g., Thera-Band® Stability Trainer, Togu© Swiss ball) surfaces. Measurements included tests for assessing trunk muscle strength/activation, countermovement jump height, sprint time, agility time, and kicking performance. Statistical analysis revealed significant main effects of test (pre vs post) for trunk extensor strength (5%, P < 0.05, d = 0.86), 10-20-m sprint time (3%, P < 0.05, d = 2.56), and kicking performance (1%, P < 0.01, d = 1.28). No significant Group × test interactions were observed for any variable. In conclusion, trunk muscle strength, sprint, and kicking performance improved following CSTU and CSTS when conducted in combination with regular soccer training.


Asunto(s)
Rendimiento Atlético/fisiología , Fuerza Muscular/fisiología , Entrenamiento de Fuerza/métodos , Fútbol/fisiología , Adolescente , Humanos , Masculino
11.
Int J Sports Med ; 36(1): 75-81, 2015 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-25264860

RESUMEN

This study investigated sex-specific effects of surface instability on kinetics and lower extremity kinematics during drop jumping and landing. Ground reaction forces as well as knee valgus and flexion angles were tested in 14 males (age: 23±2 years) and 14 females (age: 24±3 years) when jumping and landing on stable and unstable surfaces. Jump height was found to be significantly lower (9%, p<0.001) when drop jumps were performed on unstable vs. stable surface. Significantly higher peak ground reaction forces were observed when jumping was performed on unstable versus stable surfaces (5%, p=0.022). Regarding frontal plane kinematics during jumping and landing, knee valgus angles were higher on unstable compared to stable surfaces (19-32%, p<0.05). Additionally, at the onset of ground contact during landings, females showed higher knee valgus angles than males (222%, p=0.027). Sagittal plane kinematics indicated significantly smaller knee flexion angles (6-35%, p<0.05) when jumping and landing on unstable vs. stable surfaces. During drop jumps and landings, women showed smaller knee flexion angles at ground contact compared to men (27-33%, p<0.05). These findings imply that knee motion strategies were modified by surface instability and sex during drop jumps and landings.


Asunto(s)
Planificación Ambiental , Extremidad Inferior/fisiología , Ejercicio Pliométrico , Adulto , Fenómenos Biomecánicos , Femenino , Humanos , Articulación de la Rodilla/fisiología , Masculino , Movimiento , Factores Sexuales , Adulto Joven
12.
J Sports Med Phys Fitness ; 54(3): 279-88, 2014 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-24739290

RESUMEN

Based on the conflicting static stretching (SS) literature and lack of dynamic stretching (DS) literature regarding the effects of differing volumes of stretching on balance, the present study investigated the effects of 4, 8, and 12 sets of SS and DS following a 5 min aerobic running warm-up on the star excursion balance test (SEBT). The objective was to examine an optimal stretch modality and volume to enhance dynamic balance. A randomized, within-subjects experimental design with repeated measures for stretching (SS and DS) versus no-stretching treatment was used to examine the acute effects of 10 (4 sets), 20 (8 sets), and 30 (12 sets) min, of 15s repetitions per muscle of SS and/or DS following a 5 min aerobic warm-up on the performance of the SEBT. Results indicated that a warm-up employing either SS or DS of any volume generally improves SEBT by a "small" amount with effect sizes ranging from 0.06 to 0.50 (11 of 18 conditions>75% likely to exceed the 1.3-1.9% smallest worthwhile change). Secondly, the difference between static and dynamic warm-up on this observed improvement with warm-up improvement was "trivial" to "moderate" (d=0.04 to 0.57) and generally "unclear" (only two of nine conditions>75% likely to exceed the smallest worthwhile change). Finally, the effect of increasing the volume of warm-up on the observed improvement with a warm-up is "trivial" to "small" (d<0.40) and generally "unclear" (only three of 12 conditions>75% likely to exceed the smallest worthwhile change). In summary, an aerobic running warm-up with stretching that increases core and muscle temperature whether it involves SS or DS may be expected to provide small improvements in the SEBT.


