| Description | AE0047 Hydrochloride is a blocker of calcium, and used in the research of the hypertensive disease. |
| In vitro | AE0047 Hydrochloride (4e) is an antagonist of calcium[1]. AE0047 inhibits [3H]nimodipine binding to rat cardiac membrane homogenate (IC50 of 0.26 nM)[2]. AE0047 (1 μM) inhibits the high K+-evoked vascular smooth muscle contraction, and also inhibits [3H]PN200-110 binding (Ki : 40.9 nM)[3]. |
| In vivo | AE0047 (3 mg/kg) shows antihypertensive effect, and reduces systolic blood pressure(ED30 of 1.1 mg/kg)[2].In aorta isolated from stroke-prone spontaneously hypertensive rats (SHRSP), AE0047 (1 or 3 mg/25g SP diet) inhibits blood pressure elevation and improves endothelium-dependent relaxation in response to acetylcholine [4]. |
| molecular weight | 723.26 |
| Molecular formula | C41H43ClN4O6 |
| CAS | 116308-56-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Ashimori A, et al. Novel 1,4-dihydropyridine calcium antagonists. II. Synthesis and antihypertensive activity of 3-[4-(substituted amino)phenylalkyl]ester derivatives. Chem Pharm Bull (Tokyo). 1991 Jan;39(1):91-9. 2. Ashimori A, et al. Synthesis and pharmacological effects of optically active 2-[4-(4-benzhydryl-1-piperazinyl)phenyl]-ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate hydrochloride. Chem Pharm Bull (Tokyo). 1991 Jan;39(1):108-11. 3. Yamanaga K, et al. AE0047-mediated calcium channel blocking in vascular smooth muscles. Gen Pharmacol. 1997 Sep;29(3):337-43. 4. Nishikawa M, et al. Protection against endothelial abnormalities by a novel calcium channel blocker, AE0047, in stroke-prone spontaneously hypertensive rats. Gen Pharmacol. 1999 Mar;32(3):299-305. |