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Endurance training in Wistar rats decreases receptor sensitivity to a serotonin agonist
Acta Physiologica Scandinavica, 2000There is mounting evidence that increased brain serotonin during exercise is associated with the onset of CNS‐mediated fatigue. Serotonin receptor sensitivity is likely to be an important determinant of this fatigue. Alterations in brain serotonin receptor sensitivity were examined in Wistar rats throughout 6 weeks of endurance training, running on a ...
D, Dwyer, J, Browning
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5-HT1A receptor blockade increases penile erections induced by indirect serotonin agonists
NeuroReport, 1993Indirect serotonergic agonists, whether promoters of 5-HT release such as fenfluramine (5 mg kg-1) or inhibitors of 5-HT uptake such as fluoxetine (10 mg kg-1), elicited in rats penile erections at a modest but significant level. Their effects were markedly potentiated by the beta-blocker tertatolol, (0.6-5 mg kg-1) which displays 5-HT1A receptor ...
P, Simon, J, Bertrand, J, Costentin
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Clozapine is a partial agonist at cloned, human serotonin 5-HT1A receptors
Neuropharmacology, 1996Clozapine exhibited 10-fold higher affinity than haloperidol for human 5-HT1A receptors expressed in Chinese Hamster Ovary cells (CHO-h5-HT1A) (Kis = 160 and 1910 nM respectively). Whereas haloperidol did not alter the basal binding of [35S]GTP gama S to CHO-h5HT1A membranes, clozapine stimulated it with an EC50 of 2320 nM and an efficacy of 49 ...
A, Newman-Tancredi +3 more
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SEROTONIN 5-HT2C RECEPTOR AGONISTS: POTENTIAL FOR THE TREATMENT OF OBESITY
Molecular Interventions, 2005Obesity continues to be a burgeoning health problem worldwide. Before their removal from the market, fenfluramine and the more active enantiomer dexfenfluramine were considered to be among the most effective of weight loss agents. Much of the weight loss produced by fenfluramine was attributed to the direct activation of serotonin 5-HT(2C) receptors in
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Serotonin receptor ontogeny: Effects of agonists in 1-day-old rats
Pharmacology Biochemistry and Behavior, 1992Although numerous subtypes of serotonin [5-hydroxytryptamine (5-HT)] receptors have been identified in the newborn rat by radioligand binding studies, there have been few studies of the functional significance of these early receptors, most without the benefit of selective drugs.
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Effect of Selective Serotonin Receptor Agonists on Prolactin Secretion in Male Rats
Neuroendocrinology, 1993The effect of different serotonin (5-HT) receptor agonists on the release of prolactin (PRL) was investigated in conscious male rats. The 5-HT1 receptor agonists 5-carboxamidotryptamine and RU 24969 stimulated the PRL secretion dose dependently.
Jørgensen, H., Knigge, U., Warberg, J.
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Serotonin 5-HT1A Receptor Agonists as Antidepressants
CNS Drugs, 1998Jon F. Heiser, Charles S. Wilcox
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Behavioral studies of serotonin receptor agonists as antidepressant drugs.
The Journal of clinical psychiatry, 1992Recent developments in the pharmacology of antidepressant drugs have focused on compounds that enhance the neurotransmission of serotonin (5-hydroxytryptamine; 5-HT), such as 5-HT uptake inhibitors. In addition, the 5-HT1A receptor partial agonist buspirone and other similarly structured compounds termed azapirones are also candidates for ...
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Nowi selektywni funkcjonalnie agoniści receptora serotoninowego 5-HT1A
2018Przedmiotem rozprawy doktorskiej było opracowanie nowej generacji selektywnych funkcjonalnie agonistów receptora serotoninowego typu 5-HT1A, o istotnym znaczeniu w poszukiwaniu terapii schorzeń psychiatrycznych i neurodegeneracyjnych. Zaprojektowano, przy wsparciu modelowania molekularnego, oraz otrzymano drogą syntezy chemicznej bibliotekę 65 nowych ...
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