SUVN-G3031 (Samelisant) is a potent, selective, orally active histamine H3 receptor (H3R) inverse agonist with Ki of 8.73 nM (hH3R).
SUVN-G3031 exhibited an IC50 of 20 nM with progressive inhibition of (R)-α-methylhistamine (0.03 µM) induced agonist activity in [35S]-GTPγS binding assay using CHO-K1 cells expressing human H3R membranes。
SUVN-G3031 reverses (R)-α-methylhistamine induced dipsogenia in vivo.
