N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE C화학적 특성, 용도, 생산
개요
Colforsin daropate was launched in Japan as a treatment for acute
heart failure. It is a water-soluble and orally active 3-dimethylaminopropionyl
(daropate) derivative of forskolin, a labdane-type diterpene isolated from the root
of Coleus forskohlii. It is obtained from forskolin in 7 steps based upon a series
of protections and deprotections of the different OH groups and a key 7,8-
transacylation. Colforsin daropate is the first in its class of adenylate cyclase
activators to be marketed in the treatment of heart failure. As forskolin, it directly
stimulates adenylate cyclase thus increasing intracellular concentration of cAMP
and inhibiting calcium mobilization. As a direct consequence, it induces a
significant vasodilatation, so provides a moderate positive inotropic and
chronotropic effect. In contrast with well-established generators of cAMP
synthesis (dobutamine), Colforsin daropate maintains its action on cardiac
muscle in the severe stage even when the beta-adrenoceptor is down-regulated
in myocardium. In several clinical trials in patients with severe congestive heart
failure (CHF), Colforsin daproate improved hemodynamic symptoms of heart
failure patients without serious adverse effects.
용도
NKH 477 is a water-soluble analog of Forskolin (F701800), that is a potent activator of adenylyl cyclase, which shows some selectivity for cardiac (type V) adenylyl cyclase).
생물학적 활성
Water-soluble analog of forskolin ([3R-(3a,4ab,5b,6b,6aa,10a,10ab,10ba)]-5-(Acetyloxy)-3-ethenyldodecahydro-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1H-naphtho[2,1-b]pyran-1-one ) that is a potent activator of adenylyl cyclase; shows some selectivity for cardiac (type V) adenylyl cyclase. Stimulates bronchodilation (EC 50 = 32.6 nM) and is an orally active potent positive chronotrope and hypotensive agent in vivo . Also available as part of the PKA Tocriset™ .
N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE 준비 용품 및 원자재
원자재
준비 용품
N,N-DIMETHYL-(3R,4AR,5S,6AS,10S,10AR,10BS)-5-(ACETYLOXY)-3-ETHENYLDODECAHYDRO-10,10B-DIHYDROXY-3,4A,7,7,10A-PENTAMETHYL-1-OXO-1H-NAPHTHO[2,1-B]PYRAN-6-YL ESTER B-ALANINE HYDROCHLORIDE 공급 업체
