title: [Differences in the efficiency of their interaction with membrane receptors of the dialkylaminoalkyl and dialkylaminoacyl derivatives of phenothiazine].
abstract: 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).
authors.forename: M V
authors.initials: MV
authors.lastname: Savel'eva
authors.forename: E I
authors.initials: EI
authors.lastname: Ratner
authors.forename: G N
authors.initials: GN
authors.lastname: Baldenko
authors.forename: N V
authors.initials: NV
authors.lastname: Kaverina
mesh_terms: 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
chemical_list: D000889:Anti-Arrhythmia Agents; D014150:Antipsychotic Agents; D010640:Phenothiazines; D011955:Receptors, Drug; D014316:Tritium
vernacular_title: Razlichiia v éffektivnosti vzaimodeĭstviia s membrannymi retseptorami dialkilaminoalkil'nykh i dialkilaminoatsil'nykh proizvodnykh fenotiazina.