|
Biological Activity:
A potent and Kir6.2/SUR1 selective K(ATP) channels opener, which inhibits glucose stimulated insulin release in vitro and in vivo and has beneficial effects on glucose homeostasis in preclinical and clinical studies. Unfortunately, its clinical development was recently suspended due to elevated liver enzymes.
References:
RD Carr et al. NN414, a SUR1/Kir6.2-Selective Potassium Channel Opener, Reduces Blood Glucose and Improves Glucose Tolerance in the VDF Zucker Rat.
Diabetes 2003, 52(10), 2513-2518. [online]
M Zdravkovic et al. The effects of NN414, a SUR1/Kir6.2 selective potassium channel opener, in healthy male subjects. J. Clin. Pharmacol. 2005, 45(7), 763-772. [online]
JB Hansen. Towards selective Kir6.2/SUR1 potassium channel openers, medicinal chemistry and therapeutic perspectives. Curr. Med. Chem. 2006, 13(4), 361-76. [online]
M Zdravkovic et al. The effects of NN414, a SUR1/Kir6.2 selective potassium channel opener in subjects with type 2 diabetes. Exp. Clin. Endocrinol Diabetes. 2007, 115(6), 405-406. [online]
Chemical Name: 6-Chloro-3-(1-methylcyclopropylamino)-4H-thieno[3,2-e][1,2,4]thiadiazine-1,1-dioxide
|
