PRX-07034 (hydrochloride)

PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a K_i= 4-8 nM and an IC₅₀ of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility^[1]. In Vitro: PRX-07034 is both a potent and highly selective 5-HT6 receptor antagonist (≥100-fold selectivity for the 5-HT6 receptor compared to 68 other GPCRs, ion channels, and transporters. PRX-07034 inhibits 5-HT1A, 5-HT1B, 5-HT1D, Dopamine D3, Histamine H2, and Opioid μ receptor with K_is of 420 nM, 260 nM, 2.8 µM, 71 nM, 0.64 µM, and 0.45 µM, respectively. PRX-07034 inhibits 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC₅₀s of 2.5 µM, 2.5 µM, and 3.7 µM, respectively^[1].
In functional assays, PRX-07034 demonstrates low antagonist activity for the dopamine D3 receptor (IC₅₀=4.8 µM) and very low agonistic activity for the opioid μ-receptor (EC₅₀=19 µM) ^[1]. In Vivo: PRX-07034 (0.1, 1, or 3 mg/kg; i.p.; 30 min prior to delayed spontaneous alternation testing) selectively enhances a switch to a place discrimination^[1].