CGP 12177 hydrochloride

CGP 12177 hydrochloride用途

CGP 12177 ((±)-CGP 12177) hydrochloride 是一种 β Adrenergic Receptor 配体。 CGP 12177 hydrochloride 是 β1- 和 β2-AR 的高亲和力拮抗剂。 CGP 12177 hydrochloride 还显示出以较低的亲和力与 β3-AR 相互作用,并对啮齿动物和人类 β3-AR 表现出部分激动剂活性。 CGP 12177 hydrochloride 对大鼠肺动脉中的 α1-AR 表现出部分激动剂特性。

CGP 12177 hydrochloride名称

[ CAS 号 ]:
64208-32-8

[ 英文名 ]:
CGP 12177 hydrochloride

CGP 12177 hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

[ 靶点 ]

Beta-1 adrenergic receptor

Beta-2 adrenergic receptor

Beta-3 adrenergic receptor

α1-adrenergic receptor

[参考文献]

[1]. Leblais V, et al. Role of alpha-adrenergic receptors in the effect of the beta-adrenergic receptor ligands, CGP 12177, bupranolol, and SR 59230A, on the contraction of rat intrapulmonary artery. J Pharmacol Exp Ther. 2004 Apr;309(1):137-45.

CGP 12177 hydrochloride物理化学性质

[ 分子式 ]:
C₁₄H₂₂ClN₃O₃

[ 分子量 ]:
315.80

[ 精确质量 ]:
315.13500

[ PSA ]:
90.14000

[ LogP ]:
2.17690

CGP 12177 hydrochloride安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

CGP 12177 hydrochloride文献

ALpha1-adrenoceptor antagonist properties of CGP 12177A and other beta-adrenoceptor ligands: evidence against beta(3)- or atypical beta-adrenoceptors in rat aorta.

Br. J. Pharmacol. 142 , 781-787, (2004)

1. The alpha(1)-adrenoceptor antagonist properties of the beta-adrenoceptor nonconventional partial agonist, CGP 12177A, was investigated in functional assays in rat aorta and in radioligand binding a...

Contribution of beta-adrenoceptor subtypes to relaxation of colon and oesophagus and pacemaker activity of ureter in wildtype and beta(3)-adrenoceptor knockout mice.

Br. J. Pharmacol. 130 , 747-758, (2000)

The smooth muscle relaxant responses to the mixed beta(3)-, putative beta(4)-adrenoceptor agonist, (-)-CGP 12177 in rat colon are partially resistant to blockade by the beta(3)-adrenoceptor antagonist...

The effects of beta-adrenoceptor agonists on KCl-induced rhythmic contraction in the ureter of guinea pig.

J. Smooth Muscle Res. 36 , 13-19, (2000)

In the present study, we tried to determine what effects were induced by beta-adrenoceptor agonists on 40 mM KCl-induced rhythmic contraction and to clarify which beta-adrenoceptor subtypes are involv...

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