JP-1302 (hydrochloride) 是 alpha2C-adrenoceptor (α2C-adrenoceptor) 的选择性高亲和力拮抗剂,Kb 值(拮抗剂活性)为 16 nM,Ki(结合亲和力)值为 28 nM。
Cas No. | 1259314-65-2 |
Canonical SMILES | CN1CCN(C2=CC=C(NC3=C(C=CC=C4)C4=NC5=C3C=CC=C5)C=C2)CC1.Cl.Cl |
分子式 | C24H24N4•2HCl |
分子量 | 441.4 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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描述 | JP-1302 is an antagonist of α2-adrenergic receptors (α2-ARs) that is selective for α2C-ARs over α2A- and α2B-ARs (Kis = 28, 3,150, and 1,470 nM, respectively). It reduces immobility time in the forced swim test in mice when administered at doses of 1, 3, and 10 µmol/kg. JP-1302 (5 mg/kg) reverses phencyclidine-induced decreases in prepulse inhibition of the acoustic startle response in rats. It dose-dependently reduces haloperidol-induced bradykinesia and catalepsy in mice. JP-1302 (0.3 mg/kg) also increases systolic blood pressure in rats. |