Abstract
The effects of the selective 5-HT1A receptor agonist flesinoxan on neuroendocrine function, temperature, and behavior were assessed in male healthy volunteers using a double-blind, placebo-controlled crossover design. Flexinoxan (7 and 14 μg/kg), administered intravenously in 11 healthy volunteers, elicited a dose-related decrease in body temperature and increases in growth hormone, adrenocorticotropic hormone (ACTH), cortisol, and prolactin plasma levels. In a second independent study, 12 healthy volunteers were pretreated sequentially, at one-week intervals, with either the 5-HT1A antagonist pindolol (30 mg, PO), the nonselective 5-HT1 2 antagonist methysergide (4 mg, PO), or placebo, prior to being administered flesinoxan (1 mg, IV). The growth hormone response to flesinoxan was blocked by pindolol but not by methysergide, whereas the prolactin response was blocked by methysergide but not by pindolol. The ACTH and cortisol responses to flesinoxan were potentiated by methysergide. The flesinoxan-induced hypothermia was attenuated by both methysergide and pindolol, although the latter effects did not reach statistical significance. The present results suggest that the growth hormone response and the hypothermic response to the intravenous infusion of flesinoxan may serve as a valid index of 5-HT1A receptor function in humans.
Similar content being viewed by others
Article PDF
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Seletti, B., Benkelfat, C., Blier, P. et al. Serotonin1A Receptor Activation by Flesinoxan in Humans. Neuropsychopharmacol 13, 93–104 (1995). https://doi.org/10.1016/0893-133X(95)00025-9
Received:
Revised:
Accepted:
Published:
Issue Date:
DOI: https://doi.org/10.1016/0893-133X(95)00025-9
Keywords
This article is cited by
-
The Serotonin 1A (5-HT1A) Receptor as a Pharmacological Target in Depression
CNS Drugs (2023)
-
The European College of Neuropsychopharmacology (ECNP) Medicines Chest Initiative: Rationale and Promise
Pharmaceutical Medicine (2015)
-
Pharmacology of ayahuasca administered in two repeated doses
Psychopharmacology (2012)
-
Intravenous buspirone for the prevention of postoperative nausea and vomiting
European Journal of Clinical Pharmacology (2012)
-
The effect of changes in core body temperature on the QT interval in beagle dogs: a previously ignored phenomenon, with a method for correction
British Journal of Pharmacology (2008)