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Am J Physiol Gastrointest Liver Physiol 254: G883-G890, 1988;
0193-1857/88 $5.00
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AJP - Gastrointestinal and Liver Physiology, Vol 254, Issue 6 883-G890, Copyright © 1988 by American Physiological Society

ARTICLES

Characterization of ability of various substance P antagonists to inhibit action of bombesin

R. T. Jensen, P. Heinz-Erian, S. Mantey, S. W. Jones and J. D. Gardner
Digestive Diseases Branch, National Institute of Diabetes and Digestive and Kidney Diseases, Bethesda, Maryland 20892.

In the present study the ability of two classes of substance P (SP) antagonists to affect SP- and bombesin (Bn)-stimulated amylase release, as well as binding of 125I-Bolton-Hunter (BH)-SP and 125I-[Tyr4]Bn, was studied to determine their mechanism of action and the relationship between inhibition of the action of SP and the action of Bn. Four SP analogues ([D-Pro2,D-Phe7,D-Trp9]SP, [D-Pro2,D-Trp7,9]SP, [D-Arg1,D-Pro2,D-Trp7,9,Leu11]SP, and [D-Arg1,D-Trp7,9,Leu11]SP) and two SP-(4-11) analogues ([D-Pro4,D-Trp7,9]SP-(4-11) and [D-Pro4,D-Trp7,9,10]SP-(4-11)] did not stimulate amylase release when present alone but inhibited SP- and Bn-stimulated amylase release. For each SP analogue, inhibition was specific for peptides that stimulate release by interacting with SP or Bn receptors, whereas both SP-(4-11) analogues also inhibited cholecystokinin-stimulated amylase release. Each SP analogue's inhibition of Bn-stimulated amylase release was reversible. Each analogue inhibited binding of 125I-BH-SP with the same potency as it inhibited SP-stimulated amylase release and 125I-[Tyr4]Bn binding with the same potency as it inhibited Bn-stimulated amylase. In contrast, SP itself or SP-(4-11) itself did not inhibit Bn-stimulated amylase release or binding of 125I-[Tyr4]Bn. The relative affinities of the analogues for interacting with Bn and SP receptors differed. None of the analogues increased the dissociation of bound 125I-BH-SP or 125I-[Tyr4]Bn.(ABSTRACT TRUNCATED AT 250 WORDS)


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R. R. Ryan, H. C. Weber, W. Hou, E. Sainz, S. A. Mantey, J. F. Battey, D. H. Coy, and R. T. Jensen
Ability of Various Bombesin Receptor Agonists and Antagonists to Alter Intracellular Signaling of the Human Orphan Receptor BRS-3
J. Biol. Chem., May 29, 1998; 273(22): 13613 - 13624.
[Abstract] [Full Text] [PDF]


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