Merrell Pharmaceuticals, Inc.

Merrell Dow Pharmaceuticals

Stephen H Buck

Scott L Harbeson

James R McCarthy

John L Krstenansky

Elizabeth M Kudlacz

Shigetada Nakanishi

Thomas J Owen

Henry J Yamamura

William R Roeske

Alden Keith Henderson

Josephine Yuen-Wai Lai

Chester F Hassman, Iii

James R Mccarthy

Chester F Hassman

Antagonists of neurokinin A which are derivatives of naturally occurring neurokinin A in which the amide bond connecting the two amino acids on the carboxy terminal end is modified are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.

Neurokinin A antagonists

A method for producing high level expression of neuropeptide receptors and stable cell lines useful therein. This method involves culturing a cell line containing amplified copies of a cDNA sequence encoding a neuropeptide receptor containing an expression control sequence taken from the .beta.-actin transcriptional control element.

Neurokinin receptor cell lines

Cyclic neurokinin A antagonists

Antagonists of neurokinin A which are novel cyclic hexapeptide and octapeptide compounds are described. The antagonism is confirmed using conventional competitive binding and biochemical assays as well as conventional physiological tests and the use of these derivatives in a variety of conditions in which neurokinin A is implicated is also described.

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Cincinnati, OH, United States of America

Stephen H Buck