Acute effects of zimelidine and alaproclate, two inhibitors of serotonin uptake, on neuroendocrine function.
The accumulation of 14C-5-hydroxytryptamine in human platelets in vitro and plasma levels of a number of hypophyseal hormones and cortisol in healthy male volunteers were determined after acute oral administration of zimelidine and alaproclate, two selective inhibitors of serotonin (5-HT) uptake. Alaproclate (100 mg)  significantly inhibited the accumulation of 14C-5-HT by 42% at 90 minutes but showed no significant effect at 4 hours. At 200 mg the decrease in the accumulation was 55% after 90 minutes and 31% after 4 hours. Zimelidine (200 mg) caused a 72% decrease at 90 minutes and 73% at 4 hours. Plasma levels of prolactin, growth hormone, luteinizing hormone, follicle stimulating hormone, and thyroid stimulating hormone remained unchanged after zimelidine and alaproclate, and the levels were comparable to those after placebo. A physiological decline of plasma cortisol levels was noted in the morning during the test period of 4 hours, but there were slight differences in the secretory pattern after the different drugs used.
D000328:Adult; D000409:Alanine / Q000031:analogs & derivatives* / Q000494:pharmacology; D001792:Blood Platelets / Q000032:analysis; D001977:Brompheniramine / Q000031:analogs & derivatives / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D005640:Follicle Stimulating Hormone / Q000097:blood; D013006:Growth Hormone / Q000097:blood; D006801:Humans; D006854:Hydrocortisone / Q000097:blood*; D066298:In Vitro Techniques; D007986:Luteinizing Hormone / Q000097:blood; D008297:Male; D010908:Pituitary Hormones, Anterior / Q000097:blood*; D011388:Prolactin / Q000097:blood; D011725:Pyridines / Q000494:pharmacology*; D012701:Serotonin / Q000097:blood; D012702:Serotonin Antagonists / Q000494:pharmacology*; D013972:Thyrotropin / Q000097:blood; D015031:Zimeldine
D010908:Pituitary Hormones, Anterior; D011725:Pyridines; D012702:Serotonin Antagonists; D012701:Serotonin; D015031:Zimeldine; D011388:Prolactin; D007986:Luteinizing Hormone; D005640:Follicle Stimulating Hormone; D013972:Thyrotropin; D013006:Growth Hormone; C025293:alaproclate; D001977:Brompheniramine; D000409:Alanine; D006854:Hydrocortisone