EGIS-7625 free base

EGIS-7625 free base is an orally active and selective competitive antagonist of 5-HT2B receptor, with a human K i value of 1 nM. EGIS-7625 free base shows low affinity for 5-HT2A and 5-HT2C receptors. The pK i values of EGIS-7625 free base for human 5-HT2B, 5-HT2A and 5-HT2C are 9.0, 6.2 and 7.7, respectively. EGIS-7625 free base alleviates mCPP-induced hypoactivity ^[1].

In Vivo, EGIS-7625 (30 mg/kg; subcutaneous injection; single dose) free base does not antagonize mCPP-induced 5-HT2C receptor-mediated feeding suppression in rats^[1]. EGIS-7625 (3-30 mg/kg; p.o.; single administration) free base 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].

In Vitro, EGIS-7625 (1-10 nM) free base 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) free base 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].

References:
[1]. Kovács A, et al. Effects of EGIS-7625, a selective and competitive 5-HT2B receptor antagonist. Cardiovasc Drugs Ther. 2003;17(5-6):427-434.