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Kelatorphan

Chemical compound

Chemical compound

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Kelatorphan is a drug which acts as a powerful and complete inhibitor of nearly all of the enzymes responsible for catabolism of the endogenous enkephalins, including neutral endopeptidase (NEP), dipeptidyl peptidase III (DPP3), aminopeptidase N (APN), and angiotensin-converting enzyme (ACE). In mice, with the intracerebroventricular co-administration of a 50 μg dose of kelatorphan (this route is necessary because kelatorphan is incapable of crossing the blood-brain-barrier) hence alongside exogenous [Met]enkephalin (ED50 approximately 10 ng), it potentiated the analgesic effects of the latter by 50,000 times. Kelatorphan also displays potent antinociceptive effects alone, and does not depress respiration, although at high doses it actually increases it.

References

References

  1. (July 1984). "Analgesic effects of kelatorphan, a new highly potent inhibitor of multiple enkephalin degrading enzymes". European Journal of Pharmacology.
  2. (December 2002). "Spinorphin as an endogenous inhibitor of enkephalin-degrading enzymes: roles in pain and inflammation". Current Protein & Peptide Science.
  3. (5 September 1997). "Antihypertensive Drugs". CRC Press.
  4. (February 2001). "Effects of the potent analgesic enkephalin-catabolizing enzyme inhibitors RB101 and kelatorphan on respiration". Pain.
  5. (September 1989). "Potent antinociceptive effects of kelatorphan (a highly efficient inhibitor of multiple enkephalin-degrading enzymes) systemically administered in normal and arthritic rats". Brain Research.
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alpha-amino-acids enkephalinase-inhibitors opioids peripherally-selective-drugs
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