Phenyl-substituted normethadones: synthesis and pharmacology.
Phenyl-substituted normethadone derivatives were synthesized and their affinity (IC50) for opioid receptors was determined by displacement of the specific binding sites of [3H]sufentanyl on rat brain preparations. Substitution resulted in a decrease of affinity in-vitro. These results suggest that normethadone-like compounds may interact with the P subsite of the mu-opioid receptor and that the P subsite has a well-defined cavity shape of stringent dimensions.
Mbela
T K
TK
Department of Pharmaceutics and Drug Analysis, Faculty of Pharmacy, University of Kinshasa, Zaire.
Poupaert
J H
JH
Cumps
J
J
Moussebois
C
C
Haemers
A
A
Borloo
M
M
Dumont
P
P
D000700:Analgesics / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D005260:Female; D066298:In Vitro Techniques; D013058:Mass Spectrometry; D008691:Methadone / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D051379:Mice; D010636:Phenols / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D011957:Receptors, Opioid / Q000187:drug effects / Q000378:metabolism*; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship
D000700:Analgesics; D010636:Phenols; D011957:Receptors, Opioid; C008191:isomethadone; C005845:normethadone; D008691:Methadone