PRX-07034

PRX-07034 is a selective antagonist of 5-HT6 receptor. It has cognition and memory-enhancing properties and potently decreases food intake and body weight in rodents. PRX-07034 is both a potent (Ki = 4-8 nM) and highly selective 5-HT (6) receptor antagonist (≥100-fold selectivity for the 5-HT (6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D (3) (Ki = 71 nM) and 5-HT (1B) (Ki = 260 nM) receptors.PRX-07034 is both a potent (Ki = 4-8 nM) and highly selective 5-HT (6) receptor antagonist (100-fold selectivity for the 5-HT (6) receptor compared to 68 other GPCRs, ion channels, and transporters, except D (3) (Ki = 71 nM) and 5-HT (1B) (Ki = 260 nM) receptors. For cyclic AMP quantification, PRX-07034 demonstrated antagonist activity (IC (50) = 19 nM) without an effect on basal levels and did not show any agonist activity up to 10 μM. PRX-07034 at 1 and 3 mg/kg (but not 0.1 mg/kg) significantly enhanced delayed spontaneous alternation. The drug at 1 and 3 mg/kg also enhanced switching between a place and response strategy, but did not affect initial learning of either a place or response discrimination.