Competitive binding at a nicotinic receptor transmembrane site of two ?7-selective positive allosteric modulators with differing effects on agonist-evoked desensitization

• Published in: Neuropharmacology Vol. 61; no. 8; pp. 1306 - 1313
• Main Authors: Collins, Toby, Young, Gareth T, Millar, Neil S
• Format: Journal Article
• Language: English
• Published: 01.12.2011

Positive allosteric modulators (PAMs) of nicotinic acetylcholine receptors (nAChRs) have attracted considerable interest as a novel area of therapeutic drug discovery. Two types of ?7-selective PAMs have been identified (type I and type II). Whilst both potentiate peak agonist-induced responses, the...