GR 83074

Names

[ CAS No. ]:
141636-44-4

[ Name ]:
GR 83074

Biological Activity

[Description]:

GR 83074 is a potent and selective NK-2 (Neurokinin Receptor) antagonist with a pKB of 8.23. GR 83074 is inactive as an NK-3 antagonist and exhibits a 340-fold NK-2/NK-1 selectivity[1].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor
Research Areas >> Neurological Disease
Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

[In Vitro]

在离体大鼠结肠和豚鼠气管中，GR 83074 是选择性 NK-2 激动剂 GR6434 诱导的收缩的有效竞争性拮抗剂[1]。

[In Vivo]

对麻醉的人工呼吸豚鼠静脉注射 GR 83074 (compound 10) (0.3 μmol/kg) 可显着拮抗 NK-2 激动剂 GR64349 引起的气管充气压力增加[1]。

[References]

[1]. A B McElroy, et al. Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J Med Chem. 1992 Jul 10;35(14):2582-91.  

Chemical & Physical Properties

[ Molecular Formula ]:
C50H72N12O9

[ Molecular Weight ]:
985.18

Related Compounds