NPY 5RA972

Names

[ Name ]:
NPY 5RA972

[Synonym ]:
n-[4-methyl-9-(1-methylethyl)-9h-carbazol-3-yl]-4-morpholinecarboxamide

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Neuropeptide Y Receptor

[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]。

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₂₅N₃O₂

[ Molecular Weight ]:
351.44200

[ Exact Mass ]:
351.19500

[ PSA ]:
49.99000

[ LogP ]:
4.49940

Related Compounds

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