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141636-44-4

141636-44-4 Structure

141636-44-4 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[density ]

1.36±0.1 g/cm3(Predicted)
[pka]

11.23±0.46(Predicted)
[Sequence]

{Boc}-Arg-Ala-{D-Trp}-Phe-{D-Pro}-Pro-{Nle}-NH2
Hazard InformationBack 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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