http://www.cnr.it/ontology/cnr/individuo/prodotto/ID37174
In vitro evidence for the presence of [3H]-haloperidol uptake in rat brain. (Articolo in rivista)
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- In vitro evidence for the presence of [3H]-haloperidol uptake in rat brain. (Articolo in rivista) (literal)
- Anno
- 2003-01-01T00:00:00+01:00 (literal)
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Ruiu S., Marchese G., Saba PL., Gessa GL., Vaccari A., Pani L. (2003)
In vitro evidence for the presence of [3H]-haloperidol uptake in rat brain.
in British journal of pharmacology
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- Ruiu S., Marchese G., Saba PL., Gessa GL., Vaccari A., Pani L. (literal)
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- Titolo
- In vitro evidence for the presence of [3H]-haloperidol uptake in rat brain. (literal)
- Abstract
- 1 The neuroleptic [(3)H]-haloperidol (HP) was taken up in synaptosomes prepared from rat brain, in a temperature-, sodium ion-, and energy-dependent process. 2 The highest concentration of uptake sites (V(max)=2.37 pmol mg(-1) protein min(-1)) was in the striatum with the other brain areas displaying lower (by 50-70%) values. 3 The affinity values (K(m) approximately equal to 40 nM) were similar in all brain areas considered. 4 The pharmacological characterization did not indicate a well-defined group of inhibitors, which suggested that HP might not use a transporter for recognized neurotransmitters. 5 The HP metabolites tested, including HPTP, were competitive inhibitors of [(3)H]-HP uptake, an indirect indication that they may actively enter the striatal nerve endings through the same carrier. 6 Since the uptake process was partially affected by the incubation of [(3)H]-HP in the presence of several antagonists of HP-transforming cytochrome P450 isoforms, the binding of HP at some enzyme sites inside the synaptosome cannot be excluded. 7 In conclusion, the present results suggest that HP may be actively transported in the rat brain. (literal)
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