PRX-07034

Research use only, not for human use.

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 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.

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Endocrinology/Hormones

5-HT Receptor

5-HT6

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903580-39-2

490.44

C21H29Cl2N3O4S

>98% (HPLC)

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Cl.COc1cc(Cl)cc(C(C)Nc2cc(ccc2S(C)(=O)=O)N2CCNCC2)c1OC

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(-20℃)

With Ice Pack

≥ 2 years