Receptor binding potencies of chlorpromazine, trifluoperazine, fluphenazine and their 10-N-substituted analogues.
Receptor interactions of three pairs of phenothiazine derivatives, namely chlorpromazine, trifluoperazine, fluphenazine and their dialkylaminoacyl analogues were investigated. The data indicate that neuroleptic derivatives are less effective at dopamine (D2), alpha 1-adrenoceptors (AR) and histamine receptors (H1). No differences in affinity to alpha 2-AR were observed. The chlorpromazine analogue was more effective at muscarinic receptors of both types.
Savelyeva
M V
MV
Department of Cardiovascular Pharmacology, USSR Academy of Medical Sciences, Moscow.
Baldenkov
G N
GN
Kaverina
N V
NV
D000818:Animals; D001667:Binding, Competitive; D002417:Cattle; D002462:Cell Membrane / Q000378:metabolism; D002746:Chlorpromazine / Q000031:analogs & derivatives / Q000494:pharmacology*; D003342:Corpus Striatum / Q000378:metabolism*; D005476:Fluphenazine / Q000031:analogs & derivatives / Q000378:metabolism*; D007700:Kinetics; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014268:Trifluoperazine / Q000031:analogs & derivatives / Q000494:pharmacology*
D011956:Receptors, Cell Surface; D014268:Trifluoperazine; D005476:Fluphenazine; D002746:Chlorpromazine