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1.
Sensors (Basel) ; 24(13)2024 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-39001195

RESUMO

Robot manipulators are robotic systems that are frequently used in automation systems and able to provide increased speed, precision, and efficiency in the industrial applications. Due to their nonlinear and complex nature, it is crucial to optimize the robot manipulator systems in terms of trajectory control. In this study, positioning analyses based on artificial neural networks (ANNs) were performed for robot manipulator systems used in the textile industry, and the optimal ANN model for the high-accuracy positioning was improved. The inverse kinematic analyses of a 6-degree-of-freedom (DOF) industrial denim robot manipulator were carried out via four different learning algorithms, delta-bar-delta (DBD), online back propagation (OBP), quick back propagation (QBP), and random back propagation (RBP), for the proposed neural network predictor. From the results obtained, it was observed that the QBP-based 3-10-6 type ANN structure produced the optimal results in terms of estimation and modeling of trajectory control. In addition, the 3-5-6 type ANN structure was also improved, and its root mean square error (RMSE) and statistical R2 performances were compared with that of the 3-10-6 ANN structure. Consequently, it can be concluded that the proposed neural predictors can successfully be employed in real-time industrial applications for robot manipulator trajectory analysis.

2.
Sensors (Basel) ; 24(9)2024 Apr 26.
Artigo em Inglês | MEDLINE | ID: mdl-38732858

RESUMO

Nowadays, trajectory control is a significant issue for unmanned micro aerial vehicles (MAVs) due to large disturbances such as wind and storms. Trajectory control is typically implemented using a proportional-integral-derivative (PID) controller. In order to achieve high accuracy in trajectory tracking, it is essential to set the PID gain parameters to optimum values. For this reason, separate gain values are set for roll, pitch and yaw movements before autonomous flight in quadrotor systems. Traditionally, this adjustment is performed manually or automatically in autotune mode. Given the constraints of narrow orchard corridors, the use of manual or autotune mode is neither practical nor effective, as the quadrotor system has to fly in narrow apple orchard corridors covered with hail nets. These reasons require the development of an innovative solution specific to quadrotor vehicles designed for constrained areas such as apple orchards. This paper recognizes the need for effective trajectory control in quadrotors and proposes a novel neural network-based approach to tuning the optimal PID control parameters. This new approach not only improves trajectory control efficiency but also addresses the unique challenges posed by environments with constrained locational characteristics. Flight simulations using the proposed neural network models have demonstrated successful trajectory tracking performance and highlighted the superiority of the feed-forward back propagation network (FFBPN), especially in latitude tracking within 7.52745 × 10-5 RMSE trajectory error. Simulation results support the high performance of the proposed approach for the development of automatic flight capabilities in challenging environments.

3.
Sensors (Basel) ; 23(13)2023 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-37448020

RESUMO

Nowadays, Convolution Neural Network (CNN) based deep learning methods are widely used in detecting and classifying fruits from faults, color and size characteristics. In this study, two different neural network model estimators are employed to detect apples using the Single-Shot Multibox Detection (SSD) Mobilenet and Faster Region-CNN (Faster R-CNN) model architectures, with the custom dataset generated from the red apple species. Each neural network model is trained with created dataset using 4000 apple images. With the trained model, apples are detected and counted autonomously using the developed Flying Robotic System (FRS) in a commercially produced apple orchard. In this way, it is aimed that producers make accurate yield forecasts before commercial agreements. In this paper, SSD-Mobilenet and Faster R-CNN architecture models trained with COCO datasets referenced in many studies, and SSD-Mobilenet and Faster R-CNN models trained with a learning rate ranging from 0.015-0.04 using the custom dataset are compared experimentally in terms of performance. In the experiments implemented, it is observed that the accuracy rates of the proposed models increased to the level of 93%. Consequently, it has been observed that the Faster R-CNN model, which is developed, makes extremely successful determinations by lowering the loss value below 0.1.


Assuntos
Aprendizado Profundo , Malus , Procedimentos Cirúrgicos Robóticos , Redes Neurais de Computação , Frutas
4.
J Biochem Mol Toxicol ; 34(9): e22542, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32578930

RESUMO

Taxane-based chemotherapy drugs (cabazitaxel, docetaxel, and paclitaxel) are microtubule inhibitors, which are effectively and frequently used to treat metastatic prostate cancer (PCa). Among these, cabazitaxel is offered as a new therapeutic option for patients with metastatic castration-resistant PC as that are resistant to other taxanes. Here, we investigated the cellular and molecular changes in response to cabazitaxel in comparison with docetaxel and paclitaxel in androgen-independent human PCas. The androgen-independent human PCa cell lines, PC3 and DU145, were treated with 1 to 5nM cabazitaxel, docetaxel, or paclitaxel, and assessed for cell viability (MTT assay), colony forming ability and migration (scratch assay). The induction of apoptosis was determined through measurement of mitochondrial membrane potential (JC-1 assay) and caspase-3 activity assay. The protein expression changes (caspase-3, caspase-8, Bax, Bcl-2, ß-tubulin, nuclear factor-κB [NF-κB/p50, NF-κB/p65], vascular endothelial growth factor, WNT1-inducible signaling pathway protein-1 [WISP1], transforming growth factor ß [TGF-ß]) in response to drug treatment were screened via western blotting. Under our experimental conditions, all taxanes significantly reduced WISP1 and TGF-ß expressions, suggesting an anti-metastatic/antiangiogenic effect for these drugs. On the other hand, cabazitaxel induced more cell death and inhibited colony formation compared to docetaxel or paclitaxel. The highest fold change in caspase-3 activity and Bax/Bcl-2 ratio was also detected in response to cabazitaxel. Furthermore, the induction of ß-tubulin expression was lower in cabazitaxel-treated cells relative to the other taxanes. In summary, cabazitaxel shows molecular changes in favor of killing PCa cells compared to other taxanes, at least for the parameters analyzed herein. The differences with other taxanes may be important while designing other studies or in clinical settings.

