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Effect of a New Dual Neurokinin Antagonist on Airway Smooth Muscle in Situ

T Shioya, M Kagaya, M Sano, M Itaba, T Shindo, T Fujii, M Miura

Arzneimittelforschung. 1995 Nov;45(11):1194-7.

PMID: 8929238

Abstract:

The effect of FK224 (N-(N2-[N-¿N-(N-2,3-didehydro-N-methyl-N-[N-3- (2-pentylphenyl)-propionyl¿-L-threonyl]tyrosyl-L-leucynyl)-D -phenylalanyl¿-L-allothreonyl]-L-asparaginyl)-L-serine-v-lacto ne, CAS 125787-94-2) on isometric contraction of canine tracheal smooth muscle in situ was studied. Contraction was induced by administration of substance P, neurokinin A, and neurokinin B intra-arterially into the tracheal circulation in five mongrel dogs. FK224 inhibited substance P- and neurokinin A-induced contraction in a dose-dependent manner, but it did not inhibit neurokinin B-induced contraction significantly. These data suggest that FK224 is a dual antagonist of both neurokinin 1 and neurokinin 2 receptors, with a similar potency in in vivo experiments.

Chemicals Related in the Paper:

Catalog Number Product Name Structure CAS Number Price
AP56451-A L-Serine - CAS 56-45-1 L-Serine - CAS 56-45-1 56-45-1 Price
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