Chemical Name:N-cyano-N'-(1,1-dimethylpropyl)-N''-3-pyridylguanidine
Biological Activity:
Potent KATP channel opener (EC50 for
relaxation of rat aorta = 7.5 nM). Binds to SUR2A and SUR2B with high affinity
(Kd values are 17 and 3 nM respectively).
Higdonet al (1997) Tissue and species variation in the vascular
receptor binding of 3H-P1075, a potent KATP opener
vasodilator. J.Pharmacol.Exp.Ther. 280 255. Grosset al
(1999) Stoichiometry of potassium channel opener action. Mol.Pharmacol. 56
1370. Buckneret al (2000) Pharmacological and molecular analysis
of ATP-sensitive K+ channels in the pig and human detrusor.
Eur.J.Pharmacol. 400 287. Ashcroft and Gribble (2000) New
windows on the mechanism of action of KATP channel openers. TiPS 21
439.
