PRX-07034 hydrochloride

• CAT Number: I014831
• CAS Number: 903580-39-2
• Molecular Formula: C21H29Cl2N3O4S
• Molecular Weight: 490.44
• Purity: ≥95%
• Synonyms: N-[1-(5-chloro-2,3-dimethoxyphenyl)ethyl]-2-methylsulfonyl-5-piperazin-1-ylaniline;hydrochloride
• InChI: InChI=1S/C21H28ClN3O4S.ClH/c1-14(17-11-15(22)12-19(28-2)21(17)29-3)24-18-13-16(25-9-7-23-8-10-25)5-6-20(18)30(4,26)27;/h5-6,11-14,23-24H,7-10H2,1-4H3;1H
• InChIKey: PILCQJJJAFRKHO-UHFFFAOYSA-N
• SMILES: CC(C1=C(C(=CC(=C1)Cl)OC)OC)NC2=C(C=CC(=C2)N3CCNCC3)S(=O)(=O)C.Cl

PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 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].
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 Kis 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].
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].

Reference

[1]. Eric G Mohler, et al. The effects of PRX-07034, a novel 5-HT6 antagonist, on cognitive flexibility and working memory in rats. Psychopharmacology (Berl). 2012 Apr;220(4):687-96.
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