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Science 11 October 1985:
Vol. 230. no. 4722, pp. 177 - 179
DOI: 10.1126/science.2994227
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Articles

Science, Vol 230, Issue 4722, 177-179
Copyright © 1985 by American Association for the Advancement of Science

articles

A potent nonpeptide cholecystokinin antagonist selective for peripheral tissues isolated from Aspergillus alliaceus

RS Chang, VJ Lotti, RL Monaghan, J Birnbaum, EO Stapley, MA Goetz, G Albers-Schonberg, AA Patchett, JM Liesch, OD Hensens, and al. et

A new, competitive, nonpeptide cholecystokinin (CCK) antagonist, asperlicin, was isolated from the fungus Aspergillus alliaceus. The compound has 300 to 400 times the affinity for pancreatic, ileal, and gallbladder CCK receptors than proglumide, a standard agent of this class. Moreover, asperlicin is highly selective for peripheral CCK receptors relative to brain CCK and gastrin receptors. Since asperlicin also exhibits long-lasting CCK antagonist activity in vivo, it should provide a valuable tool for investigating the physiological and pharmacological actions of CCK.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
International Union of Pharmacology. XXI. Structure, Distribution, and Functions of Cholecystokinin Receptors.
F. Noble, S. A. Wank, J. N. Crawley, J. Bradwejn, K. B. Seroogy, M. Hamon, and B. P. Roques (1999)
Pharmacol. Rev. 51, 745-781
   Abstract »    Full Text »    PDF »
Intestinal fat-induced inhibition of meal-stimulated gastric acid secretion depends on CCK but not peptide YY.
X.-T. Zhao, J. H. Walsh, H. Wong, L. Wang, and H. C. Lin (1999)
Am J Physiol Gastrointest Liver Physiol 276, G550-G555
   Abstract »    Full Text »    PDF »
Identification and Characterization of Small Molecule Functional Antagonists of the CCR1 Chemokine Receptor.
J. Hesselgesser, H. P. Ng, M. Liang, W. Zheng, K. May, J. G. Bauman, S. Monahan, I. Islam, G. P. Wei, A. Ghannam, et al. (1998)
J. Biol. Chem. 273, 15687-15692
   Abstract »    Full Text »    PDF »
Effects of a Cholecystokinin Receptor Antagonist on Rat Exocrine Pancreatic Response to Raw Soya Flour.
S. Sundaram and A.D. Dayan (1991)
Human and Experimental Toxicology 10, 179-182
   Abstract »    PDF »
Cholecystokinin Augmentation of 'Surgical' Pancreatitis: Benefits of Receptor Blockade.
I. M. Modlin, A. J. Bilchik, K. A. Zucker, T. E. Adrian, J. Sussman, and S. M. Graham (1989)
Arch Surg 124, 574-578
   Abstract »    PDF »


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