[The interaction of dialkylaminoacyl derivatives of phenothiazine, dibenzazepine and dibenzdiazepine with opiate receptors].
Specific binding of dialkylaminoacyl (DAC) derivatives of phenothiazine, dibenzazepine, dibenzdiazepine with opiate receptors (OR) of mu- and delta-subtypes was studied. Some of the compounds studied exhibit moderate affinity to mu-OR in microM range. Binding with delta-OR is less pronounced. Dibenzdiazepine derivative AL-234 is the most potent compound with respect to OR of both mu- and delta- subtypes (IC50 values were 11 and 60 microM, respectively). The ability of DAC- derivatives to bind specifically OR can play a decisive role in realization of their pharmacologic properties, namely antinociceptive and probably antiarrhythmic activity.
Brusova
E G
EG
Likhosherstov
A M
AM
Gritsenko
A N
AN
D000700:Analgesics / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D003984:Dibenzazepines / Q000493:pharmacokinetics / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D066298:In Vitro Techniques; D010640:Phenothiazines / Q000493:pharmacokinetics / Q000494:pharmacology*; D011619:Psychotropic Drugs / Q000493:pharmacokinetics / Q000494:pharmacology*; D011869:Radioligand Assay; D051381:Rats; D017465:Receptors, Opioid, delta / Q000187:drug effects* / Q000378:metabolism; D017450:Receptors, Opioid, mu / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship
D000700:Analgesics; D000889:Anti-Arrhythmia Agents; D003984:Dibenzazepines; D010640:Phenothiazines; D011619:Psychotropic Drugs; D017465:Receptors, Opioid, delta; D017450:Receptors, Opioid, mu
Vzaimodeĭstvie dialkilaminoatsil'nykh proizvodnykh fenotaizina, dibenzazepina, dibenzdiazepina s opiatnymi retseptorami.