Enterostatin (APGPR) suppresses the analgesic activity of morphine by a CCK-dependent mechanism.

Peptides

Division of Food Science and Biotechnology, Graduate School of Agriculture, Kyoto University, Uji, Kyoto 611-0011, Japan.

Published: April 2008

AI Article Synopsis

  • Enterostatin (APGPR) is a pentapeptide found in the gastrointestinal tract and brain that reduces appetite (anorectic).
  • In a study, APGPR was shown to block the pain-relieving effects of morphine in mice when administered directly into the brain at a specific dose.
  • The anti-analgesic (pain relief blocking) effect of APGPR appears to involve the release of cholecystokinin (CCK), as it is influenced by antagonists targeting CCK receptors, even though APGPR itself doesn't bind to these receptors.

Article Abstract

Enterostatin (APGPR) found in the gastrointestinal tract and brain is an anorectic pentapeptide. We found that APGPR inhibited morphine-induced analgesia after intracerebroventricular administration in mice at a dose of 10nmol/mouse. The anti-analgesic effect of APGPR was inhibited by pretreatment with lorglumide and LY225910, antagonists for cholecystokinin 1 (CCK1) and cholecystokinin 2 (CCK2) receptors, respectively. The anti-analgesic effect of APGPR may be mediated by CCK release, since APGPR does not have affinity for CCK receptors.

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http://dx.doi.org/10.1016/j.peptides.2007.12.017DOI Listing

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