3-Alkyl ethers of clocinnamox: Delayed long-term μ-antagonists with variable μ efficacy

Journal of Medicinal Chemistry

Volumn 41, Issue 18, 1998, Pages 3493-3498

  Husbands, Stephen M ^a   Sadd, John ^a   Broadbear, Jillian H ^b   Woods, James H ^b   Martin, Jason ^b   Traynor, John R ^b   Aceto, Mario D ^c   Bowman, Edward R ^c   Harris, Louis S ^c   Lewis, John W ^a  

^a UNIVERSITY OF BRISTOL   (United Kingdom)

^b UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

^c VIRGINIA COMMONWEALTH UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 [ALPHA (4 ALLYL 2,5 DIMETHYL 1 PIPERAZINYL) 3 HYDROXYBENZYL] N,N DIETHYLBENZAMIDE; BREMAZOCINE; CLOCINNAMOX; CLOCINNAMOX 3 CYCLOPROPYLMETHYL ETHER; CLOCINNAMOX 3 PROPARGYL ETHER; METHOCLOCINNAMOX; MORPHINE; MU OPIATE RECEPTOR; MU OPIATE RECEPTOR ANTAGONIST; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTINOCICEPTION; ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; MORPHINE ADDICTION; MOUSE; NONHUMAN; OPIATE ADDICTION; RECEPTOR AFFINITY; SUBCUTANEOUS DRUG ADMINISTRATION;

ANIMALS; BRAIN; CINNAMATES; MACACA MULATTA; MICE; MORPHINE; MORPHINE DERIVATIVES; NARCOTIC ANTAGONISTS; PAIN MEASUREMENT; RATS; RECEPTORS, OPIOID, MU; SUBSTANCE WITHDRAWAL SYNDROME;

EID: 15644375193     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm9810248     Document Type: Article

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26. 3d using 1% DMSO in the incubation volume (as against 0.1% in the present study) C-CAM bound with the following affinities: μ 0.25 nM, κ 7.2 nM, δ 1.6 nM. MC-CAM bound with affinities of μ 0.46 nM, κ 29 nM, δ 4.5 nM.