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Kelatorphan

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Title: Kelatorphan  
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Subject: Amino acids, Kobret, 6β-Naltrexol-d4, Hemorphin, Naloxonazine
Collection: Amines, Amino Acids, Analgesics, Enkephalinase Inhibitors, Opioids
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Kelatorphan

Kelatorphan
Systematic (IUPAC) name
N-[(2R)-2-benzyl-4-(hydroxyamino)-4-oxobutanoyl]-L-alanine
Clinical data
Legal status
  • Non-regulated
Identifiers
CAS number
ATC code None
PubChem
DrugBank
ChemSpider
Chemical data
Formula C14H18N2O5 
Mol. mass 294.303 g/mol

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).[1][2][3] 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)[4] hence alongside exogenous [Met]enkephalin (ED50 approximately 10 ng), it potentiated the analgesic effects of the latter by 50,000 times.[1] Kelatorphan also displays potent antinociceptive effects alone,[5] and does not depress respiration, although at high doses it actually increases it.[4]

See also

References

  1. ^ a b Fournie-Zaluski MC, Chaillet P, Bouboutou R, et al. (July 1984). "Analgesic effects of kelatorphan, a new highly potent inhibitor of multiple enkephalin degrading enzymes". European Journal of Pharmacology 102 (3-4): 525–8.  
  2. ^ Yamamoto Y, Ono H, Ueda A, Shimamura M, Nishimura K, Hazato T (December 2002). "Spinorphin as an endogenous inhibitor of enkephalin-degrading enzymes: roles in pain and inflammation". Current Protein & Peptide Science 3 (6): 587–99.  
  3. ^ P. A. van Zwieten; William J. Greenlee (5 September 1997). Antihypertensive Drugs. CRC Press. p. 192.  
  4. ^ a b Boudinot E, Morin-Surun M, Foutz AS, Fournié-Zaluski M, Roques BP, Denavit-Saubié M (February 2001). "Effects of the potent analgesic enkephalin-catabolizing enzyme inhibitors RB101 and kelatorphan on respiration". Pain 90 (1-2): 7–13.  
  5. ^ Kayser V, Fournie-Zaluski MC, Guilbaud G, Roques BP (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 497 (1): 94–101.  


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