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Eptapirone (F-11,440) is a very potent and highly selective 5-HT1A receptor full agonist of the azapirone class. Its affinity for the 5-HT1A receptor is 4.8 nM (Ki) or 8.33 (pKi), and its intrinsic activity is 100% or equal to that of serotonin.

Eptapirone and its relatives such as F-13,640 and F-15,599 were developed under the notion that high receptor-activating efficacy is required for the maximal therapeutic benefits of 5-HT1A receptor agonists to be realized, underlying the poor clinical effectiveness of currently marketed agents like buspirone and tandospirone which act as mere weak-moderate partial agonists.

In the forced swim test, eptapirone suppresses immobility more robustly than buspirone, ipsapirone, flesinoxan, paroxetine, and imipramine, indicating that it possesses powerful antidepressant effects which may be superior to those of currently available pharmaceuticals. In this test, unlike the other agents screened, buspirone actually increases immobility time with a single administration, while repeated administration decreases it, likely as a result of buspirone's very poor intrinsic activity (~30%) in activating the 5-HT1A receptor.

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This page contains text from Wikipedia, the Free Encyclopedia - http://en.wikipedia.org/wiki/Eptapirone

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