Asunto(s)
Rendimiento Atlético , Ejercicios de Estiramiento Muscular/métodos , Equilibrio Postural/fisiología , Femenino , Humanos , Masculino , Rango del Movimiento Articular/fisiología , Reproducibilidad de los Resultados , Encuestas y Cuestionarios , Factores de Tiempo , Adulto Joven
13.
Eur J Appl Physiol ; 114(7): 1413-20, 2014.
Artículo en Inglés | MEDLINE | ID: mdl-24658878

RESUMEN

PURPOSE: Pacing strategies have been reported to occur during continuous cyclical exercises. However, currently no studies have examined if pacing takes place during repeated maximal voluntary muscle contractions (MVCs). Accordingly, the purpose of this study was to examine if informing subjects on the number of MVCs they would perform would affect force and root mean squared electromyography (EMG), during similar fatiguing protocols. METHODS: Thirty well-trained male subjects completed three fatiguing protocols in a randomized order. In the control condition participants were informed they would perform 12 MVCs, and then completed all 12. In the unknown condition they were not told how many MVCs they would perform, but were stopped after 12. Lastly, in the deception condition they were initially told they would perform only 6 MVCs, but after the 6 contractions they were asked to perform a few more repetitions and were stopped after 12. RESULTS: Compared to the unknown condition, subjects demonstrated greater forces (p < 0.05, ES = 0.35-1.14, 2-7.5%) and biceps EMG (p < 0.05, ES = 0.6, 6%) in the deception condition during the first six MVCs. Additionally, under all conditions subjects applied greater forces in the last repetition (#12) relative to the previous one (#11) (p < 0.06, ES = 0.36-0.5, 2.8-3.8%). CONCLUSIONS: The anticipation of performing a certain number of MVCs led the subjects to utilize different pacing strategies. The results also question the assumption that subjects followed the instruction to exert maximal effort during repeated MVCs.


Asunto(s)
Contracción Isométrica , Fatiga Muscular , Músculo Esquelético/fisiología , Resistencia Física , Volición , Adulto , Anticipación Psicológica , Decepción , Electromiografía , Prueba de Esfuerzo , Humanos , Masculino , Terranova y Labrador , Factores de Tiempo , Adulto Joven
14.
Diabetologia ; 56(5): 1155-65, 2013 May.
Artículo en Inglés | MEDLINE | ID: mdl-23344731

RESUMEN

AIMS/HYPOTHESIS: The small, highly conserved vasoactive peptide urotensin II (UII) is upregulated in atherosclerosis. However, its effects in diabetes-associated atherosclerosis have not been assessed. METHODS: Endothelial cells were grown in normal- and high-glucose (5 and 25 mmol/l) media with and without UII (10⁻8 mol/l) and/or the UII receptor antagonist, SB-657510 (10⁻8 mol/l). Apoe knockout (KO) mice with or without streptozotocin-induced diabetes were treated with or without SB-657510 (30 mg kg⁻¹ day⁻¹; n = 20 per group) and followed for 20 weeks. Carotid endarterectomy specimens from diabetic and non-diabetic humans were also evaluated. RESULTS: In high (but not normal) glucose medium, UII significantly increased CCL2 (encodes macrophage chemoattractant protein 1 [MCP-1]) gene expression (human aortic endothelial cells) and increased monocyte adhesion (HUVECs). UII receptor antagonism in diabetic Apoe KO mice significantly attenuated diabetes-associated atherosclerosis and aortic staining for MCP-1, F4/80 (macrophage marker), cyclooxygenase-2, nitrotyrosine and UII. UII staining was significantly increased in carotid endarterectomies from diabetic compared with non-diabetic individuals, as was staining for MCP-1. CONCLUSIONS/INTERPRETATION: This is the first report to demonstrate that UII is increased in diabetes-associated atherosclerosis in humans and rodents. Diabetes-associated plaque development was attenuated by UII receptor antagonism in the experimental setting. Thus UII may represent a novel therapeutic target in the treatment of diabetes-associated atherosclerosis.