5.
Andrologia ; 50(8): e13062, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-29920739

RESUMO

The purpose of this study was to compare the effects of nebivolol on nonadrenergic noncholinergic (NANC) relaxation functions that are mediated by electric field stimulation (EFS) in rabbit corpus cavernosum smooth muscle by comparison with other beta-adrenergic receptor blockers and show the level on which its effects through nitric oxide take place. After the effects of nebivolol on the isolated corpus cavernosum tissues that were contracted through the alpha-adrenergic pathway and application of L-NAME' (NG -nitro-L-arginine methyl ester) which is a competitive inhibitor of nitric oxide synthase (NOS), the changes that occurred were recorded. Following the effect on the tissue that was contracted with phenylephrine in the presence of atropine and guanethidine that was created by EFS, nebivolol and other beta-blockers were added and the changes were recorded. After receiving relaxation responses with EFS-mediated NANC, no difference was observed between the relaxation responses due to addition of nebivolol and other beta-adrenergic blockers (p > 0.05). The finding that nebivolol which has a NO-mediated relaxation effect did not have an effect on EFS-mediated NANC relaxation but created relaxation on the tissue that was contracted by phenylephrine and the effect was reversed by L-NAME, shows that its effects are on a postsynaptic level.


Assuntos
Agonistas de Receptores Adrenérgicos beta 1/farmacologia , Relaxamento Muscular/efeitos dos fármacos , Músculo Liso Vascular/efeitos dos fármacos , Nebivolol/farmacologia , Pênis/efeitos dos fármacos , Animais , Avaliação Pré-Clínica de Medicamentos , Masculino , Coelhos
6.
Arch Ital Urol Androl ; 86(1): 33-8, 2014 Mar 28.
Artigo em Inglês | MEDLINE | ID: mdl-24704929

RESUMO

OBJECTIVE: Hypercholesterolaemia promotes erectile dysfunction through increased superoxide formation and decreased nitric oxide bioactivity in cavernosal tissue. The role of nitric oxide on erectile function is well known. Statins have lipid lowering properties and can modulate endothelial nitric oxide bioavailability. Sildenafil, enhances smooth muscle relaxation in corpus cavernosum. We investigated in-vitro effects of sildenafil and rosuvastatin on nonadrenergic, non-cholinergic and nitric oxide mediated cavernosal smooth muscle relaxation in metabolic syndrome rabbits, since alterations in this pathway are recognised in diabetic and hypercholesterolemic erectile dysfunction. METHODS: Ten male rabbits were fed a standard diet as control group, fourty male rabbits were fed a hypercholesterolemic diet for 12 weeks. Hypercholesterolemic group were divided for without treatment, rosuvastatin treatment, sildenafil treatment, and rosuvastatin + sildenafil treatment (N = 10 per groups). RESULTS: Serum levels of cholesterol and glucose were significantly higher in the experimental group than in the control group (p < 0.05). After therapy no differences were found among the groups in relaxation responses to sodium nitroprusside. The relaxation responses to carbachol and EFS were significantly reduced in metabolic syndrome group to control group (p < 0.05), but there were no differences between the other groups and control group. There was a significantly lower in-vitro relaxation response in the metabolic syndrome rabbits than in controls and the others (p < 0.05). CONCLUSION: Both agents improve in-vitro relaxation responses of erectile tissue from metabolic syndrome rabbits to endothelial non-adrenergic, non-cholinergic and nitric oxide. This finding supports to the results of other clinical studies with these drugs.


Assuntos
Fluorbenzenos/farmacologia , Inibidores de Hidroximetilglutaril-CoA Redutases/farmacologia , Relaxamento Muscular/efeitos dos fármacos , Miócitos de Músculo Liso/efeitos dos fármacos , Pênis/efeitos dos fármacos , Inibidores da Fosfodiesterase 5/farmacologia , Piperazinas/farmacologia , Pirimidinas/farmacologia , Sulfonamidas/farmacologia , Sulfonas/farmacologia , Animais , Modelos Animais de Doenças , Técnicas In Vitro , Masculino , Síndrome Metabólica , Contração Muscular/efeitos dos fármacos , Purinas/farmacologia , Coelhos , Rosuvastatina Cálcica , Citrato de Sildenafila
7.
Exp Lung Res ; 38(8): 420-6, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-23030645

