| Bioactivity | NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor[1]. | ||||||||||||
| In Vivo | NPY5RA-972(p.o., 10.5 mg/kg) 在大鼠中的 Tmax 值为 1 小时,此时 Cmax 为 35 μM,半衰期为 6.4 小时,且即使在给药后 24 小时总血浆浓度仍大于3 μM/h[1]。NPY5RA-972 (p.o., 1-10 mg/kg) 抑制了由选择性 NPY Y5 受体激动剂引起的食物摄入,但对自由喂养的 Wistar 大鼠或膳食肥胖大鼠的摄食量或体重均无影响[1]。 | ||||||||||||
| Name | NPY5RA-972 | ||||||||||||
| CAS | 439861-56-0 | ||||||||||||
| Formula | C21H25N3O2 | ||||||||||||
| Molar Mass | 351.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Andrew V Turnbull, et al. Selective antagonism of the NPY Y5 receptor does not have a major effect on feeding in rats. Diabetes. 2002 Aug;51(8):2441-9. |