product name Tranylcypromine hemisulfate
Description: Tranylcypromine hemisulfate, also known as 2-PCPA, is a nonselective and irreversible monoamine oxidase inhibitor, which inhibits CYP2A6 with Ki of 0.08 μM and 0.2 μM in cDNA-expressing microsomes and Human Liver Microsomes, respectively. Tranylcypromine is used as an antidepressant and anxiolytic agent in the clinical treatment of mood and anxiety disorders, respectively.
References: Drug Metab Dispos. 2001 Jun;29(6):897-902; Environ Health Perspect. 2004 Aug;112(11):1159-64.
182.23
Formula
C9H12NO₂S₀.₅
CAS No.
13492-01-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 5 mg/mL
Water: 46.66 mg/mL
Ethanol:
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: R-(+)-Tranylcypromine, (±)-Tranylcypromine, and S-(−)-Tranylcypromine competitively inhibits CYP2A6-mediated metabolism of nicotine with apparent Ki values of 0.05 μM, 0.08 μM, and 2.0 μM, respectively, in human liver microsomes. Tranylcypromine (500 μg/mL) severely inhibits bradykinin-stimulated arachidonic acid release in calf aortic endothelial cells. Tranylcypromine inhibits CYP2A6 and CYP2E1 activity with IC50 of 0.42 μM and 3 μM, respectively, in human liver microsomes. Tranylcypromine induces type II and cyclopropylbenzene type I difference spectrum in human liver microsomes. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Tranylcypromine injection leads to a large, slow increase in motor activity at 5 mg/kg and 10 mg/kg compared with the saline control in male rats, although 2 mg/kg Tranylcypromine does not induce an increase. Tranylcypromine (10 mg/kg) also causes significant decreases in the number of rearing behaviors in male rats. |
| Animal model | |
| Formulation & Dosage | |
| References | Drug Metab Dispos. 2001 Jun;29(6):897-902; Environ Health Perspect. 2004 Aug;112(11):1159-64. |
