Vatinoxan hydrochloride | α2A adrenoceptor antagonist

Chemical Structure : Vatinoxan hydrochloride

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Vatinoxan hydrochloride (MK-467, L-659066)

货号: PC-25616Not For Human Use, Lab Use Only.

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生物&药学活性

Vatinoxan hydrochloride (MK-467, L-659066) is a potent and selective alpha-2 adrenoceptor (α2A adrenoceptor, α2AR) antagonist with IC50 of 3 nM against the binding of [3H]rauwolscine to rat cerebrocortical membranes, selective over alpha-1 adrenoceptors.
Vatinoxan has a pA2 of 8.44 at alpha-2 adrenoceptors in the isolated rat vas deferens.
Vatinoxan inhibits the predominately peripherally mediated inhibition of colonic propulsion caused by clonidine in vivo.
Vatinoxan increases sympathetically mediated NE release and catecholamine turnover due to inhibition of presynaptic alpha 2-receptors as well as due to reflexive sympathetic activation related to blockade of alpha 2-receptors on arterial smooth muscle cells.

物理化学性质&存储条件

分子量	454.97
分子式	C20H27ClN4O4S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Methanesulfonamide,N-[2-[(2R,12bS)-1,3,4,6,7,12b-hexahydro-2'-oxospiro[2H-benzofuro[2,3-a]quinolizine-2,4'-imidazolidin]-3'-yl]ethyl]-,hydrochloride (1:1)

参考文献

1. Clineschmidt BV, et al. J Pharmacol Exp Ther. 1988 Apr;245(1):32-40.

2. Szemeredi K, et al. Eur J Pharmacol. 1989 Oct 24;170(1-2):53-9.

Vatinoxan hydrochloride (MK-467, L-659066)

生物&药学活性

物理化学性质&存储条件

参考文献

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Vatinoxan hydrochloride (MK-467, L-659066)

生物&药学活性

物理化学性质&存储条件

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