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。

Midaglizole hydrochloride (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor.

The inhibitory effect of midazolam (DG-5128) at a concentration of up to 10 μM in the cerebral cerebral membrane of [3H] clonidine is more effective than that of [3H] prazosin. The suppression method is uniform and conforms to the simple law of mass action. The EC50 values of midazolazole-induced insulin release in rat pancreatic islets and MIN6β cell lines were 200 nM and 24 μM, respectively. The IC50 values of midazolam for Kir6.2 and Kir6.2/SUR1 induced KATP current were 3.8 μM and 4.4 uM, respectively.

Midaglizole (3 and 30 mg/kg, i.v.) increases blood pressure in pithed rats[1].

79689-25-1

C16H19Cl2N3

324.25

DG5128 hydrochloride;(±)-DG5128 hydrochloride;Midaglizole hydrochloride

DMSO:450mg/mL (1387.8mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years