An α2C-adrenergic receptor antagonist
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).1 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.2 JP-1302 (0.3 mg/kg) also increases systolic blood pressure in rats.3
1.Sallinen, J., H?glund, I., Engstr?m, M., et al.Pharmacological characterization and CNS effects of a novel highly selective α2C-adrenoceptor antagonist JP-1302Br. J. Pharmacol.150(4)391-402(2007) 2.Imaki, J., Mae, Y., Shimizu, S., et al.Therapeutic potential of α2 adrenoceptor antagonism for antipsychotic-induced extrapyramidal motor disordersNeurosci. Lett.454(2)143-147(2009) 3.Zefirov, T.L., Khisamieva, L.I., Ziyatdinova, N.I., et al.Effect of selective blockade of α?-adrenoceptor subtypes on cardiovascular system in ratsBull. Exp. Biol. Med.158(4)410-412(2015)
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