Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor

AB McElroy, SP Clegg, MJ Deal, GB Ewan…

Index: McElroy, Andrew B.; Clegg, Stephen P.; Deal, Martyn J.; Ewan, Georg B.; Hagan, Russell M.; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 14 p. 2582 - 2591

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Citation Number: 75

Abstract

Incorporation of pro^ into substance P related peptides is known to enhance neurokinin NK- 2 receptor agonist potency and selectivity with respect to other neurokinin receptors. We now report that replacement of D-wg by D-Pros in the nonselective neurokinin antagonist [Ar $,~-Trp'*~, Nle" 1-SP (5-11) gave a partial agonist with NK-2 receptor selectivity. Further incorporation of Prolo provided the weak but selective NK-2 antagonist Arg-Ala-D-Trp-Phe ...