179756-58-2

Eptapirone is a potent agonist of the serotonin (5-HT) receptor subtype 5-HT_1A (K_i = 4.8 nM in a radioligand binding assay). It is selective for 5-HT_1A over other 5-HT receptor subtypes, dopamine D₂ receptors, α₁-adrenergic receptors, and histamine H₁ receptors (K_is = <10,000, 1,770, 691.8, and <10,000 nM, respectively). Eptapirone inhibits cAMP stimulation induced by forskolin in HA7 cells transfected with human 5-HT_1A receptors (EC₅₀ = 158 nM). In vivo, eptapirone increases extracellular 5-HT in the ventral hippocampus of rats (ED₅₀ = 0.049 mg/kg) and serum corticosterone levels when administered p.o. or i.p. (ED₅₀s = 0.16 and 0.057 mg/kg, respectively). It decreases immobility in rats in a forced swim test and increases punished responding in a pigeon conflict procedure, demonstrating antidepressant-like and anxiolytic activity. Eptapirone (2.5 mg/kg, p.o.) also attenuates hypertension and tachycardia induced by sibutramine in rats with no effect on sibutramine-induced hypophagia.

Eptapirone is 5-HT1A receptor agonist with anxiolytic and antidepressant potential.

ChEBI: Eptapirone is a N-arylpiperazine.

5-HT_1A Receptor

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[2] GERARD H. THOMAS. 5-HT1A Activation Counteracts Cardiovascular But Not Hypophagic Effects of Sibutramine in Rats[J]. Obesity, 2012, 17 3: 467-473. DOI: 10.1038/oby.2008.550