m-Chlorophenylpiperazine (mCPP) is an antagonist at the cloned human 5-HT2B receptor.
The behavioural effects of m-chlorophenylpiperazine (mCPP) in rats and its clinical effects in man are thought to be related to its action at 5-HT2B/2C receptors. However, although mCPP is a partial agonist at these subtypes in rat, its efficacy at human 5-HT2B/2C receptors is unknown. We therefore investigated the activity of mCPP at cloned human 5-HT2B and 5-HT2C receptors. mCPP was a partial agonist at the human 5-HT2C receptor but antagonized the human 5-HT2B receptor. Therefore, while supporting the proposal that at least some of the clinical effects of mCPP are likely to be mediated via stimulation of the 5-HT2C receptor, this study also suggests that any 5-HT2B receptor-mediated effects are more likely to result from receptor blockade than from receptor activation.
Thomas
D R
DR
Department of Psychiatry Research, SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
Gager
T L
TL
Holland
V
V
Brown
A M
AM
Wood
M D
MD
D000818:Animals; D002460:Cell Line; D003001:Cloning, Molecular; D006801:Humans; D007668:Kidney / Q000166:cytology / Q000187:drug effects* / Q000196:embryology; D016015:Logistic Models; D010879:Piperazines / Q000494:pharmacology*; D051381:Rats; D012702:Serotonin Antagonists / Q000494:pharmacology*; D017366:Serotonin Receptor Agonists / Q000494:pharmacology
D010879:Piperazines; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; C015068:1-(3-chlorophenyl)piperazine