79689-25-1

中文名称 MIDAGLIZOLE HYDROCHLORIDE

英文名称 2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenyl-ethyl]pyridine dihydrochl oride

CAS 79689-25-1

分子式 C16H19Cl2N3

MOL 文件 79689-25-1.mol

更新日期 2023/03/20 15:41:19

79689-25-1 结构式

基本信息物理化学性质图谱信息常见问题列表

基本信息

中文别名

咪格列唑盐酸盐

英文别名

Midaglizole hydrochloride
2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenyl-ethyl]pyridine dihydrochl oride

物理化学性质

储存条件-20°C储存

溶解度溶于二甲基亚砜

形态Solid

颜色White to off-white

图谱信息

MIDAGLIZOLE HYDROCHLORIDE(79689-25-1)核磁图(¹HNMR)

常见问题列表

生物活性

Midaglizole hydrochloride (DG5128) 是有效的 α2-肾上腺素受体拮抗剂。Midaglizole hydrochloride (DG5128) 对 α2-肾上腺素能受体的亲和力 (pKi= 6.28) 比 α1-肾上腺素能受体高 7.4 倍。

靶点

pKi :6.28 (α2-adrenoceptor)

体外研究

Midaglizole (DG-5128) at concentrations up to 10 μM inhibits [ ³ H]clonidine binding more effectively than it doed [ ³ H]prazosin binding in rat cerebral cortex membranes. The mode of inhibition is homogeneous and consistent with the law of simple mass action. The EC ₅₀ values for stimulation of insulin release from rat islets and the MIN6 β-cell line induced by Midaglizole are 200 nM and 24 μM, respectively. The IC ₅₀ values for K _ATP current inhibition induced by Midaglizole are 3.8 μM and 4.4 uM for Kir6.2 and Kir6.2/SUR1 , respectively.

体内研究

Midaglizole (3 and 30 mg/kg, i.v.) increases blood pressure in pithed rats.