Ethylketazocine
From Wikipedia, the free encyclopedia
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Systematic (IUPAC) name | |
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(1S,9R)-10-(cyclopropylmethyl)-1-ethyl-4-hydroxy-13-methyl-10-azatricyclo[7.3.1.02,7]trideca-2,4,6-trien-8-one
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Identifiers | |
CAS Number | 36292-66-7 |
ATC code | None |
PubChem | CID 644273 |
ChemSpider | 559289 |
Chemical data | |
Formula | C19H25NO2 |
Molar mass | 299.407 |
3D model (Jmol) | Interactive image |
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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]
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References[edit]
- ^ a b William O. Foye; Thomas L. Lemke (24 September 2007). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. p. 657. ISBN 978-0-7817-6879-5. Retrieved 22 April 2012.
- ^ Edythe D. London (1993). Imaging Drug Action in the Brain. CRC Press. p. 130. ISBN 978-0-8493-8843-9. Retrieved 22 April 2012.
- ^ 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. ISBN 978-1-4020-5946-9. Retrieved 22 April 2012.