N-Cyano-N''-(1,1-dimethylpropyl)-N''''-3-pyridinyl-guanidine is an ATP-sensitive potassium channels activator or opener (KATPCO) by causing relaxation of various isolated animal and human blood vessels.
생물학적 활성
Potent K ATP channel opener (EC 50 for relaxation of rat aorta = 7.5 nM). Binds to SUR2A and SUR2B with high affinity (K d values are 17 and 3 nM respectively).
효소 저해제
This potent potassium ion channel opener, or KCO (FW = 231.30 g/mol; CAS 60559-98-0; Solubility: 50 mM in Ethanol; 100 mM in DMSO), also known as N-cyano-N'-(1,1-dimethylpropyl)-N''-3-pyridyl-guanidine, targets Kir6 (or KATP) channels (EC50 = 7.5 nM; for relaxation of rat aorta). In studies on rats, rabbit and dogs, P1075 effects only correlate with the presence of specific receptor binding sites in rat vascular preparations, showing there are significant species-specific and raising questions about the pharmacological significance of this KATP opener binding site. These channels are heteromultimers composed with a 4:4 stoichiometry of an inwardly rectifying K+ channel subunit plus a regulatory subunit comprising the receptor sites for hypoglycemic sulfonylureas and KCOs (a sulfonylurea receptor). P1075-induced channel activation IS mediated by drug interaction with a single binding site per tetradimeric complex. P-1075 also binds to sulfonylurea receptors SUR2A (Kd = 17 nM) and SUR2B (Kd = 3 nM)
