Monatepil

Monatepil (AJ-2615 free base) is a calcium antagonist with potent α1-adrenoceptor blocking activity. Monatepil inhibits vasopressin- or methacholine-induced ischemic electrocardiographic changes in a rat model of vasospastic angina and reduces the mean arterial pressure in anesthetized rats. Monatepil also enhances low-density lipoprotein (LDL) receptor activity in human skin fibroblasts. Monatepil can be used in research related to hypertension, atherosclerosis, hyperlipidemia and vasospastic angina^[1][2][3]. In Vitro:Monatepil enhances LDL receptor activity in human skin fibroblasts^[3]. In Vivo:Monatepil (3 mg/kg; p.o.; 1 h prior to vasopressin administration) significantly inhibits vasopressin (0.2 IU/kg; i.v.)-induced ST-segment depression in male Nrc:Donryu rats; a significant inhibitory effect remains 7 h after oral administration of 30 mg/kg^[2].
Monatepil (0.3 mg/kg; i.v.) significantly inhibits acetylcholine (16 μg/kg; intracoronary administration)-induced ST-segment elevation in male Jcl:Sprague-Dawley rats; the inhibition rate exceeds 60% at a dose of 1 mg/kg^[2].
Monatepil (0.1-1 mg/kg; i.v.) reduces the mean arterial pressure of anesthetized male Std:Wistar rats by 14.0, 40.6, and 50.2 mmHg, respectively; at doses of 0.3 and 1 mg/kg, it also significantly decreases heart rate^[2].