产品
编 号:F512857
分子式:C21H29Cl2N3O4S
分子量:490.44
产品类型
结构图
CAS No: 903580-39-2
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产品详情
生物活性:
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.
体内研究:
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 g
Dosage: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.
体外研究:
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) .