Synthesis and pharmacological testing of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]azepin and its enantiomers in comparison with the two antidepressants mianserin and mirtazapine

被引：33
作者：
Wikström, HV
Mensonides-Harsema, MM
Cremers, TIFH
Moltzen, EK
Arnt, J
机构：
[1] Univ Groningen, Ctr Pharm, Dept Med Chem, NL-9713 AV Groningen, Netherlands
[2] H Lundbeck & Co AS, Dept Med Chem & Pharmacol, Copenhagen, Denmark
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 15期
关键词：
D O I：
10.1021/jm010566d
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis and resolution of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[cf]-pyrazino[1,2-alpha]azepin (6-methoxymianserin, 6) are described. Furthermore, the in vitro and in vivo effects of 6 and its enantiomers are presented. 6 displayed high affinity for the 5-HT2A/2C receptors, only moderate affinity for the adrenoceptors, and no affinity for the NA reuptake site. Surprisingly, 6 also showed moderate to high affinity for the dopamine D2 receptor, an effect that resides in the (R)-(-)-enantiomer.
引用
收藏
页码：3280 / 3285
页数：6
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