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Peer-reviewed veterinary case report

Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2006
Authors:
Adams, David R et al.
Affiliation:
Vernalis plc · United Kingdom
Species:
rodent

Abstract

A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was synthesised and evaluated as 5-HT(2C) receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for the compounds at 5-HT(2) receptor subtypes are reported. The analogue which showed the highest 5-HT(2C) binding affinity (27, 1.6nM) was found to be successful in reducing food intake in rats.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/16257207/