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编 号:F599838
分子式:C24H24N4
分子量:368.47
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生物活性:
JP1302 is a potent, selective, high affinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research.

体内研究:
JP1302 (1-10 μmol/kg) decreases immobility time in the FST to a level similar to that seen with 10-30?μmol/kg of the antidepressant Desipramine (HY-B1272A).JP1302 (5 μmol/kg, once) is capable of complete reversal of the impairment in PPI induced in Sprague-Dawley rats by the psychotomimetic NMDA receptor antagonist, phencyclidine and similar results are found in Wistar rats.JP1302 (3 mg/kg, IV, once) significantly ameliorates renal dysfunction.Animal Model:Male Sprague Dawley rats (8 weeks old)
Dosage:3 mg/kg
Administration:IV, pre-treatment: administered 5 min before the induction of ischemia, post-treatment: injected 45 min after the initiation of reperfusion
Result:Significantly ameliorated renal dysfunction in the rats at 24 h after reperfusion. post-ischemic administration of JP-1302 significantly ameliorated renal dysfunction, histological damage and reduced apoptotic cells and pro-inflammatory cytokine mRNA expression.

体外研究:
JP1302 shows about 100-fold higher affinity than for α2A or α2B.
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