Synthesis of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamides and their affinities for 5-HT3 and dopamine D2 receptors.
作者信息
Hirokawa Y, Yoshida N, Kato S
机构信息
Discovery Research Laboratory I, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
出版信息
Bioorg Med Chem Lett. 1998 Jun 16;8(12):1551-4. doi: 10.1016/s0960-894x(98)00258-3.
PMID:9873388
Abstract
A series of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamide derivatives were prepared and evaluated for their binding to 5-HT3 and dopamine D2 receptors. Among them, the 5-bromo-2-methoxy-6-methylaminonicotinamide 16 and its (R)-isomer were found to have potent affinities for both receptors. The affinities of (R)-16 for 5-HT3 and dopamine D2 receptors are approximately 3-fold higher than those of the corresponding benzamide (R)-1 (IC50: 1.1 and 12 nM vs. 2.9 and 35 nM, respectively).
摘要
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