Casokefamide

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Casokefamide
Casokefamide.svg
Systematic (IUPAC) name
L-tyrosyl-D-alanyl-L-phenylalanyl-D-alanyl-L-tyrosinamide
Clinical data
Legal status ?
Identifiers
CAS number 98815-38-4
ATC code None
PubChem CID 5464104
ChemSpider 4576538
ChEMBL CHEMBL2106384
Chemical data
Formula C33H40N6O7 
Mol. mass 632.707 g/mol

Casokefamide (INN), also known as β-casomorphin 4027 (β-CM-4027) and [D-Ala2,4,Tyr5]-β-casomorphin-5-amide, is a peripherally-specific, synthetic opioid pentapeptide with the amino acid sequence Tyr-D-Ala-Phe-D-Ala-Tyr-NH2.[1] Derived from the β-casomorphin sequence, it was designed with the intention of improving resistance to digestive enzymes so that it could potentially be used as an antidiarrheal medicine.[1][2] Unlike other casomorphins, which are generally selective μ-opioid receptor agonists, casokefamide binds to both the μ- and δ-opioid receptors.[1] In a clinical study, casokefamide was found to be effective via the oral route for the treatment of chronic diarrhea, and did not produce any side effects.[2] However, further clinical development was not pursued and it was never marketed.

See also[edit]

References[edit]

  1. ^ a b c Brantl V, Picone D, Amodeo P, Temussi PA (March 1993). "Solution structure of casokefamide". Biochemical and Biophysical Research Communications 191 (3): 853–9. doi:10.1006/bbrc.1993.1295. PMID 8466524. 
  2. ^ a b Schulte-Frohlinde E, Reindl W, Bierling D, et al. (March 2000). "Effects of oral casokefamide on plasma levels, tolerance, and intestinal transit in man". Peptides 21 (3): 439–42. doi:10.1016/S0196-9781(00)00166-2. PMID 10793229.