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[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]
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)
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 ...
It is both a precursor in the synthesis of aripiprazole and one of its metabolites. [1] [2] It is unclear whether 2,3-DCPP is pharmacologically active as a serotonin receptor agonist similar to its close analogue 3-chlorophenylpiperazine (mCPP), though it has been shown to act as a partial agonist of the dopamine D 2 and D 3 receptors. [3]
oMeOPP and mCPP have both been found to suppress conditioned avoidance responses (CARs) without markedly affecting escape behavior in animals, indicative that they have antipsychotic-like effects. [2] The serotonin receptor antagonist metergoline reversed the suppression of CARs by mCPP but not by oMeOPP.
The cause of death, following toxicology tests, was determined to be a drug overdose from a combination of trazodone, an antidepressant; mCPP, a metabolite of trazodone; and risperidone, used to treat schizophrenia. The death was ruled a suicide.
Plasma levels of mCPP are very low at about 7% of those of nefazodone; hence, mCPP is only a minor metabolite. [2] [35] mCPP is thought to be formed from nefazodone specifically by CYP2D6. [3] [35] The ratios of brain-to-plasma concentrations of mCPP to nefazodone are 47:1 in mice and 10:1 in rats, suggesting that brain exposure to mCPP may be ...
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