Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
P-[F-18]-MPPF - A POTENTIAL RADIOLIGAND FOR PET STUDIES OF 5-HT1A RECEPTORS IN HUMANS
Autore:
SHIUE CY; SHIUE GG; MOZLEY PD; KUNG MP; ZHUANG ZP; KIM HJ; KUNG HF;
Indirizzi:
UNIV PENN,DEPT RADIOL,MED CTR,3400 SPRUCE ST PHILADELPHIA PA 19104
Titolo Testata:
Synapse
fascicolo: 2, volume: 25, anno: 1997,
pagine: 147 - 154
SICI:
0887-4476(1997)25:2<147:P-APRF>2.0.ZU;2-W
Fonte:
ISI
Lingua:
ENG
Soggetto:
POSTSYNAPTIC 5-HT(1A) RECEPTORS; RAT-BRAIN; P-MPPI; SELECTIVE ANTAGONIST; H-3 WAY-100635; HIGH-AFFINITY; SEROTONIN; NAN-190; BINDING; BMY-7378;
Keywords:
5-HT1A RECEPTORS; P-[F-18]-MPPF; PET;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
60
Recensione:
Indirizzi per estratti:
Citazione:
C.Y. Shiue et al., "P-[F-18]-MPPF - A POTENTIAL RADIOLIGAND FOR PET STUDIES OF 5-HT1A RECEPTORS IN HUMANS", Synapse, 25(2), 1997, pp. 147-154

Abstract

The purpose of this study was to develop a radiopharmaceutical that could be used to selectively image 5-HT1A receptors with positron emission tomography (PET). No-carrier-added pyridinyl)-p-[F-18]fluorobenzamido]ethylpiperazine (p-[F-18]-MPPF, 2) was synthesized by the nucleophilic substitution of the corresponding nitro precursor 1 with K[F-18]/Kryptofix 2.2.2. in dimethyl sulfoxide (DMSO) at 140 degrees C for 20 min followed by purification with high-performance liquid chromatography (HPLC) in 10% yield in a synthesis time of 90 min from end of bombardment (EOB). Specific activity was 1-4 Ci/mu M. Biodistribution studies in rats showed that the initial uptake of 2 in the brain was high (0.7% dose/g tissue at 2 min). It was then rapidly eliminated. Rates ofelimination were significantly slower in brain regions with high concentrations of 5-HT1A receptors (hippocampus, cortex, and hypothalamus)than in control regions. The maximum hippocampal/cerebellar ratio was5.6:1 at 30 min postinjection. Uptake values in serotonergic, but notin control, regions were significantly reduced by prior treatment with either (+/-)-8-OH-DPAT (2 mg/kg, i.v., 5 min priori or WAY 100635 (1mg/kg, i.v., 5 min prior). Radioactivity in the femur did not increase with time, suggesting that in vivo defluorination may not be the major route of metabolism. PET studies of 2 in a monkey demonstrated selective uptake and retention of 2 in the hippocampus. The hippocampal/cerebellar ratio was 3:1 at 30 min postinjection. The ratio was reduced to I:1 by administering (+/-)-8-OH-DPAT (2 mg/kg, i.v.) 23 min postinjection of 2. Analyses of arterial plasma by HPLC revealed that 20% of radioactivity in the plasma remained as the parent compound 2 at 30 min postinjection. The results suggest that p-[F-18]-MPPF may be a useful radioligand for studying cerebral 5-HT1A receptors in humans with PET techniques. (C) 1997 Wiley-Liss, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/01/20 alle ore 19:23:19