| Identification | Back Directory | [Name]
L-Norleucinamide, N2-[(1,1-dimethylethoxy)carbonyl]-L-arginyl-L-alanyl-D-tryptophyl-L-phenylalanyl-D-prolyl-L-prolyl- | [CAS]
141636-44-4 | [Synonyms]
L-Norleucinamide, N2-[(1,1-dimethylethoxy)carbonyl]-L-arginyl-L-alanyl-D-tryptophyl-L-phenylalanyl-D-prolyl-L-prolyl- | [Molecular Formula]
C50H72N12O9 | [MOL File]
141636-44-4.mol | [Molecular Weight]
985.18 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Intravenous administration of GR 83074 (Compound 10) to anaesthetized, artificially-respired guinea-pigs (0.3 μmol/kg) causes a marked antagonism of the increase in tracheal insufflation pressure induced by the NK-2 agonist, GR64349[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. DOI:10.1021/jm00092a008 |
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fuanbio.com |
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