EGIS-7625

EGIS-7625 is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human K_i value of 1 nM. EGIS-7625 shows low affinity for 5-HT2A and 5-HT2C receptors. The pK_i values of EGIS-7625 for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 alleviates mCPP-induced hypoactivity^[1]. In Vitro:EGIS-7625 (1-10 nM) acts as a potent competitive antagonist of 5-HT₂B receptor-mediated contraction in rat fundus strips, with a pA₂ value of 9.4^[1].
EGIS-7625 (1-30 μM; 30 minutes) acts as a weak competitive antagonist of 5-HT₂A receptor-mediated contraction in rabbit pulmonary artery strips, with a pA₂ value of 6.7^[1]. In Vivo:EGIS-7625 (30 mg/kg; subcutaneous injection; single dose) does not antagonize mCPP-induced 5-HT₂C receptor-mediated feeding suppression in rats^[1].
EGIS-7625 (3-30 mg/kg; p.o.; single administration) antagonizes mCPP-induced 5-HT2C receptor-mediated hypoactivity in rats at the highest dose of 30.0 mg/kg, while no significant effects are observed at lower doses^[1].