Asunto(s)
Aterosclerosis/prevención & control , Diabetes Mellitus Tipo 1/complicaciones , Angiopatías Diabéticas/prevención & control , Endotelio Vascular/efectos de los fármacos , Sustancias Protectoras/uso terapéutico , Receptores Acoplados a Proteínas G/antagonistas & inhibidores , Urotensinas/antagonistas & inhibidores , Animales , Aorta/efectos de los fármacos , Aorta/inmunología , Aorta/metabolismo , Aorta/patología , Aterosclerosis/complicaciones , Aterosclerosis/metabolismo , Aterosclerosis/patología , Adhesión Celular/efectos de los fármacos , Células Cultivadas , Cruzamientos Genéticos , Angiopatías Diabéticas/inmunología , Angiopatías Diabéticas/metabolismo , Angiopatías Diabéticas/patología , Endotelio Vascular/inmunología , Endotelio Vascular/metabolismo , Endotelio Vascular/patología , Células Endoteliales de la Vena Umbilical Humana/efectos de los fármacos , Células Endoteliales de la Vena Umbilical Humana/inmunología , Células Endoteliales de la Vena Umbilical Humana/metabolismo , Células Endoteliales de la Vena Umbilical Humana/patología , Humanos , Masculino , Ratones , Ratones Endogámicos C57BL , Ratones Noqueados , Monocitos/efectos de los fármacos , Monocitos/inmunología , Proyectos Piloto , Sustancias Protectoras/farmacología , Receptores Acoplados a Proteínas G/metabolismo , Sulfonamidas/farmacología , Sulfonamidas/uso terapéutico , Urotensinas/biosíntesis , Urotensinas/metabolismo
15.
Br J Pharmacol ; 161(1): 207-28, 2010 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-20718751

RESUMEN

BACKGROUND AND PURPOSE: Recently identified antagonists of the urotensin-II (U-II) receptor (UT) are of limited utility for investigating the (patho)physiological role of U-II due to poor potency and limited selectivity and/or intrinsic activity. EXPERIMENTAL APPROACH: The pharmacological properties of two novel UT antagonists, GSK1440115 and GSK1562590, were compared using multiple bioassays. KEY RESULTS: GSK1440115 (pK(i)= 7.34-8.64 across species) and GSK1562590 (pK(i)= 9.14-9.66 across species) are high affinity ligands of mammalian recombinant (mouse, rat, cat, monkey, human) and native (SJRH30 cells) UT. Both compounds exhibited >100-fold selectivity for UT versus 87 distinct mammalian GPCR, enzyme, ion channel and neurotransmitter uptake targets. GSK1440115 showed competitive antagonism at UT in arteries from all species tested (pA(2)= 5.59-7.71). In contrast, GSK1562590 was an insurmountable UT antagonist in rat, cat and hUT transgenic mouse arteries (pK(b)= 8.93-10.12 across species), but a competitive antagonist in monkey arteries (pK(b)= 8.87-8.93). Likewise, GSK1562590 inhibited the hU-II-induced systemic pressor response in anaesthetized cats at a dose 10-fold lower than that of GSK1440115. The antagonistic effects of GSK1440115, but not GSK1562590, could be reversed by washout in rat isolated aorta. In ex vivo studies, GSK1562590 inhibited hU-II-induced contraction of rat aorta for at least 24 h following dosing. Dissociation of GSK1562590 binding was considerably slower at rat than monkey UT. CONCLUSIONS AND IMPLICATIONS: Whereas both GSK1440115 and GSK1562590 represent high-affinity/selective UT antagonists suitable for assessing the (patho)physiological role of U-II, only GSK1562590 exhibited sustained UT residence time and improved preclinical efficacy in vivo.


