产品
编 号：F034499
分子式：C34H36FN5O2
分子量：565.68
分子式：C34H36FN5O2
分子量：565.68
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CAS No: 1094873-17-2
产品详情
生物活性：
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
体内研究：
(R)-JNJ-31020028 (5.6 μg; chronic icv infusion; daily for 10 days) has antidepressant like effects in the olfactory bulbectomized rat (OBX) model.Chronic icv administration of (R)-JNJ-31020028 at 5.6 μg/day using osmotic Alzet pump resulted in a significant decreases number of grooming events.(R)-JNJ-31020028 treatment shows the Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively.Animal Model:Male Sprague Dawley rats weighing 150-170 (OBX model)
Dosage:5.6 μg
Administration:chronic icv infusion; daily for 10 days
Result:Reduced OBX rat immobility time.
Animal Model:male Sprague-Dawley rat
Dosage:10 mg/kg
Administration:s.c. (Pharmacokinetic Analysis)
Result:The Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively.
(R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
体内研究：
(R)-JNJ-31020028 (5.6 μg; chronic icv infusion; daily for 10 days) has antidepressant like effects in the olfactory bulbectomized rat (OBX) model.Chronic icv administration of (R)-JNJ-31020028 at 5.6 μg/day using osmotic Alzet pump resulted in a significant decreases number of grooming events.(R)-JNJ-31020028 treatment shows the Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively.Animal Model:Male Sprague Dawley rats weighing 150-170 (OBX model)
Dosage:5.6 μg
Administration:chronic icv infusion; daily for 10 days
Result:Reduced OBX rat immobility time.
Animal Model:male Sprague-Dawley rat
Dosage:10 mg/kg
Administration:s.c. (Pharmacokinetic Analysis)
Result:The Cmax, Tmax , AUCinf, Vd, and t1/2 were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively.
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