RESUMO

Asthma is a chronic inflammatory disease in which cell components play important roles. We aimed to evaluate the effects of NO/cGMP cleavage at trachea preparations isolated from ovalbumin-sensitized guinea pigs in vitro. Trachea rings were exposed to 3-ethyl-3-(ethylaminoethyl)-1-hydroxy-2-oxo-1-triazene (NOC-12), (±)-(E)-4-ethyl-2-[(Z)-hydroxyimino]-5-nitro-3-hexen-1-yl-nicotinamide (NOR-4), 2-(2-methylpyridin-4-yl)methyl-4-(3,4,5-trimethoxyphenyl)-8-(pyrimidin-2-yl) methoxy-1,2-dihydro-1-oxo-2,7-naphthyridine-3-carboxylic acid methyl ester hydrochloride (T-0156), and electrical field stimulation (EFS). cGMP levels in trachea tissues were also measured. The relaxation responses of NOC-12, NOR-4, T-0156, and EFS were significantly decreased at ovalbumin-sensitized group. Nitric oxide (NO) donors significantly decreased the relaxation responses in the presence of 1H-[1,2,4] oxadiazolo [4,3-a] quinoxalin-1-one (ODQ). L-Nitro-Arginine Methyl Ester (L-NAME) significantly decreased the EFS relaxation responses in both groups (experimental group and control group), but this effect was reversed by L-Arginine addition. In the experimental group, cGMP levels after EFS, carbachol, NOC-12, NOR-4, and T-0156 exposure were significantly lower than control group. In both groups, cGMP levels after NO donors' exposure were significantly lower in the presence of ODQ and the cGMP levels after EFS + L-NAME were significantly lower than EFS alone. These results may show the increased formation of NO because of the increased iNOS activity in airway sensitization leading to the inhibition of cNOS resulting in the decrease of endogen NO and decrease of activation of guanylyl cyclase.


Assuntos
Asma/tratamento farmacológico , Broncodilatadores/farmacologia , GMP Cíclico/metabolismo , Músculo Liso/efeitos dos fármacos , Óxido Nítrico/metabolismo , Traqueia/efeitos dos fármacos , Animais , Asma/induzido quimicamente , Asma/fisiopatologia , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Cobaias , Técnicas In Vitro , Contração Isométrica/efeitos dos fármacos , Masculino , Músculo Liso/imunologia , Naftiridinas/farmacologia , Doadores de Óxido Nítrico/farmacologia , Compostos Nitrosos/farmacologia , Ovalbumina/imunologia , Piridinas/farmacologia , Pirimidinas/farmacologia , Traqueia/fisiologia
8.
Curr Ther Res Clin Exp ; 72(5): 195-203, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-24653506

RESUMO

BACKGROUND: Pancuronium, vecuronium, rocuronium, and mivacurium are nondepolarizing neuromuscular blocking agents that affect the cardiovascular system with different potencies. Their cardiovascular effects are clinically significant in the anesthetic management of patients, particularly those undergoing cardiac surgery. OBJECTIVE: We aimed to compare the cardiac effects of these compounds, such as heart rate and developed force, in one species under identical experimental conditions in isolated rat atria. METHODS: The left or right atria of rats were removed and suspended in organ baths. Pancuronium, vecuronium, rocuronium, or mivacurium were added cumulatively (10(-9)-10(-5) M) in the presence and absence of the nonselective ß-blocker propranolol (10(-8) M) and the noradrenaline reuptake inhibitor desipramine (10(-7) M), and heart rate changes were recorded in spontaneously beating right atria. Left atrial preparations were stimulated by electrical field stimulation using a bipolar platinum electrode, and the effects of cumulative concentrations of these nondepolarizing neuromuscular blocking agents on the developed force in the presence and absence of propranolol (10(-8) M) and desipramine (10(-7) M) were recorded. RESULTS: Pancuronium increased heart rate in a dose-dependent manner compared with the control group (P < 0.027). Vecuronium, rocuronium, and mivacurium also increased heart rate in a dose-dependent manner, but the changes were not statistically significant. Although propranolol decreased the pancuronium heart rate effect (P < 0.05), it did not change the heart rate effects with vecuronium, rocuronium, or mivacurium. Desipramine did not change the heart rate effects of vecuronium, rocuronium, mivacurium, or pancuronium. All 4 drugs increased developed force in a dose-dependent manner; the increases were significant at 10(-5) M concentration for pancuronium and at 10(-6) and 10(-5) M concentrations for vecuronium, rocuronium, and mivacurium (P < 0.038). These increases in developed force were abolished with the addition of propranolol. Desipramine did not change the developed force effects of any of the 4 drugs. CONCLUSIONS: The heart rate effect of pancuronium and developed force effects of pancuronium, vecuronium, rocuronium, and mivacurium may occur via direct stimulation of ß receptors. Although our investigation was an in vitro study, the effects found may be important especially under pathologic conditions, such as hypertension, in which patients usually use ß-blocking agents, which cause ß receptor upregulation.

