N-Substituted-3-arylpyrrolidines: Potent and Selective Ligands at Serotonin 1A Receptor

Article abstract of DOI:10.1016/S0960-894X(99)00201-2

3-Arylpyrrolidines are synthesized through the coupling of N-benzyl-3-(methanesulfonyloxy)pyrrolidine with diarylcuprates. Pharmacological evaluation of a series of N-substituted-3-arylpyrrolidines toward several neurotransmitter receptors indicated that some of them are good ligands for serotonin 1A receptor. Particularly, N-<(N-saccharino)butyl>pyrrolidines were found to be potent and selective ligands. A preliminary biological evaluation for several selected compounds indicated that they are potentially effective antianxiety and antidepressant agents.