Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo[1][2][3].
Midaglizole stimulates insulin release with the EC50 values of 200 nM, 24 µM for rat islets and MIN6 β-cell line, respectively[3].
Midaglizole (3, 30 mg/kg; i.v.) increases blood pressure in rats[1].
Midaglizole (0.2, 1, 2 mg/kg; infusion) reduces blood glucose levels in dags[2].
| Animal Model: | 290-450 g, Male Wistar rats[1] |
| Dosage: | 3, 30 mg/kg |
| Administration: | I.v. |
| Result: | Increased the blood pressure by 27 and 64 mmHg at 3, 30 mg/kg, respectively. |
| Animal Model: | Dogs[2] |
| Dosage: | 0.2, 1, 2 mg/kg |
| Administration: | Superior pancreaticoduodeneal artery infusion |
| Result: | Reduced blood glucose levels by stimulating insulin release from the pancreatic islets. |
[1]. 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.
[2]. Ohneda K, et al. Mechanism of insulin secretion by midaglizole. Diabetes Res Clin Pract. 1993 Feb;19(2):127-32.
[3]. 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.