9.
J Surg Res ; 155(1): 70-6, 2009 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-19394644

RESUMO

BACKGROUND: Common bile duct ligation (CBDL) produces gallbladder distension and acute inflammation similar to that seen in human acute acalculous cholecystitis. CBDL in the guinea pig affects smooth muscle contractility. The aim of this study was to determine whether the nitric oxide-L-arginine pathway plays a role in the inflammatory process and abnormal gallbladder contractility that occur after CBDL. MATERIALS AND METHODS: Contractility of gallbladder muscle from CBDL and sham-operated guinea pigs was studied in vitro. Animals were treated with saline, aminoguanidine (AG), or an aminoguanidine + L-arginine combination (AG + L-Arg) in vivo. Potassium chloride, carbachol, and electric field stimulation (EFS) were used for contracting the gallbladder muscle strips or activating intrinsic nerves. Hematoxylin and eosin-stained slides of muscle strips were scored for inflammation. RESULTS: Contraction responses to carbachol and EFS were decreased significantly in CBDL guinea pigs compared with those in the sham-operated group. AG partly reversed the smooth muscle contractile response to carbachol and EFS, but did not reduce the inflammation score. Treatment with AG + L-arg did not reverse either the contraction response or the inflammation score. CONCLUSIONS: These findings suggest that AG and AG + L-Arg treatments have no beneficial effect on inflammation in guinea pigs after CBDL, although AG significantly reversed the effect on muscle contractility (P < 0.05). This improvement was independent of inflammation and may be due to a decreased level of NO and its diminished relaxant effect.


Assuntos
Arginina/metabolismo , Colecistite/metabolismo , Vesícula Biliar/fisiopatologia , Músculo Liso/fisiopatologia , Óxido Nítrico/metabolismo , Animais , Carbacol , Ducto Colédoco/cirurgia , Estimulação Elétrica , Guanidinas , Cobaias , Técnicas In Vitro , Ligadura , Masculino , Contração Muscular , Óxido Nítrico Sintase Tipo II/antagonistas & inibidores , Cloreto de Potássio
10.
Eur J Anaesthesiol ; 26(2): 155-9, 2009 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-19142091

RESUMO

BACKGROUND AND OBJECTIVE: Pancuronium, vecuronium, mivacurium and rocuronium are nondepolarizing neuromuscular blocking agents, which are competitive antagonists against acetylcholine at nicotinic receptors, and considered to have no direct actions on vascular smooth muscle. We aimed to investigate the relaxant effects and possible underlying mechanisms of these agents on isolated rat thoracic aorta. METHODS: The preparations were precontracted with prostaglandin F2alpha (10(-7) mol l(-1)) and pancuronium (10(-7)-10(-4) mol l(-1)), rocuronium (10(-7)-10(-4) mol l(-1)), vecuronium (10(-7)-10(-4) mol l(-1)) and mivacurium (10(-7)-10(-4) mol l(-1)) added at cumulative concentrations in the presence or absence of a prostaglandin synthesis inhibitor, indomethacin (10(-6) M), and a nitric oxide synthesis inhibitor, N(omega)-nitro-L-arginine methylester (3 x 10(-5)). The same protocol was applied to both endothelia (+) and endothelia (-) aortic rings. The preparations precontracted with prostaglandin F2alpha (10(-7) mol l(-1)) were stimulated with electrical field stimulation at a frequency of 10 Hz as square-wave pulses of 50 V (0.2 ms) in the presence of a noradrenaline reuptake inhibitor desipramine (10(-7) mol l(-1)) and a nonselective beta-blocker propranolol (10(-6) mol l(-1)). Drugs were added at ineffective concentration of 10(-7) mol l(-1). Tetrodotoxin (10(-7) mol l(-1)) was added to test whether the changes were dependent on the neuronal response. RESULTS: Pancuronium and rocuronium relaxed aortic rings precontracted by prostaglandin F2alpha in a dose-dependent manner, but vecuronium and mivacurium did not. The relaxation effect of pancuronium and rocuronium was endothelium independent because there was not a significant response difference from the endothelium-denuded group. CONCLUSION: In conclusion, their relaxation effect may be due to an increase in prostaglandin synthesis. The increased relaxation effect of these agents at electrical field stimulation may be by the decreasing effect of noradrenaline reuptake from nerve endings because a noradrenaline reuptake inhibitor desipramine did not change this effect. Also, these neuromuscular agents may affect beta-receptors, because a nonselective beta-blocker agent, propranolol, decreased their electrical field stimulation-induced relaxations.


Assuntos
Androstanóis/farmacologia , Aorta Torácica/efeitos dos fármacos , Isoquinolinas/farmacologia , Pancurônio/farmacologia , Brometo de Vecurônio/farmacologia , Animais , Masculino , Mivacúrio , Ratos , Ratos Wistar , Rocurônio
11.
World J Gastroenterol ; 14(29): 4667-71, 2008 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-18698681

RESUMO

AIM: To investigate the tolerance development against the relaxant effect of nitric oxide donating drug isosorbide dinitrate (ISDN) and sodium nitroprusside (SNP) in internal anal sphincter (IAS) smooth muscle. METHODS: Relaxation responses of ISDN, and electrical field stimulation (EFS) were obtained before and after tolerance induction by ISDN incubation. RESULTS: ISDN (10(-7)-10(-4) mol/L) and SNP (10(-8)-10(-4) mol/L) caused a concentration-dependent relaxation on the basal tonus of the isolated rabbit IAS strips. After a period of 2 h incubation of the 6 multiply 10(-4) mol/L ISDN the relaxation effects of ISDN and SNP did not change compared to control strips. EFS evoked frequency-dependent relaxation in internal anal sphincter smooth muscle and E(max) obtained from control strips were not changed in ISDN tolerance-inducing condition. In this study nitrate tolerance was not observed in rabbit IAS smooth muscle. CONCLUSION: This result shows that nitric oxide donating drugs relaxes the internal anal sphincter of the rabbits without the development of tolerance.


