Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity

M Isaac; A Slassi; A O'Brien; L Edwards; N MacLean; D Bueschkens; D K Lee; K McCallum; I De Lannoy; L Demchyshyn; R Kamboj

doi:10.1016/s0960-894x(00)00141-4

Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity

Bioorg Med Chem Lett. 2000 May 1;10(9):919-21. doi: 10.1016/s0960-894x(00)00141-4.

Authors

M Isaac¹, A Slassi, A O'Brien, L Edwards, N MacLean, D Bueschkens, D K Lee, K McCallum, I De Lannoy, L Demchyshyn, R Kamboj

Affiliation

¹ NPS Allelix Corp., Mississauga, ON, Canada. misaac@allelix.com

PMID: 10853660
DOI: 10.1016/s0960-894x(00)00141-4

Abstract

A series of pyrrolo[3,2,1-ij]quinoline derivatives was synthesized, evaluated for their activity against the 5-HT2c and 5-HT2a, receptors and found to be agonists at 5-HT2c with selectivity over 5-HT2a.

MeSH terms

Anti-Obesity Agents / chemical synthesis*
Anti-Obesity Agents / pharmacology
Anticonvulsants / chemical synthesis*
Anticonvulsants / pharmacology
Cell Line
Humans
Pyrroles / chemical synthesis*
Pyrroles / pharmacology
Quinolines / chemical synthesis*
Quinolines / pharmacology
Receptor, Serotonin, 5-HT2A
Receptor, Serotonin, 5-HT2C
Receptors, Serotonin / drug effects*
Serotonin Receptor Agonists / chemical synthesis*
Serotonin Receptor Agonists / pharmacology
Stereoisomerism
Structure-Activity Relationship

Substances

Anti-Obesity Agents
Anticonvulsants
Pyrroles
Quinolines
Receptor, Serotonin, 5-HT2A
Receptor, Serotonin, 5-HT2C
Receptors, Serotonin
Serotonin Receptor Agonists