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Trazodone has a minor active metabolite known as meta-chlorophenylpiperazine (mCPP), and this metabolite may contribute to some degree to the pharmacological properties of trazodone. [11] [110] In contrast to trazodone, mCPP is an agonist of various serotonin receptors. [111]
Trazodone, nefazodone, mepiprazole, and others produce mCPP as a metabolite. para-Substituted. 4-Chlorophenylpiperazine (pCPP) 4-Fluorophenylpiperazine (pFPP)
[2] [51] [52] The elimination half-life of mCPP is 4 to 14 hours. [2] mCPP is a metabolite of a variety of other piperazine drugs including trazodone, nefazodone, etoperidone, enpiprazole, mepiprazole, cloperidone, peraclopone, and BRL-15,572. [52] [additional citation(s) needed] It is formed by dealkylation via CYP3A4. [52]
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These drugs act as antagonists or inverse agonists of the 5-HT 2A, α 1-adrenergic, and H 1 receptors, as partial agonists of the 5-HT 1A receptor, [3] and as inhibitors of the transporters. mCPP is an antagonist of the 5-HT 2B receptor, an agonist of the 5-HT 1A, [3] 5-HT 2C, and 5-HT 3 receptors, [4] [5] and acts as a partial agonist of the ...
The serotonin receptor agonist mCPP has a significant affinity for 5-HT 2C receptors. mCPP patients experience multiple side effects due to non-selectivity over 5-HT 2A and 5-HT 2B receptors. The absence of the hypophagic (reduced food consumption) effect of mCPP in 5-HT 2C receptor knockout mice suggests that this effect is mediated through 5 ...
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