Assuntos
Canal Anal/efeitos dos fármacos , Dinitrato de Isossorbida/farmacologia , Relaxamento Muscular/efeitos dos fármacos , Nitratos/farmacologia , Doadores de Óxido Nítrico/farmacologia , Nitroprussiato/farmacologia , Canal Anal/fisiologia , Animais , Modelos Animais , Relaxamento Muscular/fisiologia , Músculo Liso/efeitos dos fármacos , Músculo Liso/fisiologia , Coelhos
12.
Food Chem Toxicol ; 46(6): 2124-7, 2008 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-18353519

RESUMO

Aflatoxins are a group of mycotoxins produced by toxigenic strains of Aspergillusflavus, Aspergillusparasiticus and Aspergillusnomius as secondary metabolites. Most of the studies on the aflatoxins have focused mainly on their chronic toxic effects but aflatoxins have also a lot of acute effects on the respiratory, cardiovascular and gastrointestinal systems. In this study the acute gastrointestinal effects of the aflatoxins on rat isolated ileum and the possible mechanisms underlying contractile responses to them were investigated. Aflatoxin increased both of the amplitude and the frequency of spontaneous contractions in a dose-dependent manner. Pretreatment with a cholinergic system inhibitor, atropine sulfate (23.6nM), a specific sodium-channel blocker, tetrodotoxin (0.3microM) and an inhibitor of ACh release from terminal motor neurons, morphine (0.3microM) decreased both of aflatoxin induced spontaneous contractions' amplitude and frequency, in contrast a nicotinic ganglionic blocker, hexamethonium chloride (55microM) did not change the aflatoxin effect. But the decrease of amplitude was more than the frequency in the presence of these antagonists. In conclusion, these findings of aflatoxin on isolated rat ileum may explain their acute gastrointestinal effects in humans and animals.


Assuntos
Aflatoxinas/farmacologia , Íleo/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Acetilcolina/metabolismo , Analgésicos Opioides/farmacologia , Animais , Atropina/farmacologia , Relação Dose-Resposta a Droga , Motilidade Gastrointestinal/efeitos dos fármacos , Hexametônio/farmacologia , Técnicas In Vitro , Contração Isométrica/efeitos dos fármacos , Masculino , Morfina/farmacologia , Antagonistas Muscarínicos/farmacologia , Antagonistas Nicotínicos/farmacologia , Ratos , Ratos Wistar , Bloqueadores dos Canais de Sódio/farmacologia , Tetrodotoxina/farmacologia
13.
Food Chem Toxicol ; 46(8): 2876-80, 2008 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-18620790

RESUMO

Aflatoxins are one of the most potent toxic, mutagenic, teratogenic, cancerogenic, and immunosuppresive substances that naturally occurring contaminants of food. There are some studies in various animal species that have reported aflatoxin effects on gastrointestinal systems, but acute effects of aflatoxins have not been clearly investigated. In this study, we aimed to investigate the acute gastrointestinal effects of total aflatoxin on rat isolated proximal and distal colon. Aflatoxin was given cumulatively at 10(-8)-10(-5)M concentrations and the amplitude and frequency of proximal and distal colon contractions were increased significantly. In the presence of atropine sulfate (23.6 nM) and morphine (0.3 microM) the amplitude and frequency of aflatoxin induced spontan contractions in the proximal and distal colon decreased significantly, on the other hand, L-NNA (0.3 microM) increased contractions' amplitude and frequency significantly in the proximal colon but not in the distal colon. In conclusion, aflatoxin may increase the amplitude and frequency of contractions by increasing muscarinic activity or by decreasing NO synthase and/or release in proximal colon and by increasing muscarinic activity in the distal colon. These findings of aflatoxin on isolated rat proximal and distal colon may explain their acute gastrointestinal effects in humans and animals.


