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Titolo:
Discrepancies in apparent dopamine D2 receptor occupancy between H-3-raclopride and H-3-N-methylspiperone
Autore:
Inoue, O; Kobayashi, K; Hosoi, R; Yamaguchi, M; Gee, A;
Indirizzi:
Osaka Univ, Fac Med, Sch Allied Hlth Sci, Dept Phys Med, Osaka 5650871, Japan Osaka Univ Osaka Japan 5650871 Sci, Dept Phys Med, Osaka 5650871, Japan Aarhus Kommune Hosp, PET Ctr, DK-8000 Aarhus, Denmark Aarhus Kommune HospAarhus Denmark DK-8000 Ctr, DK-8000 Aarhus, Denmark Fukuoka Univ, Fac Pharmaceut Sci, Fukuoka 81401, Japan Fukuoka Univ Fukuoka Japan 81401 ac Pharmaceut Sci, Fukuoka 81401, Japan
Titolo Testata:
JOURNAL OF NEURAL TRANSMISSION
fascicolo: 11-12, volume: 106, anno: 1999,
pagine: 1099 - 1104
SICI:
0300-9564(1999)106:11-12<1099:DIADDR>2.0.ZU;2-Q
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSITRON EMISSION TOMOGRAPHY; HUMAN-BRAIN; H-3 RACLOPRIDE; BINDING; PET;
Keywords:
dopamine D2 receptor; occupancy; raclopride; N-methylspiperone;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
14
Recensione:
Indirizzi per estratti:
Indirizzo: Inoue, O Osaka Univ, Fac Med, Sch Allied Hlth Sci, Dept Phys Med, 1-7 Yamada Oka, Osaka 5650871, Japan Osaka Univ 1-7 Yamada Oka Osaka Japan 5650871aka 5650871, Japan
Citazione:
O. Inoue et al., "Discrepancies in apparent dopamine D2 receptor occupancy between H-3-raclopride and H-3-N-methylspiperone", J NEURAL TR, 106(11-12), 1999, pp. 1099-1104

Abstract

Competitive inhibition of H-3-raclopride (RAC) and H-3-N-methylspiperone (NMSP) binding against haloperidol, raclopride and NMSP was measured in the mouse striatum. H-3-RAC binding was more sensitive to competitive inhibition by all three compounds compared with H-3-NMSP. For example, 0.3 mg/kg of haloperidol resulted in 95% inhibition of H-3-RAC binding, however only 60%of inhibition of H-3-NMSP binding was found at the same dose of haloperidol. The cross-inhibition experiments using nonradioactive RAC or NMSP as competitors indicated different binding sites for H-3-RAC and H-3-NMSP in mouse striatum. Specifically, about 40% of H-3-NMSP binding was not displaced by treatment with a very high dose of raclopride (3 mg/kg). The time course of inhibition of the specific binding of H-3-RAC and H-3-NMSP were measuredfollowing i.p. injection of 0.5 mg/kg of haloperidol. No significant differences in the kinetics of haloperidol inhibition were observed between two radioligands.

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Documento generato il 17/01/20 alle ore 20:38:51