Biomaterial Database

N-substituted-3-arylpyrrolidines: potent and selective ligands at serotonin 1A receptor. 1999

K H Ahn, and S J Lee, and C H Lee, and C Y Hong, and T K Park

Department of Chemistry and Center for Biofunctional Molecules, POSTECH, Pohang, Korea. ahn@vision.postech.ac.kr

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.

UI	MeSH Term	Description	Entries
D008024	Ligands	A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)	Ligand
D011485	Protein Binding	The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.	Plasma Protein Binding Capacity,Binding, Protein
D011759	Pyrrolidines	Compounds also known as tetrahydropyridines with general molecular formula (CH2)4NH.	Tetrahydropyridine,Tetrahydropyridines
D011985	Receptors, Serotonin	Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.	5-HT Receptor,5-HT Receptors,5-Hydroxytryptamine Receptor,5-Hydroxytryptamine Receptors,Receptors, Tryptamine,Serotonin Receptor,Serotonin Receptors,Tryptamine Receptor,Tryptamine Receptors,Receptors, 5-HT,Receptors, 5-Hydroxytryptamine,5 HT Receptor,5 HT Receptors,5 Hydroxytryptamine Receptor,5 Hydroxytryptamine Receptors,Receptor, 5-HT,Receptor, 5-Hydroxytryptamine,Receptor, Serotonin,Receptor, Tryptamine,Receptors, 5 HT,Receptors, 5 Hydroxytryptamine
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D001522	Behavior, Animal	The observable response an animal makes to any situation.	Autotomy Animal,Animal Behavior,Animal Behaviors
D044263	Receptors, Serotonin, 5-HT1	A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.	Serotonin 5-HT1 Receptor,Serotonin Receptors, 5-HT1,5-HT1 Receptor,5-HT1 Receptors,Serotonin 5-HT1 Receptors,Serotonin, 5-HT1 Receptors,5 HT1 Receptor,5 HT1 Receptors,5-HT1 Receptor, Serotonin,5-HT1 Receptors Serotonin,5-HT1 Receptors, Serotonin,5-HT1 Serotonin Receptors,Receptor, 5-HT1,Receptor, Serotonin 5-HT1,Receptors Serotonin, 5-HT1,Receptors, 5-HT1,Receptors, 5-HT1 Serotonin,Receptors, Serotonin 5-HT1,Serotonin 5 HT1 Receptor,Serotonin 5 HT1 Receptors,Serotonin Receptors, 5 HT1,Serotonin, 5 HT1 Receptors
D051381	Rats	The common name for the genus Rattus.	Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus
D018490	Serotonin Agents	Drugs used for their effects on serotonergic systems. Among these are drugs that affect serotonin receptors, the life cycle of serotonin, and the survival of serotonergic neurons.	Serotonergic Agents,Serotonergic Drugs,Serotonin Drugs,Serotonin Effect,Serotonin Effects,Serotoninergic Effect,Serotoninergic Effects,Agents, Serotonergic,Agents, Serotonin,Drugs, Serotonergic,Drugs, Serotonin,Effect, Serotonin,Effect, Serotoninergic,Effects, Serotonin,Effects, Serotoninergic