Pargyline

Pargyline is an irreversible monoamine oxidase (MAO) inhibitor with K_is of 13 μM and 0.5 μM for MAO-A and MAO-B, respectively. Pargyline has antihypertensive and anticancer activities^[1][2][3]. Pargyline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. In Vitro: Pargyline (0.5-2 mM; 24-120 hours; LNCaP-LN3 cells) treatment inhibits the proliferation of prostate cancer cells in a time- and dose-dependent manner^[2].
Pargyline (0.5-2 mM; 24-48 hours; LNCaP-LN3 cells) treatment decreases S phase and increases the G1 phase in the cells in a dose-dependent manner^[2].
Pargyline (0.5 mM; 24 hours; LNCaP-LN3 cells) treatment increases the apoptotic cells^[2].
Pargyline (2 mM; 48 hours; LNCaP-LN3 cells) treatment induces an increase of cytochrome c and a decrease of caspase-3 in the cells, but does not lead to a change of BCL-2 expression^[2]. In Vivo: Pargyline (10 mg/kg; iv) treatment induces a moderate (about 20 mm Hg) but persistent (48 h) decrease of systolic blood pressure in unanesthetized adult spontaneously hypertensive rats (SHR) but not in normotensive rats^[3].
A low dose of Pargyline (200 μg; icv) injected directly into the brain lowered arterial pressure. The hypotensive action of Pargylline in SHR appears to be the consequence of Norepinephrine accumulating at an inhibitory α-adrenoceptor in brain^[3].