Hyperglycemic properties of serotonin receptor antagonists.
Several serotonin (5-HT) receptor antagonists with varying specificities for the 5-HT receptor types, were studied with regard to their effects on blood glucose levels in mice. The non-selective antagonists, metergoline and methysergide, proved to be hyperglycemic at doses commonly used to antagonize 5-HT receptors. In contrast, ritanserin (a 5-HT2 and 5-HT1c antagonist) and MDL 72222 (a 5-HT3 antagonist) were effective only at doses which surpassed the dose range considered to be selective for their respective receptors. The results suggest that 5-HT systems play a role in maintaining glucose homeostasis and that 5-HT1 receptors may be particularly important in this function. Furthermore, the inherent hyperglycemic properties of non-selective serotonin antagonists described here, are pertinent to studies using these agents to investigate glucose metabolism.
Wozniak
K M
KM
Laboratory of Clinical Studies, National Institute on Alcohol Abuse & Alcoholism, DICBR, Bethesda, MD 20892.
Linnoila
M
M
D000818:Animals; D001786:Blood Glucose / Q000032:analysis*; D008297:Male; D008711:Metergoline / Q000494:pharmacology; D008784:Methysergide / Q000494:pharmacology; D051379:Mice; D010880:Piperidines / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000378:metabolism; D016713:Ritanserin; D012702:Serotonin Antagonists / Q000494:pharmacology*; D014326:Tropanes / Q000494:pharmacology
D001786:Blood Glucose; D010880:Piperidines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014326:Tropanes; D016713:Ritanserin; D008711:Metergoline; C042253:bemesetron; D008784:Methysergide