Ethylketazocine
Chemical compound
- None
- (1S,9R)-10-(cyclopropylmethyl)-1-ethyl-4-hydroxy-13-methyl-10-azatricyclo[7.3.1.02,7]trideca-2,4,6-trien-8-one
- 36292-66-7
- 644273
- 1602
- 559289
- ChEMBLCHEMBL279968
- DTXSID40957665
- Interactive image
- O=C2c1c(cc(O)cc1)[C@@]3(C([C@H]2N(CC3)CC4CC4)C)CC
InChI
- InChI=1S/C19H25NO2/c1-3-19-8-9-20(11-13-4-5-13)17(12(19)2)18(22)15-7-6-14(21)10-16(15)19/h6-7,10,12-13,17,21H,3-5,8-9,11H2,1-2H3/t12?,17-,19+/m1/s1
- Key:SEJUQQOPVAUETF-MKFRLIFGSA-N
Ethylketazocine (WIN-35,197-2), 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
- ^ a b Foye WO, Lemke TL (24 September 2007). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. p. 657. ISBN 978-0-7817-6879-5. Retrieved 22 April 2012.
- ^ London ED (1993). Imaging Drug Action in the Brain. CRC Press. p. 130. ISBN 978-0-8493-8843-9. Retrieved 22 April 2012.
- ^ Freye E (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.
- v
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modulators
| Calcium blockers |
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| Sodium blockers |
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| Potassium openers |
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
