Characterization of the vasoinhibitory actions of KT2-230, a new benzothiazepine vasodilator derivative on isolated rabbit vascular smooth muscles: An alpha-adrenergic- and serotonergic-receptor antagonist

Add time:07/25/2019    Source:sciencedirect.com

1. Pharmacological properties of KT2-230 (benzothiazepine derivative), a newly synthesized vasorelaxing agent, were studied.2. In the anesthetized dogs, KT2-230 increased the femoral and vertebral blood flow without effect on systemic blood pressure.3. In rabbit aorta, KT2-230, methysergide and phentolamine inhibited contractile responses to 5-hydroxytryptamine.4. The response to norepinephrine was also inhibited by KT2-230 and phentolamine. Responses to histamine were not affected by KT2-230.5. Responses to KCl and Ca2+ in K+ depolarized aorta in Ca2+-free medium were inhibited by a high concentration of KT2-230.6. In rabbit iliac artery, KT2-230 inhibited the response to caffeine in Ca2+-free medium.7. KT2-230 decreased total La3+-resistant Ca2+-binding at high affinity sites.8. These results indicate that KT2-230 inhibits α1-adrenoceptors and 5-HT-receptors and at high concentrations it inhibits slow Ca2+-channels. KT2-230 may inhibit the Ca2+ release from caffeine- and agonist-sensitive Ca2+ stores.

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