Assuntos
Aflatoxinas/toxicidade , Colo/efeitos dos fármacos , Contração Muscular/efeitos dos fármacos , Músculo Liso/efeitos dos fármacos , Analgésicos Opioides/farmacologia , Animais , Atropina/farmacologia , Inibidores Enzimáticos/farmacologia , Contração Isométrica/efeitos dos fármacos , Masculino , Morfina/farmacologia , Antagonistas Muscarínicos/farmacologia , NG-Nitroarginina Metil Éster/farmacologia , Óxido Nítrico Sintase/antagonistas & inibidores , Cloreto de Potássio/farmacologia , Ratos , Ratos Wistar
14.
Anadolu Kardiyol Derg ; 6(1): 34-8, 2006 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-16524798

RESUMO

OBJECTIVE: In this study, the effect of agmatine was studied on sympathetic neurotransmission in the frog isolated ventricular strips. METHODS: Ventricular strips were prepared from the heart of the pitched frog. Each strip was mounted vertically in an organ bath. Muscle contractions were recorded isometrically by a force displacement transducer and displayed on a polygraph. RESULTS: Concentration-response relationships to noradrenaline were obtained on contractility of frog ventricular strips evoked by electrical stimulation. The responses of noradrenaline were re-obtained in presence of agmatine (3X10(-4) M). Agmatine was found to be ineffective on contractile responses of noradrenaline in electrically driven ventricular strips of frog heart. Transient additional stimulations (TAS) induced contractions. The contractions induced by TAS were re-obtained in presence of agmatine, idazoxan + agmatine and yohimbine + agmatine. Agmatine significantly increased the positive inotropic responses of TAS. The effect of agmatine on contractile responses of TAS was not changed by idazoxan, indicating that imidazoline receptors have not functions in this response. The effect of agmatine on the contractile responses to TAS was reversed by yohimbine, indicating involvement of alpha2 adrenoceptors in this response. Agmatine did not change the contractile responses of ventricular strips to exogenous noradrenaline, indicating that agmatine does not affect postjunctional adrenoceptors. CONCLUSION: These results suggest that agmatine facilitates sympathetic neurotransmission in frog myocardium via an action on prejunctional alpha2 adrenergic receptors located on sympathetic nerve terminals.


Assuntos
Agmatina/farmacologia , Contração Miocárdica/efeitos dos fármacos , Miocárdio/metabolismo , Receptores Adrenérgicos alfa/metabolismo , Transmissão Sináptica/efeitos dos fármacos , Fibras Adrenérgicas/efeitos dos fármacos , Antagonistas Adrenérgicos alfa/farmacologia , Animais , Relação Dose-Resposta a Droga , Estimulação Elétrica , Norepinefrina/farmacologia , Rana temporaria , Receptores Adrenérgicos alfa/efeitos dos fármacos , Técnicas de Cultura de Tecidos , Ioimbina/farmacologia
15.
Eur J Obstet Gynecol Reprod Biol ; 202: 45-50, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-27160814

RESUMO

OBJECTIVES: Rho-kinases (ROCKs), are one of the dynamic structures of the actin cytoskeleton and they mediate different biological processes, including regulation of calcium sensitivity of smooth muscle contraction. The activation of Rho A/ROCK system is thought to be effective on the termination time of the pregnancy process. The aim of this study, was to investigate in vitro effects of the ROCK enzyme inhibitors, clinically available fasudil hydrochloride, and a new promising inhibitor AS1892802, on the contractions of isolated pregnant rat myometrium. STUDY DESIGN: Term pregnant Wistar albino rats (n=12), weighing 200-220g, were used in this study. Myometrial tissues obtained from rats were dissected into four full-thickness longitudinal muscle strips and then myometrial tension was recorded isometrically. The inhibitory effects of cumulative concentrations of AS1892802 and of fasudil hydrochloride in the presence and absence of ODQ (guanylate cyclase inhibitor), l-NAME (nitric oxide synthase inhibitor) and l-NNA (endothelial nitric oxide synthase inhibitor) on oxytocin-induced myometrial contractions were measured, and values for -log10EC50 (pD2) and mean maximal inhibition (Emax) were compared. RESULTS: Both ROCK inhibitors, AS1892802 and fasudil hydrochloride starting from the concentrations of 10(-6)M reached statistical significance on contraction amplitude and frequency of myometrial strips (p<0.05). The inhibition of the amplitude and frequency of myometrial contractions was antagonized with ODQ (10(-5)M; only amplitude), l-NAME (3×10(-5)M) and l-NNA (10(-5)M) (p<0.05). CONCLUSION: These results suggest that fasudil hydrochloride and AS1892802 may contribute to the development of new tocolytic drugs. We conclude that AS1892802 and fasudil hydrochloride perform this inhibitory effect partially through ROCK inhibition and the NO/cGMP pathway.


Assuntos
1-(5-Isoquinolinasulfonil)-2-Metilpiperazina/análogos & derivados , Miométrio/efeitos dos fármacos , Compostos de Fenilureia/farmacologia , Inibidores de Proteínas Quinases/farmacologia , Piridinas/farmacologia , Contração Uterina/efeitos dos fármacos , Quinases Associadas a rho/antagonistas & inibidores , 1-(5-Isoquinolinasulfonil)-2-Metilpiperazina/farmacologia , Animais , Feminino , Gravidez , Ratos , Ratos Wistar
16.
J Oral Sci ; 58(3): 339-45, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27665972

RESUMO

The study aimed to evaluate the effects of different post morphologies and placement lengths on the fracture resistance of teeth with oval canal morphology that had been restored with crowns. Extracted mandibular premolars with similar dimensions were decoronated. After the root canal treatment, the teeth were mounted on acrylic blocks. Samples were randomly divided into four groups (n = 10 each). In groups C-10 and C-5, 10-mm- and 5-mm-long circular post spaces were created. In groups O-10 and O-5, 10-mm- and 5-mm-long oval post spaces were ultrasonically created. After post cementation, all specimens were restored with composite cores and prepared at height of 6 mm. Thereafter, all teeth were restored with crowns. After thermocycling, all specimens underwent fracture resistance testing. Oval posts and placement at 10-mm depth showed higher fracture resistance than circular posts and placement at 5-mm depth (P < 0.001). Increased post length and use of oval posts enhanced the fracture strength of teeth with oval canal morphology. Based on the results of this study, although the fracture resistance of teeth restored with crowns was enhanced by deep fiber post placement, the use of oval fiber post is recommended in cases where deep placement is impossible. (J Oral Sci 58, 339-345, 2016).


