Tranylcypromine (2-PCPA) hydrochloride 是一种单胺氧化酶抑制剂，可有效治疗重度抑郁症、心境恶劣障碍和非典型抑郁症。它是由苯丙胺侧链环化形成的丙胺。它对恐慌和恐惧症也很有用。

Tranylcypromine Hydrochloride, a monoamine oxidase inhibitor, is effective in the treatment of major depression, dysthymic disorder, and atypical depression. It is a propylamine formed from the cyclization of the side chain of amphetamine. It also is useful in panic and phobic disorders.

与空白对照组相比,Tranylcypromine（5 mg/kg和10 mg/kg）可大而缓的增加雄性大鼠的肌肉活动,但2 mg/kg的Tranylcypromine没有效果. Tranylcypromine（10 mg/kg）使雄性大鼠饲养行为数量显著增加.

在小牛主动脉内皮细胞中,Tranylcypromine（500 μg/mL）可强烈抑制缓激肽诱导的花生四烯酸释放。 Tranylcypromine还能抑制HLMs中的CYP2A6（IC50：0.42 μM）和CYP2E1（IC50：3 μM）活性。在HLMs中,Tranylcypromine引起II型和环丙基苯I型的差异谱。HLMs中CYP2A6介导的尼古丁代谢可被R-(+)-Tranylcypromine（Ki：0.05 μM）,(±)-Tranylcypromine（Ki：0.08 μM）以及S-(-)-Tranylcypromine（Ki：2.0 μM）完全抑制。

PDE activity is determined with some modifications. The assay mixture contain 50 mM Tris (pH 7.4), 5 mM MgCl2, 0.5 μM cAMP or cGMP, and [3H]cAMP or [3H]cGMP (about 30,000 cpm/assay), the indicated concentration of the inhibitor and an aliquot of the enzyme solution at a final assay volume of 200 μL. Stock solutions of the compounds are diluted 1:100 (v/v) in the Tris buffer mentioned above; appropriate dilutions are prepared in 1% (v/v) DMSO/Tris buffer, which are diluted 1:2 (v/v) in the assays to obtain the desired final concentrations of the inhibitors at a DMSO concentration of 0.5% (v/v). DMSO itself affected none of the PDE activities. After preincubation for 5 min at 37°C, the reaction is started by the addition of substrate (cAMP or cGMP) and the assays are incubated for further 15 min at 37°C. Then 50 μL of 0.2 N HCl is added to stop the reaction and the assays are left on ice for about 10 min. Following incubation with 25 μg of 5′-nucleotidase (Crotalus atrox snake venom) for 10 min at 37°C, the assays are loaded on QAE Sephadex A-25 (1 mL of bed volume in Poly-Prep chromatography columns). The columns are eluted with 2 mL of 30 mM ammonium formate (pH 6.0) and the eluate is counted for radioactivity. Results are corrected for blank values (measured in the presence of denatured protein) that are below 5% of total radioactivity. The amount of cyclic nucleotides hydrolyzed did not exceed 30% of the original substrate concentration[3].

1986-47-6

C9H12ClN

169.65

SKF-385 HCl;Tranylcypromine (2-PCPA) HCl;反苯环丙胺盐酸盐

H2O:17 mg/mL (100 mM)
DMSO:17 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years