Asunto(s)
Benzamidas/farmacología , Benzoxazinas/farmacología , Receptores Acoplados a Proteínas G/antagonistas & inhibidores , Urotensinas/metabolismo , Animales , Arterias/efectos de los fármacos , Arterias/fisiología , Benzamidas/química , Benzoatos/química , Benzoatos/farmacología , Benzoxazinas/química , Gatos , Línea Celular , Relación Dosis-Respuesta a Droga , Haplorrinos , Humanos , Masculino , Ratones , Ratones Transgénicos , Estructura Molecular , Ensayo de Unión Radioligante , Ratas , Ratas Sprague-Dawley , Receptores Opioides kappa/agonistas , Taquicininas , Vasoconstricción
16.
Br J Pharmacol ; 155(3): 374-86, 2008 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-18587423

RESUMEN

BACKGROUND AND PURPOSE: The recent development of the UT ligand palosuran (1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulphate salt) has led to the proposition that urotensin-II (U-II) plays a significant pathological role in acute and chronic renal injury in the rat. EXPERIMENTAL APPROACH: In the present study, the pharmacological properties of palosuran were investigated further using a series of radioligand binding and functional bioassays. KEY RESULTS: Palosuran functioned as a 'primate-selective' UT ligand in recombinant cell membranes (monkey and human UT K(i) values of 4 +/- 1 and 5 +/- 1 nM), lacking appreciable affinity at other mammalian UT isoforms (rodent and feline K(i) values >1 microM). Paradoxically, however, palosuran lost significant (10- to 54-fold) affinity for native and recombinant human UT when radioligand binding was performed in intact cells (K(i) values of 50 +/- 3 and 276 +/- 67 nM). In accordance, palosuran also exhibited diminished activity in hUT (human urotensin-II receptor)-CHO (Chinese hamster ovary) cells (IC50 323 +/- 67 nM) and isolated arteries (K(b)>10 microM in rat aorta; K(b)>8.5 microM in cat arteries; K(b)>1.6 microM in monkey arteries; K(b) 2.2 +/- 0.6 microM in hUT transgenic mouse aorta). Relative to recombinant binding K(i) values, palosuran was subjected to a 392- to 690-fold reduction in functional activity in monkey isolated arteries. Such phenomena were peculiar to palosuran and were not apparent with an alternative chemotype, SB-657510 (2-bromo-N-[4-chloro-3-((R)-1-methyl-pyrrolidin-3-yloxy)-phenyl]-4,5-dimethoxybenzenesulphonamide HCl). CONCLUSIONS AND IMPLICATIONS: Collectively, such findings suggest that caution should be taken when interpreting data generated using palosuran. The loss of UT affinity/activity observed in intact cells and tissues cf. membranes offers a potential explanation for the disappointing clinical efficacy reported with palosuran in diabetic nephropathy patients. As such, the (patho)physiological significance of U-II in diabetic renal dysfunction remains uncertain.


Asunto(s)
Quinolinas/farmacología , Receptores Acoplados a Proteínas G/efectos de los fármacos , Urea/análogos & derivados , Urotensinas/efectos de los fármacos , Animales , Células CHO , Gatos , Línea Celular , Membrana Celular/efectos de los fármacos , Membrana Celular/metabolismo , Cricetinae , Cricetulus , Humanos , Concentración 50 Inhibidora , Macaca fascicularis , Masculino , Ratones , Quinolinas/administración & dosificación , Ensayo de Unión Radioligante , Ratas , Ratas Sprague-Dawley , Ratas Wistar , Receptores Acoplados a Proteínas G/metabolismo , Especificidad de la Especie , Urea/administración & dosificación , Urea/farmacología , Urotensinas/metabolismo
17.
Eur J Appl Physiol ; 104(3): 515-22, 2008 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-18584200

