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18 April 2011 - Just published: Review of "biased agonism" at 5-HT1A receptors

Recent studies have shown that agonists acting at G-protein coupled receptors (GPCRs) can preferentially activate certain signalling responses whilst other agonists acting at the same receptor can activate different responses. This phenomenon is known as "biased agonism" or "functional selectivity" and offers a means of potentially increasing therapeutic effectiveness and/or decreasing side-effects, if these are associated with specific signaling responses.

However, few well-characterized examples of such agonists have been described and the present review examines the evidence for "biased agonism" at serotonin 5-HT1A receptors, notably as regards the preferential post-synaptic agonist, F15599. Preferential activation of post-synaptic cortical 5-HT1A receptors is a promising strategy for management of a variety of disorders including depression and cognitive deficits.

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Newman-Tancredi A.

Neuropsychiatry, April 2011, Vol. 1, No. 2, Pages 149-164.