PRX-07034

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PRX-07034 是 5-HT6 受体的选择性拮抗剂。它具有增强认知和记忆的特性，可有效减少啮齿动物的食物摄入量和体重。 PRX-07034 是一种有效 (Ki = 4-8 nM) 和高选择性 5-HT(6) 受体拮抗剂（与 68 种其他 GPCR、离子通道、和转运蛋白，D(3) (Ki = 71 nM) 和 5-HT(1B) (Ki = 260 nM) 受体除外。

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.

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.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) .

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. Animal Model:Male Long-Evans rats weighing approximately 350 gDosage:0.1, 1, or 3 mg/kg Administration:Injected intraperitoneal Result: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)

In Vitro:?DMSO : 31.25 mg/mL (63.72 mM)

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

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(-20℃)

With Ice Pack

≥ 2 years