Assuntos
Cavidade Pulpar , Técnica para Retentor Intrarradicular , Fraturas dos Dentes , Humanos
17.
J Gastroenterol ; 40(5): 498-503, 2005 May.
Artigo em Inglês | MEDLINE | ID: mdl-15942715

RESUMO

BACKGROUND: Electrical field stimulation of gallbladder muscle strips produces frequency-dependent contractions by activating cholinergic nerves. The cholinergic motor function of the gallbladder and enteric system is also modulated by other mediators. The aim of this study was to investigate the role of agmatine, a ligand for alpha 2-adrenoceptors and imidazoline binding sites, in the cholinergic motor activity of guinea pig gallbladder smooth muscle. METHODS: Gallbladder muscle strips obtained from guinea pigs were subjected to electrical field stimulation (1-64 Hz, 100 V, 1-ms pulse width, and 10-s train duration). Frequency-response contractions of gallbladder muscle strips were traced before and after the addition of cumulative concentrations of agmatine (10(-5)-10(-3) M) to the tissue bath. The same set of experiments was repeated in the presence of different antagonists. RESULTS: Agmatine by itself did not produce any contractions in guinea pig gallbladder muscle strips, but significantly enhanced the contractile response produced by electrical field stimulation. Yohimbine (10(-6) M), a selective alpha 2-adrenergic blocker, neither decreased nor increased the enhancement induced by agmatine. However, idazoxan (10(-4) M), an alpha-receptor blocker and imidazoline receptor antagonist, abolished this enhanced contractile response. Pretreatment with N(W)-nitro L-arginine methyl ester (L-NAME; 30 microM), and indomethacin (10 microM) did not inhibit the effect of agmatine. CONCLUSIONS: Our findings indicate that agmatine has a modulator role in the electrical field stimulation-induced cholinergic contractions of guinea pig gallbladder smooth muscle strips, and this role could be mediated by imidazoline receptors. Receptor binding studies should be done to determine the presence of endogenous agmatine and imidazoline receptors in gallbladder smooth muscle.


Assuntos
Agmatina/farmacologia , Estimulação Elétrica , Vesícula Biliar/efeitos dos fármacos , Contração Muscular/efeitos dos fármacos , Animais , Vesícula Biliar/fisiologia , Cobaias , Masculino , Modelos Animais , Contração Muscular/fisiologia , Músculo Liso/efeitos dos fármacos , Músculo Liso/fisiologia , Probabilidade , Sensibilidade e Especificidade , Estatísticas não Paramétricas , Técnicas de Cultura de Tecidos
18.
Interact Cardiovasc Thorac Surg ; 21(3): 342-5, 2015 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26015507

RESUMO

OBJECTIVES: In both low- and high-risk patients undergoing coronary artery bypass grafting, the internal mammary artery is the first choice of arterial graft, and the second choice is the radial artery (RA). Unfortunately, RA spasms are a significant problem for a surgical team to overcome in the perioperative and postoperative period. In current surgical practice, the use of vasodilator agents perioperatively in the pending graft preparation is generally accepted and these may be implemented topically, endoluminally or both ways. Moxonidine is the latest second-generation, centrally acting antihypertensive agent, and the intention in this paper is to investigate its direct vasorelaxant effects and relaxation mechanisms on the human radial artery in vitro. METHODS: RA rings were mounted in an organ bath and tested for changes in isometric tension in its relaxation response to moxonidine in the presence and absence of NG-nitro-L-arginine methyl ester (L-NAME, non-specific inhibitor of nitric oxide synthase), idazoxan (non-selective I1 and α2-antagonist) and yohimbine (selective α2-antagonist). RESULTS: Moxonidine induced concentration-dependent relaxations on the RA rings precontracted with phenylephrine (P < 0.05). L-NAME and idazoxan significantly reduced the relaxation caused by moxonidine (P < 0.05), while yohimbine significantly increased the relaxation by moxonidine (P < 0.05). In the presence of L-NAME + idazoxan, the relaxation by moxonidine was eliminated completely (P < 0.05). CONCLUSIONS: We speculate that the relaxant effect of moxonidine may be attributed partly to the synthesis and/or release of nitric oxide, and partly to the stimulation of imidazoline I1 receptors. We suggest that moxonidine may help to prevent RA spasms during the preparation period in operation when used topically or/and endoluminally.


