[Differences in the efficiency of their interaction with membrane receptors of the dialkylaminoalkyl and dialkylaminoacyl derivatives of phenothiazine].
New dialkylaminoacyl phenothiazine derivatives (DAC) were compared with their dialkylaminoalkyl analogues (neuroleptics chlorpromazine, trifluoperazine and fluphenazine) as well as with anti-arrhythmia drugs ethmozine and ethacizine for their receptor-blocking potencies. It was established that DAC are significantly less potent with dopamine alpha 1-adrenergic and H1-histamine receptors of calf and rabbit brain, which can explain the absence of neuroleptic effect of DAC drugs. DAC affinities to muscarinic and alpha-adrenergic receptors of both types are very similar to those of ethmozine and ethacizine. New DAC substance G-512 (chlorpromazine analogue) demonstrated high affinity to M1-muscarinic receptors of rabbit brain cortex (Ki = 4.2 nM) and to M2-muscarinic receptors of the rabbit heart (Ki = 48 nM).
Savel'eva
M V
MV
Ratner
E I
EI
Baldenko
G N
GN
Kaverina
N V
NV
D000818:Animals; D000889:Anti-Arrhythmia Agents; D014150:Antipsychotic Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D002417:Cattle; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D003342:Corpus Striatum / Q000187:drug effects / Q000378:metabolism; D004347:Drug Interactions; D008297:Male; D010640:Phenothiazines / Q000493:pharmacokinetics / Q000494:pharmacology*; D011817:Rabbits; D011955:Receptors, Drug / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014316:Tritium
D000889:Anti-Arrhythmia Agents; D014150:Antipsychotic Agents; D010640:Phenothiazines; D011955:Receptors, Drug; D014316:Tritium
Razlichiia v éffektivnosti vzaimodeĭstviia s membrannymi retseptorami dialkilaminoalkil'nykh i dialkilaminoatsil'nykh proizvodnykh fenotiazina.