RESUMEN

The recently reported static stretching impairments found in adults have not been studied in youth. Furthermore, stretch-training effects on sprint performance are equivocal, hence the purpose of this study was to examine the effect of stretch and sprint training on the acute effects of static stretching in 13-15 year olds. A total of 48 students were randomly divided into a sprint only and a stretch and sprint training groups who performed static stretching at the beginning and middle of the speed training sessions (6 weeks). Flexibility tests and 30-m sprints were performed before and after training. Sprint performance was evaluated with and without prior stretching. A main effect indicated that prior static stretching impairs sprint times at 10 (P = 0.01) and 30 m (P = 0.0005). Both groups improved times over 10 (0.7%; P = 0.04) and 30-m (1.5%; P = 0.0007) sprint distance after training. Stretch and sprint trained participants were more resistant to stretch-induced sprint deficits with 3.2% (P < 0.0001), 3.6% (P = 0.0002) and 1.3% (P < 0.0001) faster times at 5, 10, and 30 m, respectively, than the sprint only group. In conclusion, a stretch and sprint training program in 13-15 year olds diminished the detrimental effects of static stretching compared to a sprint only training program.


Asunto(s)
Ejercicio Físico/fisiología , Articulaciones/fisiología , Ejercicios de Estiramiento Muscular , Músculo Esquelético/fisiología , Carrera , Adolescente , Femenino , Humanos , Masculino , Rango del Movimiento Articular , Análisis y Desempeño de Tareas , Factores de Tiempo
18.
Br J Pharmacol ; 152(5): 825-31, 2007 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-17704827

RESUMEN

BACKGROUND AND PURPOSE: Atypical cannabinoids are thought to cause vasodilatation through an as-yet unidentified 'CBx' receptor. Recent reports suggest GPR55 is an atypical cannabinoid receptor, making it a candidate for the vasodilator 'CBx' receptor. The purpose of the present study was to test the hypothesis that human recombinant GPR55 is activated by atypical cannabinoids and mediates vasodilator responses to these agents. EXPERIMENTAL APPROACH: Human recombinant GPR55 was expressed in HEK293T cells and specific GTPgammaS activity was monitored as an index of receptor activation. In GPR55-deficient and wild-type littermate control mice, in vivo blood pressure measurement and isolated resistance artery myography were used to determine GPR55 dependence of atypical cannabinoid-induced haemodynamic and vasodilator responses. KEY RESULTS: Atypical cannabinoids O-1602 and abnormal cannabidiol both stimulated GPR55-dependent GTPgammaS activity (EC50 approximately 2 nM), whereas the CB1 and CB2-selective agonist WIN 55,212-2 showed no effect in GPR55-expressing HEK293T cell membranes. Baseline mean arterial pressure and heart rate were not different between WT and GPR55 KO mice. The blood pressure-lowering response to abnormal cannabidiol was not different between WT and KO mice (WT 20+/-2%, KO 26+/-5% change from baseline), nor was the vasodilator response to abnormal cannabidiol in isolated mesenteric arteries (IC50 approximately 3 micro M for WT and KO). The abnormal cannabidiol vasodilator response was antagonized equivalently by O-1918 in both strains. CONCLUSIONS: These results demonstrate that while GPR55 is activated by atypical cannabinoids, it does not appear to mediate the vasodilator effects of these agents.


Asunto(s)
Cannabidiol/farmacología , Agonistas de Receptores de Cannabinoides , Receptores Acoplados a Proteínas G/agonistas , Vasodilatación/efectos de los fármacos , Animales , Benzoxazinas/farmacología , Presión Sanguínea/efectos de los fármacos , Cannabidiol/análogos & derivados , Línea Celular , Membrana Celular/efectos de los fármacos , Membrana Celular/metabolismo , Femenino , Guanosina 5'-O-(3-Tiotrifosfato)/metabolismo , Frecuencia Cardíaca/efectos de los fármacos , Humanos , Técnicas In Vitro , Masculino , Arterias Mesentéricas/efectos de los fármacos , Arterias Mesentéricas/fisiología , Ratones , Ratones Noqueados , Morfolinas/farmacología , Tono Muscular/efectos de los fármacos , Músculo Liso Vascular/efectos de los fármacos , Músculo Liso Vascular/fisiología , Naftalenos/farmacología , Fenilefrina/farmacología , Cloruro de Potasio/farmacología , Receptores de Cannabinoides/genética , Receptores de Cannabinoides/metabolismo , Receptores Acoplados a Proteínas G/genética , Receptores Acoplados a Proteínas G/metabolismo , Resorcinoles/farmacología
19.
Undersea Hyperb Med ; 30(2): 103-15, 2003.
Artículo en Inglés | MEDLINE | ID: mdl-12964854

