α(2)肾上腺素能受体拮抗剂性质opc - 28326,一种新型选择性外围血管舒张。

文章的细节

引用
复制到剪贴板

Orito K,岸M, Imaizumi T, Nakazawa T,桥本,Mori T, Kambe T

α(2)肾上腺素能受体拮抗剂性质opc - 28326,一种新型选择性外围血管舒张。

Br J杂志。2001年10月,134 (4):763 - 70。

PubMed ID
11606316 (在PubMed
]
文摘

1。敌对性质的opc - 28326 ([4 - (N-methyl-2-phenylethylamino) 1 - (3, 5-dimethyl-4-propionyl-aminobenzoyl)]哌啶盐酸盐一水化物),研究了选择性外围血管舒张,通过分析数据从大鼠各组织功能研究和绑定的研究药物α肾上腺素受体亚型(2)。2。使用人类重组受体大鼠肾皮质,我们发现opc - 28326显示关联性α(2)-α(2 b) -和α(2 c) -adrenoceptors K (i)值为2040,285年,分别和55纳米。育亨宾的K (i)值α(2)-α(2 b) -和α(2 c) -adrenoceptors分别为3.0,2.0和11.0 nM,分别。3所示。B-HT 920,一个α(2)肾上腺素能受体受体激动剂,产生一个加压反应通过外围突触后α(2)肾上腺素能受体刺激(被认为是一个α(2 b)亚型)在reserpine-pretreated髓老鼠准备。opc - 28326(3 - 30毫克公斤(1),注射)和育亨宾(0.3 - 3毫克公斤(1),注射)导致剂量依赖性右转920年B-HT引起的加压的剂量反应曲线。明显的pA(2)值分别为1.55(0.87 - 2.75,95%置信区间)和0.11(0.06 - 0.21)毫克公斤(1),分别。opc - 28326的效力低于育亨宾14倍左右。beplayapp 4. Clonidine inhibited the tension developed by electrical stimulation, of the rat vas deferens, by its peripheral presynaptic alpha(2A/D)-adrenoceptor action. OPC-28326 (1 - 100 microM) and yohimbine (10 - 1000 nM) caused a rightward shift in the concentration-response curve of clonidine. The pA(2) values were 5.73 (5.54 - 5.91) and 7.92 (7.84 - 8.01), respectively, providing evidence for a potency of OPC-28326 of about 155 times less than that of yohimbine. 5. Mydriasis was induced by brimonidine via stimulation of central alpha(2A/D)-adrenoceptors in anaesthetized rats. Intravenous OPC-28326 had no effect on this action, even at a very high dose of 10 mg kg(-1) i.v., while yohimbine (0.1 - 0.3 mg kg(-1) i.v.) inhibited mydriasis in a dose-dependent manner, indicating that OPC-28326 was at least 100 times less potent than yohimbine in regard to the anti-mydriatic effect. 6. These data suggest that OPC-28326 preferentially exerts peripheral and postsynaptic antagonistic actions on the alpha(2B)- and alpha(2C)-adrenoceptor subtypes.

beplay体育安全吗DrugBank数据引用了这篇文章

药物
药物靶点
药物 目标 类 生物 药理作用 行动
Brimonidine Alpha-2C肾上腺素能受体 蛋白质 人类
是的
受体激动剂
 细节