Based on O ‐methylasparvenone ( 1 ), a N‐free 5HT 2 C antagonist with moderate affinity (p K i = 6.7), derivatives bearing dimethylamino ( 7 ), (dimethylamino)methyl ( 17 , 18 , 21 , and 22 ), and aminomethyl substituents ( 26 ) in place of the benzylic OH group of 1 as well as pyrrolidine‐ ( 33 ) and piperidine‐fused derivatives ( 29 , 43 , and 45 ) were synthesized. In contrast to the lead structure 1 , these new ligands were active in vivo in the rat. The tricycles 33 and 45 display high affinities for the 5HT 2 C receptor (p K i = 8).
No takes yet. Share an insight, caveat, or question.
Bös et al. (1998) studied this question.
Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context: