Details of the Metabolic Reaction (MR)

General Information of This Metabolic Reaction (MR) (ID: MR000523)
Formula
SVG example
N-Dealkylation
Reactant Buspirone Product 1-Pyrimidinylpiperazine
Reactant Info Product Info
Metabolic Enzyme Cytochrome P450 3A4 (CYP3A4) DME Info
Metabolic Type Oxidation - N-Dealkylation
Other MR(s) Related to The Reactant of This MR
Other MR(s) That Metabolize The Reactant of This MR
MR ID Reactant Product MR Type Related Drug REF
MR000525 Buspirone 3'-hydroxybuspirone Oxidation - Hydroxylation Buspirone [1]
MR000522 Buspirone 5-hydroxybuspirone Oxidation - Hydroxylation Buspirone [2]
MR000526 Buspirone 6'-hydroxybuspirone Oxidation - Hydroxylation Buspirone [1], [3]
MR000524 Buspirone Buspirone N-oxide Oxidation - N-Oxidation Buspirone [1]
Other MR(s) Related to The Product of This MR
Other MR(s) That Produce The Product of This MR
MR ID Reactant Product MR Type Related Drug REF
MR012622 Gepirone 2-(1-Piperazinyl)pyrimidine Unclear - Unclear Gepirone [4]
MR001842 Org-33062 1-Pyrimidinylpiperazine Unclear Org-33062 [5]
MR013728 PF-00734200 PF-00734200 metabolite M3 Oxidation - N-dealkylation PF-00734200 [6]
MR008816 Tandospirone 1\(2\pyrimidinyl)\piperazine (1\PP) Oxidation - Oxidative cleavage Tandospirone [7], [8]
Other MR(s) That Metabolize The Produtc of This MR
MR ID Reactant Product MR Type Related Drug REF
MR012623 2-(1-Piperazinyl)pyrimidine 2-(Piperazin-1-yl)pyrimidin-5-ol Unclear - Unclear Gepirone [9]
MR008817 1\(2\pyrimidinyl)\piperazine (1\PP) 5-OH-1-PP Unclear - Unclear Tandospirone [8]
References
1 DrugBank(Pharmacology-Metabolism)Buspirone
2 Metabolism and disposition of buspirone Am J Med. 1986 Mar 31;80(3B):41-51. doi: 10.1016/0002-9343(86)90331-1.
3 Interaction of buspirone and its major metabolites with human organic cation transporters. Fundam Clin Pharmacol. 2023 Feb 26. doi: 10.1111/fcp.12883.
4 Gepirone and 1-(2-pyrimidinyl)-piperazine in vitro: human cytochromes mediating transformation and cytochrome inhibitory effects
5 Human cytochromes mediating gepirone biotransformation at low substrate concentrations. Biopharm Drug Dispos. 2003 Mar;24(2):87-94.
6 Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human
7 Simultaneous determination of tandospirone and its active metabolite, 1-[2-pyrimidyl]-piperazine in rat plasma by LC-MS/MS and its application to a pharmacokinetic study
8 Identification of CYP3A4 as the primary cytochrome P450 responsible for the metabolism of tandospirone by human liver microsomes
9 PubChem:Gepirone

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