Midaglizole hydrochloride (DG5128) is a preferential α2-adrenoceptor antagonist. Midaglizole hydrochloride (DG5128) exhibits 7.4 times higher affinity (pK_i=6.28) toward α2-adrenoceptor than α1-adrenoceptor.

Midaglizole (DG-5128) at concentrations up to 10 μM inhibits [³H]clonidine binding more effectively than it doed [³H]prazosin binding in rat cerebral cortex membranes. The mode of inhibition is homogeneous and consistent with the law of simple mass action. The EC₅₀ 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 IC₅₀ 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Yamanaka K, et al. The selectivity of DG-5128 as an alpha 2-adrenoceptor antagonist. Eur J Pharmacol. 1984 Nov 27;106(3):625-8.  [Content Brief]

  . Proks P, et al. Inhibition of recombinant K(ATP) channels by the antidiabetic agents midaglizole, LY397364 and LY389382. Eur J Pharmacol. 2002 Sep 27;452(1):11-9.  [Content Brief]

  . Hirohashi M, et al. Intrinsic pressor activity of midaglizole, an alpha-2 adrenoceptor antagonist, in pithed rats. Jpn J Pharmacol. 1990 Aug;53(4):519-20.  [Content Brief]