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CI-988

Chemical compound

Chemical compound

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CI-988 (PD-134,308) is a drug which acts as a cholecystokinin antagonist, selective for the CCKB subtype. In animal studies it showed anxiolytic effects and potentiated the analgesic action of both morphine and endogenous opioid peptides, as well as preventing the development of tolerance to opioids and reducing symptoms of withdrawal. Consequently, it was hoped that it might have clinical applications for the treatment of pain and anxiety in humans, but trial results were disappointing with only minimal therapeutic effects observed even at high doses. The reason for the failure of CI-988 and other CCKB antagonists in humans despite their apparent promise in pre-clinical animal studies is unclear, although poor pharmacokinetic properties of the currently available drugs are a possible explanation, and CCKB antagonists are still being researched for possible uses as adjuvants to boost the activity of other drugs.

References

References

  1. (September 1990). "Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity". Proceedings of the National Academy of Sciences of the United States of America.
  2. (September 1991). "The behavioural properties of CI-988, a selective cholecystokininB receptor antagonist". British Journal of Pharmacology.
  3. (September 1990). "PD134308, a selective antagonist of cholecystokinin type B receptor, enhances the analgesic effect of morphine and synergistically interacts with intrathecal galanin to depress spinal nociceptive reflexes". Proceedings of the National Academy of Sciences of the United States of America.
  4. (March 1994). "CCK-B antagonists exhibit antidepressant-like effects and potentiate endogenous enkephalin analgesia. Correlation with in vivo binding affinities and brain penetration". Annals of the New York Academy of Sciences.
  5. (July 1994). "Cholecystokinin B antagonists strongly potentiate antinociception mediated by endogenous enkephalins". The Journal of Pharmacology and Experimental Therapeutics.
  6. (March 1992). "CI988, a selective antagonist of cholecystokininB receptors, prevents morphine tolerance in the rat". British Journal of Pharmacology.
  7. (December 1994). "The CCK-B receptor antagonist Cl 988 reverses tolerance to morphine in rats". NeuroReport.
  8. (March 1995). "Inhibition of morphine withdrawal by the association of RB 101, an inhibitor of enkephalin catabolism, and the CCKB antagonist PD-134,308". British Journal of Pharmacology.
  9. (March 1998). "Cholecystokinin modulates the aversive component of morphine withdrawal syndrome in rats". Neuroscience Letters.
  10. (December 1995). "Effect of CI-988 on cholecystokinin tetrapeptide-induced panic symptoms in healthy volunteers". Biological Psychiatry.
  11. (December 1995). "A double-blind, placebo-controlled study of a CCK-B receptor antagonist, CI-988, in patients with generalized anxiety disorder". Journal of Clinical Psychopharmacology.
  12. (February 1997). "The cholecystokinin-B receptor antagonist CI-988 failed to affect CCK-4 induced symptoms in panic disorder patients". Psychopharmacology.
  13. (March 1999). "Effects of the CCK(B) antagonist CI-988 on responses to mCPP in generalized anxiety disorder". Psychiatry Research.
  14. (September 1999). "Placebo-controlled trial of the CCK-B antagonist, CI-988, in panic disorder". Biological Psychiatry.
  15. (July 2003). "Pain management by a new series of dual inhibitors of enkephalin degrading enzymes: long lasting antinociceptive properties and potentiation by CCK2 antagonist or methadone". Pain.
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