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The antagonistic effect of cholecystokinin octapeptide (CCK-8) on opioid effects in cardiovascular activities was mediated by CCK-B receptor.

Abstract
Previous studies have shown that CCK-8 has distinct antiopioid effect in the central sites related with pain control and blood pressure control. The aim of this study was to explore the receptor mechanism by which CCK-8 antagonized the depressor effect of u- and k-opioid agonists, and to observe whether CCK-8 could antagonize the depressor effect induced by muscimol, a nonopioid substance. The results showed that (i) The antagonistic effect of CCK-8 on opioid-induced hypotension could be blocked by intrathecal (i. t.) administration of CCK-B antagonist L-365, 260 at nanogram doses, or by CCK-A antagonist devazepide at doses 20-40 times higher than L-365, 260, indicating that it was the CCK-B receptor which mediates the antiopioid effect. (ii) The depressor effect induced by intrathecal muscimol, a GABA agonist, was blocked neither by naloxone nor by CCK-8, supporting the notion that CCK-8 is an endogenous opioid antagonist rather than a universal anti-hypotension agent.
AuthorsL Mei, J S Han
JournalScience in China. Series B, Chemistry, life sciences & earth sciences (Sci China B) Vol. 36 Issue 7 Pg. 817-23 (Jul 1993) ISSN: 1001-652X [Print] China
PMID8216742 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Benzodiazepinones
  • Phenylurea Compounds
  • Receptors, Cholecystokinin
  • Muscimol
  • L 365260
  • Proglumide
  • Devazepide
  • Sincalide
Topics
  • Animals
  • Benzodiazepinones (pharmacology)
  • Blood Pressure (drug effects)
  • Devazepide
  • Female
  • Hypotension (chemically induced, drug therapy)
  • Muscimol
  • Phenylurea Compounds
  • Proglumide (pharmacology)
  • Rats
  • Rats, Wistar
  • Receptors, Cholecystokinin (antagonists & inhibitors, physiology)
  • Sincalide (pharmacology, therapeutic use)

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