(R)-JNJ-31020028 是一种高亲和力，选择性，透过血脑屏障的神经肽 Y Y2 受体 (neuropeptide Y Y2 receptor) 拮抗剂，对人，大鼠和小鼠 Y2 受体的pIC50分别为 8.07、8.22 和 8.21。 (R)-JNJ-31020028 与人类Y1，Y4 和 Y5 受体相比，显示出大于 100 倍的选择性。(R)-JNJ-31020028 具有抗抑郁样作用。
| 生物活性 | (R)-JNJ-31020028 is a high affinity, selective brain penetrantneuropeptide Y Y2 receptorantagonist, withpIC50values 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[1][2]. |
| IC50& Target[1] | human Y2receptor 8.07 (pIC50) | rat Y2receptor 8.22 (pIC50) | mouse Y2receptor 8.21 (pIC50) |
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体内研究
(In Vivo) | (R)-JNJ-31020028 (5.6 μg; chronic icv infusion; daily for 10 days) has antidepressant like effects in the olfactory bulbectomized rat (OBX) model[1].
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[1].
(R)-JNJ-31020028 treatment shows the Cmax, Tmax, AUCinf, Vd, and t1/2were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively[1].
| Animal Model: | Male Sprague Dawley rats weighing 150-170 (OBX model)[1] | | Dosage: | 5.6 μg | | Administration: | chronic icv infusion; daily for 10 days | | Result: | Reduced OBX rat immobility time. |
| Animal Model: | male Sprague-Dawley rat[2] | | Dosage: | 10 mg/kg | | Administration: | s.c. (Pharmacokinetic Analysis) | | Result: | The Cmax, Tmax, AUCinf, Vd, and t1/2were 4.35 μM, 0.5 hours, 7.91 h μM and 0.83 hours, respectively. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
