(S)(-)-Bay K8644 is an L-type Ca2+-channel activator with positive inotropic, vasoconstrictive and behavioral effects in vivo. It is an enantiomer of (±)-Bay K8644. (S)(-)-Bay K8644 is a dihydropyridine that can, among other effects, constrict blood vessels and increase the force of contraction of the heart. The drug is thought to increase the entry of Ca2+ into cells by increasing the open-state probability of Ca2+ channels, either by prolonging the duration of individual openings or by increasing the number of openings. It was noted in early experiments with Bay K8644 that the dose-response curve is biphasic. The action of (S)(-)-Bay K8644 was studied in rat tail artery and guinea pig ileal longitudinal smooth muscle using pharmacologic and radioligand binding assays. It induced concentration-dependent contractions in both smooth muscle preparations with EC50 values of 1.98-11 nM. With increasing concentrations, (S)(-)-Bay K8644 relaxed the tissue with IC50 values of 0.53-2.60 μM.
产品描述
An Activator of L-Type CaV Channels
产品形式
(S)(-)-Bay K8644 is an L-type Ca2+-channel activator with positive inotropic, vasoconstrictive and behavioral effects in vivo. It is an enantiomer of (±)-Bay K8644. (S)(-)-Bay K8644 is a dihydropyridine that can, among other effects, constrict blood vessels and increase the force of contraction of the heart. The drug is thought to increase the entry of Ca2+ into cells by increasing the open-state probability of Ca2+ channels, either by prolonging the duration of individual openings or by increasing the number of openings. It was noted in early experiments with Bay K8644 that the dose-response curve is biphasic. The action of (S)(-)-Bay K8644 was studied in rat tail artery and guinea pig ileal longitudinal smooth muscle using pharmacologic and radioligand binding assays. It induced concentration-dependent contractions in both smooth muscle preparations with EC50 values of 1.98-11 nM. With increasing concentrations, (S)(-)-Bay K8644 relaxed the tissue with IC50 values of 0.53-2.60 μM.