N-Cyclohexylethyl-N-noroxymorphindole: a mu-opioid preferring analogue of naltrindole.
The position of the indole in the indolomorphinans, which includes the delta opioid antagonist naltrindole, is considered to be responsible for the delta opioid selectivity for this class of ligands. Herein is described the N-cyclohexylethyl substituted N-nor-derivative, which is shown to be mu preferring. Thus, the nature of the N-substituent is equally important to the receptor selectivity for this class of ligands.
Coop
A
A
Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore 21201, USA. acoop@rx.umaryland.edu
Jacobson
A E
AE
Aceto
M D
MD
Harris
L S
LS
Traynor
J R
JR
Woods
J H
JH
Rice
K C
KC
D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D051379:Mice; D015394:Molecular Structure; D009020:Morphine / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D009022:Morphine Derivatives; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D009292:Narcotic Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D010147:Pain Measurement; D017450:Receptors, Opioid, mu / Q000378:metabolism*
D000700:Analgesics; D009022:Morphine Derivatives; C421327:N-Cyclohexylethyl-N-noroxymorphindole; D009292:Narcotic Antagonists; D017450:Receptors, Opioid, mu; D009271:Naltrexone; D009020:Morphine; C055382:naltrindole