79689-25-1
中文名稱
MIDAGLIZOLE HYDROCHLORIDE
英文名稱
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 結(jié)構(gòu)式
基本信息
中文別名
咪格列唑鹽酸鹽 英文別名
Midaglizole hydrochloride2-[2-(4,5-dihydro-1H-imidazol-2-yl)-1-phenyl-ethyl]pyridine dihydrochl oride
常見問題列表
生物活性
Midaglizole hydrochloride (DG5128) 是有效的 α2-腎上腺素受體拮抗劑。Midaglizole hydrochloride (DG5128) 對(duì) α2-腎上腺素能受體的親和力 (pKi= 6.28) 比 α1-腎上腺素能受體高 7.4 倍。靶點(diǎn)
pKi :6.28 (α2-adrenoceptor)
體外研究
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.
體內(nèi)研究
Midaglizole (3 and 30 mg/kg, i.v.) increases blood pressure in pithed rats.