N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor.
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.
Ahn
K H
KH
Department of Chemistry and Center for Biofunctional Molecules, POSTECH, Pohang, Korea. ahn@vision.postech.ac.kr
Lee
S J
SJ
Lee
C H
CH
Hong
C Y
CY
Park
T K
TK
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D008024:Ligands; D011485:Protein Binding; D011759:Pyrrolidines / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology; D051381:Rats; D011985:Receptors, Serotonin / Q000378:metabolism*; D044263:Receptors, Serotonin, 5-HT1; D018490:Serotonin Agents / Q000138:chemical synthesis / Q000378:metabolism* / Q000494:pharmacology
D008024:Ligands; D011759:Pyrrolidines; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D018490:Serotonin Agents