AE0047Hydrochloride是一种calcium阻滞剂，可用于高血压症的研究。
CAS：116308-56-6
分子式：C41H43ClN4O6
分子量：723.26
纯度：98%
存储：Store at -20°C

Background:

AE0047 Hydrochloride is a calcium blocker, used in the research of hypertensive disease.

AE0047 Hydrochloride (4e) is a calcium antagonist[1]. AE0047 inhibits [3H]nimodipine binding to rat cardiac membrane homogenate with an 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 with a Ki of 40.9 nM[3].

AE0047 (3 mg/kg) shows antihypertensive effect, and reduces systolic blood pressure with ED30 of 1.1 mg/kg[2]. AE0047 (1 or 3 mg/25g SP diet) inhibits blood pressure elevation and improves endothelium-dependent relaxation in response to acetylcholine in aorta isolated from stroke-prone spontaneously hypertensive rats (SHRSP)[4].

[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.