ISSN:
1435-1463
Keywords:
Phenylpiperazine
;
monoamine uptake
;
NA
;
DA
;
5-HT
;
MAO
;
phenylethylamine
;
rat
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Summary The diastereomers of 3,N,N′-trimethyl-2-phenyl-1,4-piperazine dihydrochloride (TPP) were tested for their effects on NA, DA and 5-HT uptake in synaptosomes prepared from hypothalamus, corpus striatum, and frontal cortex, respectively. The diastereomers differed with respect to their inhibitory properties. (2R, 3R)-TPP was more potent than the other diastereomers on NA and DA uptake, whereas (2S, 3S)-TPP was least potent. In contrast, the (2S, 3S)- and (2 S, 3R)-diastereomers of TPP were more potent than (2R, 3R)- and (2R, 3S)-TPP as inhibitors of 5-HT uptake. None of the diastereomers affected monoamine oxidase activity. The findings show that the diastereomers of TPP interact stereoselectively with neuronal mechanisms for monoamine uptake, and that the (S)-configuration at the 2 carbon is important for inhibitory actions of TPP on 5-HT uptake.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01244731
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