Clinical perspectives of cholecystokinin antagonists in pain management

  • M. Amanzio
  • F. Benedetti
Part of the Topics in Anaesthesia and Critical Care book series (TIACC)


Cholecystokinin (CCK) is a peptide widely distributed in the central nervous system. Since its characterization in the porcine intestine, evidence has accumulated that it plays an essential role in several brain functions such as nociception, anxiety, memory, sleep and dopamine modulation. In mammalian brain, CCK is mainly found as an octapeptide (CCK-8) and tetrapeptide (CCK-4) and its effects are mediated by two types of receptors: CCK-A and CCK-B [1, 2]. CCK-8 acts at both receptors whereas CCK-4 shows its main activity at the CCK-B receptors. The distribution of the type-A and type-B receptors shows species differences and this fact has important clinical implications [3]. For example, CCKB binding sites are predominant in the spinal cord of rodents whereas CCK-A receptors prevail in the spinal cord of primates and humans. Therefore, the original nomenclature of peripheral alimentary (type A) and brain (type B) receptors no longer holds. It should be pointed out that, whereas the gene cckA encodes for the CCK-A receptor, the gene cckB encodes for both the CCK-B and gastrin receptor, thus indicating that the type-B binding site is better defined as CCK-B-gastrin receptor.


Endogenous Opioid Morphine Analgesia Placebo analgeSia Gastrin Receptor Dopamine Modulation 
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© Springer Verlag Italia, Milano 1999

Authors and Affiliations

  • M. Amanzio
  • F. Benedetti

There are no affiliations available

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