RESUMEN

The objective of this study was to investigate the effect of 6 atmospheres of pressure (ATA) on plantar flexors' (PF) voluntary force and activation, force-frequency characteristics, and rate of torque development (RTD). Eight subjects performed PF isometric contractions. Muscle activation was monitored by electromyographic (EMG) activity (PF and dorsiflexors) and the interpolated twitch technique (ITT). Maximal evoked contractions of the PF were elicited at 1, 2, 3, 5, 10, 20, and 40 Hz. PF RTD was calculated with maximal voluntary, 1 and 40 Hz contractions. Hyperbaric pressures significantly decreased PF voluntary torque; 6.2%, ITT activation; 2.8% with a trend for a 19.1% decrease in EMG (p = 0.1). There were no significant differences in the dorsiflexors/PF EMG ratio. One Hz torque was potentiated 15.7% with an increased absolute RTD of 12.8%, but no change in relative RTD. The results suggested hyperbaric-induced decreases in PF activation contributed to voluntary torque loss. A lack of torque reduction with higher frequency tetanic stimulation (2-40 Hz) suggested that 6 ATA does not impair myofilament kinetics, whereas twitch potentiation may include changes in excitation-contraction coupling.


Asunto(s)
Presión Atmosférica , Contracción Muscular/fisiología , Músculo Esquelético/fisiología , Adulto , Fuerza Compresiva , Femenino , Humanos , Masculino
20.
J Sports Med Phys Fitness ; 43(1): 21-7, 2003 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-12629458

RESUMEN

AIM: The interaction between running, stretching and practice jumps during warm-up for jumping tests has not been investigated. The purpose of the present study was to compare the effects of running, static stretching of the leg extensors and practice jumps on explosive force production and jumping performance. METHODS: Sixteen volunteers (13 male and 3 female) participated in five different warm-ups in a randomised order prior to the performance of two jumping tests. The warm-ups were control, 4 min run, static stretch, run + stretch, and run + stretch + practice jumps. After a 2 min rest, a concentric jump and a drop jump were performed, which yielded 6 variables expressing fast force production and jumping performance of the leg extensor muscles (concentric jump height, peak force, rate of force developed, drop jump height, contact time and height/time). RESULTS: Generally the stretching warm-up produced the lowest values and the run or run + stretch + jumps warm-ups produced the highest values of explosive force production. There were no significant differences (p<0.05) between the control and run + stretch warm-ups, whereas the run yielded significantly better scores than the run + stretch warm-up for drop jump height (3.2%), concentric jump height (3.4%) and peak concentric force (2.7%) and rate of force developed (15.4%). CONCLUSION: The results indicated that submaximum running and practice jumps had a positive effect whereas static stretching had a negative influence on explosive force and jumping performance. It was suggested that an alternative for static stretching should be considered in warm-ups prior to power activities.


Asunto(s)
Ejercicio Físico/fisiología , Desempeño Psicomotor/fisiología , Carrera/fisiología , Análisis y Desempeño de Tareas , Adulto , Análisis de Varianza , Electromiografía , Femenino , Humanos , Pierna/fisiología , Masculino , Músculo Esquelético/fisiología , Educación y Entrenamiento Físico/métodos , Práctica Psicológica
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