The L-type Ca2+ channels possess binding sites for at least three distinct organic drug types: dihydropyridines (DHP), phenylalkylamines (PAA), and benzothiazepines (BTZ). These binding sites are known to reside in the α1 subunit of the channel. (R)(+)-Bay K8644 is a DHP L-type Ca2+-channel blocker with negative inotropic and vasodilatatory effects in vivo. (R)(+)-Bay K8644 shows opposite effects to (S)(-)-Bay K8644. The action of the of (R)(+)-Bay K8644 was studied in rat tail artery and guinea pig ileal longitudinal smooth muscle using pharmacologic and radioligand binding assays. (R)(+)-Bay K8644 inhibited the responses to KCI-induced depolarization with IC50 values of 16.1-25.6 nM.
产品描述
A Blocker of L-Type CaV Channels
产品形式
The L-type Ca2+ channels possess binding sites for at least three distinct organic drug types: dihydropyridines (DHP), phenylalkylamines (PAA), and benzothiazepines (BTZ). These binding sites are known to reside in the α1 subunit of the channel. (R)(+)-Bay K8644 is a DHP L-type Ca2+-channel blocker with negative inotropic and vasodilatatory effects in vivo. (R)(+)-Bay K8644 shows opposite effects to (S)(-)-Bay K8644. The action of the of (R)(+)-Bay K8644 was studied in rat tail artery and guinea pig ileal longitudinal smooth muscle using pharmacologic and radioligand binding assays. (R)(+)-Bay K8644 inhibited the responses to KCI-induced depolarization with IC50 values of 16.1-25.6 nM.