Assuntos
Ponte de Artéria Coronária/métodos , Doença da Artéria Coronariana/cirurgia , Imidazóis/farmacologia , Músculo Liso Vascular/efeitos dos fármacos , Artéria Radial/transplante , Vasodilatação/efeitos dos fármacos , Anti-Hipertensivos/farmacologia , Doença da Artéria Coronariana/diagnóstico , Doença da Artéria Coronariana/fisiopatologia , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Artéria Radial/efeitos dos fármacos
19.
J Thorac Cardiovasc Surg ; 149(4): 1036-40, 2015 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-25749140

RESUMO

OBJECTIVE: Beta-blockers are a heterogeneous class of agents that are used in the treatment of many cardiovascular diseases, especially hypertension and atherosclerosis, and that are commonly prescribed after cardiac surgery. In the present study, the aim is to investigate the vasorelaxant effects of some common beta-adrenoceptor blockers on the human radial artery in vitro, as well as their relaxation mechanisms. METHODS: Radial artery rings sourced from human patients were mounted in an organ bath and tested for changes in isometric tension in relaxation response to labetalol, nebivolol, and propranolol in the presence and absence of NG-nitro-L-arginine methyl ester (3 × 10(-5) mol/L) and tetraethyl ammonium (3 × 10(-4) mol/L). RESULTS: The labetalol (10(-8) to 10(-4) mol/L), nebivolol (10(-8) to 10(-4) mol/L), and propranolol (10(-8) to 10(-4) mol/L) induced concentration-dependent relaxations on the radial artery rings, which had been precontracted with phenylephrine (10(-6) mol/L). The relaxation response induced by labetalol in the isolated radial artery rings was significantly higher when compared with the nebivolol and propranolol samples (P < .05). NG-nitro-L-arginine methyl ester significantly reduced the relaxation of nebivolol (P < .05), and tetraethyl ammonium significantly reduced the relaxation of labetalol, nebivolol, and propranolol (P < .05). CONCLUSIONS: We speculated that the relaxant effect of labetalol, nebivolol, and propranolol was due partly to the Ca(2+)-activated K(+) channels. In addition, the relaxation induced by nebivolol was largely related with nitric oxide release. Nebivolol, and partly propranolol, may provide significant therapeutic benefit, but labetalol can be a good alternative for coronary artery bypass grafting with radial artery use.


Assuntos
Antagonistas Adrenérgicos beta/farmacologia , Ponte de Artéria Coronária/métodos , Labetalol/farmacologia , Nebivolol/farmacologia , Propranolol/farmacologia , Artéria Radial/efeitos dos fármacos , Vasodilatação/efeitos dos fármacos , Vasodilatadores/farmacologia , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/farmacologia , Feminino , Humanos , Técnicas In Vitro , Masculino , Pessoa de Meia-Idade , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase/antagonistas & inibidores , Óxido Nítrico Sintase/metabolismo , Bloqueadores dos Canais de Potássio/farmacologia , Canais de Potássio Cálcio-Ativados/efeitos dos fármacos , Canais de Potássio Cálcio-Ativados/metabolismo , Artéria Radial/fisiologia , Artéria Radial/cirurgia
20.
Eur J Pharmacol ; 462(1-3): 155-60, 2003 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-12591108

RESUMO

Erectile dysfunction is common in men with chronic renal failure. Previously nitrergic and endothelium-dependent relaxation responses have been shown to be reduced in chronic renal failure rabbits. We have therefore investigated the efficacy of phosphodiesterase inhibitors on the corpora cavernosa obtained from uremic rabbits. Uremia was induced with 5/6 nephrectomy and 4 weeks later cavernosal tissue strips were isolated. The relaxant effect of phosphodiesterase 5 inhibitors, zaprinast (1-300 microM) and sildenafil (0.01-300 microM), phosphodiesterase 3 inhibitor amrinone (1-100 microM) and non-specific phosphodiesterase inhibitor papaverine (1-300 microM) were investigated on phenylephrine (10 microM)-induced tone. We found a shift in the dose-response curve of only phosphodiesterase 5 inhibitors. These results suggest that the decreased production or availability of endogenous nitric oxide in chronic renal failure animals leads to decreased efficacy of phosphodiesterase 5 inhibitors to induce relaxation.


Assuntos
Falência Renal Crônica/fisiopatologia , Relaxamento Muscular/efeitos dos fármacos , Pênis/efeitos dos fármacos , Inibidores de Fosfodiesterase/farmacologia , Amrinona/farmacologia , Animais , Peso Corporal/efeitos dos fármacos , Cálcio/sangue , Cálcio/urina , Creatinina/sangue , Relação Dose-Resposta a Droga , Estimulação Elétrica , Técnicas In Vitro , Isoenzimas/antagonistas & inibidores , Falência Renal Crônica/etiologia , Masculino , Nefrectomia/efeitos adversos , Papaverina/farmacologia , Hormônio Paratireóideo/metabolismo , Pênis/fisiologia , Fosfatos/sangue , Fosfatos/urina , Fosfolipases/antagonistas & inibidores , Piperazinas/farmacologia , Purinas , Purinonas/farmacologia , Coelhos , Citrato de Sildenafila , Sulfonas , Testosterona/metabolismo
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