Effects of ritanserin, a novel serotonin-s2 receptor antagonist, on the secretion of pituitary hormones in normal humans

• Published in: Journal of endocrinological investigation Vol. 17; no. 1; pp. 1 - 5
• Main Authors: TEPAVCEVIC, D, GILJEVIC, Z, KORSIC, M, HALIMI, S, SUCHANEK, E, JELIC, T, AGANOVIC, I, KOZIC, B, PLAVSIC, V
• Format: Journal Article
• Language: English
• Published: Milano Kurtis 1994
• Subjects: Adolescent; Adrenocorticotropic Hormone - blood; Adrenocorticotropic Hormone - secretion; Adult; Biological and medical sciences; Dose-Response Relationship, Drug; Female; Follicle Stimulating Hormone - blood; Follicle Stimulating Hormone - secretion; Growth Hormone - blood; Growth Hormone - secretion; Humans; Hydrocortisone - blood; Hydrocortisone - secretion; Luteinizing Hormone - blood; Luteinizing Hormone - secretion; Male; Medical sciences; Middle Aged; Neuropharmacology; Neurotransmitters. Neurotransmission. Receptors; Pharmacology. Drug treatments; Pituitary Gland - secretion; Ritanserin - pharmacology; Serotonin Antagonists - pharmacology; Serotoninergic system; Thyrotropin - blood; Thyrotropin - secretion; Human; Pituitary hormone; Adenohypophyseal hormone; Serotonin antagonist; Peptide hormone; S2 receptor; ACTH; Neuroendocrine regulation; Pituitary gland; Biological activity
• ISSN: 0391-4097; 1720-8386
• DOI: 10.1007/BF03344953

The availability of a new potent and selective serotonin-S2 antagonist, ritanserin (RIT), encouraged us to further investigate the effect of serotonin on the basal secretion of anterior pituitary hormones in normal humans. Administered in a single 30-mg dose to group 1 consisting of 10 normal women, RIT failed to affect the baseline LH, FSH, GH or TSH levels. In group 2 consisting of 20 normal subjects (ten males and ten females), the same dose of RIT decreased in parallel both ACTH and cortisol levels but only at 180 min. Group 3 consisting of 8 normal men was studied on three separate occasions seven days apart: each subject received graded doses of 10 mg, 20 mg and 30 mg RIT. The mean baseline PRL concentration at 180 min as well as the net integrated area under the hormone curve (nAUC) decreased only after the highest dose, while the baseline cortisol concentrations at 180 min as well as the corresponding nAUC values displayed a clear dose-dependent response. The findings indicated the serotonin-S2 receptors to be only partially involved in the basal secretion of ACTH in normal humans.