1,2-ジヒドロ-5-(イミダゾ[1,2-a]ピリジン-6-イル)-6-メチル-2-オキソ-3-ピリジンカルボニトリル·塩酸塩

説明

Coatec was launched in Japan for acute cardiac insufficiency in cases resistant to other treatments. There are three related synthetic routes, 5-6 steps each, to loprinone all converging on 1-(imidazo[1,2a]pyridyl-6-yl)-Zpropanone as an advanced intermediate. It is a potent and selective inhibitor of PDE Ⅲ and a long lasting, orally active, positive inotropic agent. The PDE Ⅲ inhibition caused increased levels of CAMP which leads to the positive inotropic effect that was not altered by β or H₂-preceptor antagonists. It was 100 times less potent at PDE I and PDE Ⅱ with no Na-K-ATPase activity. Improved hemodynamic parameters with slight changes in heart rate and blood pressure were seen in vivo. It is not mutagenic and its primary metabolite was less active.

化学的特性

Off-White Crystalline Powder