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Am J Physiol Endocrinol Metab 263: E712-E717, 1992;
0193-1849/92 $5.00
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AJP - Endocrinology and Metabolism, Vol 263, Issue 4 E712-E717, Copyright © 1992 by American Physiological Society

ARTICLES

Endocrine effects of new bombesin/gastrin-releasing peptide antagonists in rats

J. Pinski, T. Yano, K. Groot, R. Z. Cai, S. Radulovic and A. V. Schally
Endocrine, Polypeptide and Cancer Institute, Department of Veterans Affairs Medical Center, New Orleans, Louisiana.

Four new and specific pseudononapeptide bombesin/gastrin-releasing peptide (GRP) receptor antagonists, containing the D-forms of Trp or Trp analogue (Tpi) at position 6, were studied for their effects on the endocrine pancreas and GRP-(14-27)-induced gastrin release in pentobarbital-anesthetized rats. One of the analogues, D-Tpi6,Leu13-psi (CH2NH)Leu14-bombesin-(6-14) (RC-3095), was injected into the lateral brain ventricle just preceding intracerebroventricular administration of GRP-(14-27) to evaluate its antagonistic effect on GRP-induced serum growth hormone (GH) suppression. Analogues RC-3095, D-Trp6,Leu13-psi (CH2NH)Leu14-bombesin-(6-14) (RC-3125), and D-Trp6,Leu13-psi (CH2NH)Phe14-bombesin-(6-14) (RC-3420), but not D-Tpi6,Leu13-psi (CH2NH)Phe14-bombesin-(6-14) (RC-3105), significantly (P < 0.01) inhibited GRP-(14-27)-stimulated serum gastrin secretion. Analogues RC-3095, RC-3420, and RC-3105, but not RC-3125, demonstrated significant (P < 0.05) antagonistic activities on GRP-(14-27)-stimulated plasma glucagon secretion. Intracerebroventricular injection of RC-3095 (10 micrograms) immediately before GRP-(14-27) (1 microgram) completely prevented the GRP-(14-27)-induced serum GH suppression. These results indicate that 1) marked differences exist in the ability of these analogues to antagonize GRP-(14-27)-induced gastrin or glucagon release, suggesting the existence of different bombesin/GRP receptor subtypes, and 2) the central effect of bombesin/GRP on GH release from the pituitary is probably mediated through specific bombesin/GRP receptors.


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 Proc. Natl. Acad. Sci. USAHome page
K. Szepeshazi, A. V. Schally, G. Halmos, N. Lamharzi, K. Groot, and J. E. Horvath
A single in vivo administration of bombesin antagonist RC-3095 reduces the levels and mRNA expression of epidermal growth factor receptors in MXT mouse mammary cancers
PNAS, September 30, 1997; 94(20): 10913 - 10918.
[Abstract] [Full Text] [PDF]


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