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Titolo:
[C-11]-methyl 4-[(3,4-dichiorophenyl)acetyl]-3-[(1-pyrrolidinyl) methyl]-1-piperazinecarboxylate ([C-11]GR89696): Synthesis and in vivo binding to kappa opiate receptors
Autore:
Ravert, HT; Mathews, WB; Musachio, JL; Scheffel, U; Finley, P; Dannals, RF;
Indirizzi:
Johns Hopkins Med Inst, Dept Radiol, Div Nucl Med, Baltimore, MD 21287 USAJohns Hopkins Med Inst Baltimore MD USA 21287 ed, Baltimore, MD 21287 USA
Titolo Testata:
NUCLEAR MEDICINE AND BIOLOGY
fascicolo: 7, volume: 26, anno: 1999,
pagine: 737 - 741
SICI:
0969-8051(199910)26:7<737:[4M>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
OPIOID RECEPTORS; IN-VIVO; AGONIST; POTENT; BRAIN; DOPAMINE; RAT; AUTORADIOGRAPHY; LOCALIZATION; RADIOTRACER;
Keywords:
C-11; kappa opioid receptors; PET;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
26
Recensione:
Indirizzi per estratti:
Indirizzo: Ravert, HT Johns Hopkins Med Inst, Dept Radiol, Div Nucl Med, Nelson Bldg Room B1-167,600 N Wolfe St, Baltimore, MD 21287 USA Johns Hopkins Med Inst Nelson Bldg Room B1-167,600 N Wolfe St Baltimore MD USA 21287
Citazione:
H.T. Ravert et al., "[C-11]-methyl 4-[(3,4-dichiorophenyl)acetyl]-3-[(1-pyrrolidinyl) methyl]-1-piperazinecarboxylate ([C-11]GR89696): Synthesis and in vivo binding to kappa opiate receptors", NUCL MED BI, 26(7), 1999, pp. 737-741

Abstract

GR89696, racemic methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazinecarboxylate, a kappa opioid receptor ligand, was labeled with [C-11]methyl chloroformate. The radiochemical yield was 20% with anobserved specific radioactivity of 15.5 GBq/mu mol at end of synthesis (2,040 mCi/mu mol). Five minutes after intravenous administration, 5.4% of theinjected dose accumulated in mouse whole brain. Brain region to cerebellarratios increased over time with ratios at 90 min of 7.8, 5.6, and 4.5 for the hypothalamus, olfactory tubercle, and striatum, respectively. The uptake of [C-11]GR89696 correlated with known kappa opioid receptor densities and was inhibited by kappa opioid selective drugs. NUCL MED BIOL 26;7:737-741, 1999. (C) 1999 Elsevier Science Inc. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 22/10/20 alle ore 02:55:16