Ethylketazocine

Ethylketazocine

Ethylketazocine
Systematic (IUPAC) name
(1S,9R)-10-(cyclopropylmethyl)-1-ethyl-4-hydroxy-13-methyl-10-azatricyclo[7.3.1.02,7]trideca-2,4,6-trien-8-one
Clinical data
Legal status
?
Identifiers
CAS number
ATC code None
PubChem
ChemSpider
Chemical data
Formula C19H25NO2 
Mol. mass 299.407

Ethylketazocine (WIN-35,197-2), also known as ethylketocyclazocine (EKC), is an opioid drug of the benzomorphan family which has been used extensively in scientific research in the last few decades as a tool to aid in the study of the κ-opioid receptor.[1] However, due to its relatively poor selectivity for the κ-opioid receptor over the μ- and δ-opioid receptors (of which it has approximately 80% and 20% of the affinity for, respectively, in comparison), as well as its relatively poor intrinsic activity at all sites (i.e., acts as a partial agonist with mixed agonist and antagonist properties), it has been mostly replaced in recent times by newer and more potent and selective compounds like U-50,488 and ICI-199,441.[1][2][3]

See also

References

  1. ^ a b William O. Foye; Thomas L. Lemke (24 September 2007). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. p. 657.  
  2. ^ Edythe D. London (1993). Imaging Drug Action in the Brain. CRC Press. p. 130.  
  3. ^ Enno Freye (3 April 2008). Opioids in Medicine: A Comprehensive Review on the Mode of Action and the Use of Analgesics in Different Clinical Pain States. Springer. p. 103.