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25 May 2010 - Just published: articles on a new-generation 5-HT1A agonist

Another research paper has just been published describing a novel ligand that preferentially activates frontal cortex serotonin 5-HT1A sites.

F15599, is highly selective for 5-HT1A receptors and potently activates cortical sites at doses that do not activate 5-HT1A autoreceptors. This translates to a favourable profile in tests of anti-depressant like activity and cognition without inducing serotonin syndrome(Depoortère et al., 2010; Assié et al., 2010). At a molecular level, F15599 preferentially activates G-proteins  of the Galpha-i subtype rather than Galpha-o. I also activates ERK1/2 phosphorylation more potently than other signal transuction pathways (Newman-Tancredi et al., 2009).
These data suggest that a new generation of functionally-selective 5-HT1A agonists may provide a strategy for improved therapy via this target. For more information Contact.
 

F15599, a preferential post-synaptic 5-HT(1A) receptor agonist: Activity in models of cognition in comparison with reference 5-HT(1A) receptor agonists.
Depoortère R, Auclair AL, Bardin L, Colpaert FC, Vacher B, Newman-Tancredi A.
Eur Neuropsychopharmacol. 2010 May 18. [Epub ahead of print]
 

F15599, a highly selective post-synaptic 5-HT1A receptor agonist: in-vivo profile in behavioural models of antidepressant and serotonergic activity.
Assié MB, Bardin L, Auclair AL, Carilla-Durand E, Depoortère R, Koek W, Kleven MS, Colpaert F, Vacher B, Newman-Tancredi A.
Int J Neuropsychopharmacol. 2010 Jan 11:1-14. [Epub ahead of print]
 

Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist.
Newman-Tancredi A, Martel JC, Assié MB, Buritova J, Lauressergues E, Cosi C, Heusler P, Bruins Slot L, Colpaert FC, Vacher B, Cussac D.
Br J Pharmacol. 2009 Jan;156(2):338-53. Epub 2009 Jan 12.