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

Autor: Wikstrom, H. V., Mensonides-Harsema, M., M., Cremers, T. I. F. H., Moltzen, E. K., Arnt, J.
Zdroj: Journal of Medicinal Chemistry; July 2002, Vol. 45 Issue: 15 p3280-3285, 6p
Abstrakt: The synthesis and resolution of 1,2,3,4,10,14b-hexahydro-6-methoxy-2-methyldibenzo[c,f]pyrazino[1,2-a]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.
Databáze: Supplemental Index