Pharmacodynamics +<unk>  Site Ki (nM) Species Refs 202–432 Human 1,940–4,360 Human 5-HT1A 44–400 Human 5-HT1B 89–501 Human 5-HT1D 210–1,300 Human 5-HT1E 5-HT1F 5-HT2A 32–398 Human 5-HT2B 3.2–63 Human 5-HT2C 3.4–251 Human 5-HT3 427 Human 5-HT4 5-HT5A 1,354 Human 5-HT6 1,748 Human 5-HT7 163 Human α1 97–2,900 Human α1A 1,386 Human α1B 915 Human α1D α2 112–570 Human α2A 145 Human α2B 106 Human α2C 124 Human β 2,500 Human β1 2,359 Human β2 3,474 Human D1 7,000 Human D2 >10,000 Human D3 >10,000 Rat D4 D5 >10,000 Human H1 326 Human mAChRs >10,000 Human >10,000 Human σ1 σ2 8,350 Rat I1 759 Rat 6,043 Rat Values are Ki (nM). The smaller the value, the more strongly the drug binds to the site.<unk>  possesses significant affinity for the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, and 5-HT7 receptors, as well as the SERT. It also has some affinity for α1-adrenergic, α2-adrenergic, H1, I1, and NET. It behaves as an agonist at most serotonin receptors.<unk>  has been shown to act not only as a serotonin reuptake inhibitor but as a serotonin releasing agent as well.<unk> 's strongest actions are at the 5-HT2B and 5-HT2C receptors and its discriminative cue is mediated primarily by 5-HT2C. Its negative effects such as anxiety, headaches, and appetite loss are likely mediated by its actions on the 5-HT2C receptor. Other effects of<unk>  include nausea, hypoactivity, and penile erection, the latter two the result of increased 5-HT2C activity and the former likely via 5-HT3 stimulation. In comparison studies,<unk>  has approximately 10-fold selectivity for the human 5-HT2C receptor over the human 5-HT2A and 5-HT2B receptors (Ki = 3.4 nM vs. 32.1 and 28.8 nM). It acts as a partial agonist of the human 5-HT2A and 5-HT2C receptors but as an antagonist of the human 5-HT2B receptors. Pharmacokinetics<unk>  is<unk> bolized via the CYP2D6 isoenzyme by hydroxylation to para-hydroxy-mCPP (p-OH-mCPP) and this plays a major role in its<unk> bolism. The elimination half-life of<unk>  is 4 to 14 hours.<unk>  is a<unk> bolite of a variety of other piperazine drugs including trazodone, nefazodone, etoperidone, enpiprazole, mepiprazole, cloperidone, peraclopone, and BRL-15,572. It is formed by dealkylation via CYP3A4. Caution should be exercised in concomitant administration of CYP2D6 inhibitors such as bupropion, fluoxetine, paroxetine, and thioridazine with drugs that produce<unk>  as a<unk> bolite as these drugs are known to increase concentrations of the parent molecule (e.g., trazodone) and of<unk> .
Meta-Chlorophenylpiperazine
Para-Methoxyphenylpiperazine
Para-Iodoamphetamine
Methylpiperidinopyrazole
Methylbenzylpiperazine
Quazinone
Benzylpiperazine
Bromazine