Ajmalicine (Raubasine) 阿吗里新，长春花草药中发现，是一种降压药，用于治疗高血压，降低外周阻力和血压。Ajmalicine (Raubasine) 是一种肾上腺素能药物，优先阻断 α1-肾上腺素受体 alpha 1-adrenoceptor。Ajmalicine (Raubasine) 是一种可逆的非竞争性尼古丁受体拮抗剂 (IC50=72.3 μM)。Ajmalicine (Raubasine) 优先作用于突触后部位，竞争性拮抗去甲肾上腺素对突触后 α 肾上腺素受体的作用 (pA2=6.57), 竞争性阻断可乐定的抑制作用 (pA2=6.2)。
| Cas No. | 483-04-5 |
| 别名 | 萝巴新,Raubasine |
| Canonical SMILES | O=C(C1=CO[C@@H](C)[C@](CN2CC3)([H])[C@]1([H])C[C@@]2([H])C4=C3C5=CC=CC=C5N4)OC |
| 分子式 | C21H24N2O3 |
| 分子量 | 352.43 |
| 溶解度 | Methanol: soluble |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Ajmalicine (Raubasine) is found in herbs of Catharanthus roseus, is an antihypertensive drug used in the treatment of high blood pressure, decreases peripheral resistance and blood pressure[1].Ajmalicine (Raubasine) is an adrenolytic drug which preferentially blocks alpha 1-adrenoceptor than alpha 2-adrenoceptor[2].Ajmalicine (Raubasine) is an reversible non-competitive nicotine receptor antagonist with an IC50 of 72.3 μM[3].Ajmalicine (Raubasine) acts preferentially at postsynaptic sites, competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptor with a pA2 value of 6.57, blocks the inhibitory effect of clonidine with an pA2 value of 6.2[4]. [1]. Wink, Michael; Roberts, M. W. (1998). Alkaloids: biochemistry, ecology, and medicinal applications. New York: Plenum Press. ISBN 0-306-45465-3.
[2]. Roquebert J, et al. Inhibition of the alpha 1 and alpha 2-adrenoceptor-mediated pressor response in pithed rats by raubasine, tetrahydroalstonine and akuammigine. Eur J Pharmacol. 1984 Oct 30;106(1):203-5.
[3]. Pereira DM, et al. Pharmacological effects of Catharanthus roseus root alkaloids in acetylcholinesterase inhibition and cholinergic neurotransmission. Phytomedicine. 2010 Jul;17(8-9):646-52.
[4]. •Demichel P, et al. Effects of raubasine stereoisomers on pre- and postsynaptic alpha-adrenoceptors in the rat vas deferens. Br J Pharmacol. 1984 Oct;83(2):505-10 |
