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Titolo:
PHARMACOLOGICAL EVALUATION OF [C-11] A-84543 - AN ENANTIOSELECTIVE LIGAND FOR IN-VIVO STUDIES OF NEURONAL NICOTINIC ACETYLCHOLINE-RECEPTORS
Autore:
KASSIOU M; SCHEFFEL UA; RAVERT HT; MATHEWS WB; MUSACHIO JL; LONDON ED; DANNALS RF;
Indirizzi:
ROYAL PRINCE ALFRED HOSP,DEPT PET & NUCL MED,MISSENDEN RD CAMPERDOWN NSW 2050 AUSTRALIA NATL INST DRUG ABUSE,BRAIN IMAGING SECT,DIV INTRAMURAL RES BALTIMORE MD 21224 JOHNS HOPKINS MED INST,DIV NUCL MED BALTIMORE MD 21205 JOHNS HOPKINS MED INST,DIV RADIAT HLTH SCI BALTIMORE MD 21205
Titolo Testata:
Life sciences
fascicolo: 1, volume: 63, anno: 1998,
pagine: 13 - 18
SICI:
0024-3205(1998)63:1<13:PEO[A->2.0.ZU;2-8
Fonte:
ISI
Lingua:
ENG
Soggetto:
IN-VIVO; BINDING-SITES; HUMAN BRAIN; EPIBATIDINE; DIVERSITY; DEMENTIA; AGONIST;
Keywords:
[C-11] A-84543; NACHR RADIOTRACER; BRAIN; ENANTIOMER;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
17
Recensione:
Indirizzi per estratti:
Citazione:
M. Kassiou et al., "PHARMACOLOGICAL EVALUATION OF [C-11] A-84543 - AN ENANTIOSELECTIVE LIGAND FOR IN-VIVO STUDIES OF NEURONAL NICOTINIC ACETYLCHOLINE-RECEPTORS", Life sciences, 63(1), 1998, pp. 13-18

Abstract

[C-11]A-84543, (1-[C-11]methyl-2(S)-pyrrolidinyl)methoxy]pyridine is a specific and enantioselective neuronal nicotinic acetylcholine receptor (nAChR) radiotracer. The in vivo biodistribution of this radiotracer in mice showed high brain uptake and a distribution consistent withthe density of nAChRs. Highest uptake was observed in the thalamus (9.6 %ID/g), cortex (9.9 %ID/g), superior colliculus (7.6 %ID/g) and hippocampus (7.6 %ID/g) at 5 min followed by clearance. As a measure of specificity, the thalamus/cerebellar ratio reached a maximum of 2.3 at 30 min post-injection. Radioactivity in the thalamus and superior colliculus was reduced by 33% by pre-administration of unlabeled A-84543. The nAChR agonists (-)nicotine, cytisine, and (+) epibatidine reduced the radioactivity due to [C-11]A-84543 in the superior colliculus by 41%, 38%, and 27%, respectively, while lobeline, which also interacts with central nAChRs, produced a 24% inhibition. The noncompetitive nAChR ligand, mecamylamine displayed no inhibitory effect on [C-11]A-84543accumulation in any brain region. Ketanserin (5-HT2/5-HT2C), scopolamine (mAChR antagonist), (+)butaclamol (DA receptor antagonist), and haloperidol (D-2/sigma) also displayed no inhibitory effect in any brainregion studied. With the pharmacologically less active enantiomer, 3-[(1-[C-11]methyl-2(R)-pyrrolidinyl)methoxy] pyridine, high brain uptake was also observed, but with a low thalamus/cerebellar ratio of 1.4 at 30 min post-injection. [C-11]A-84543 displays enantioselectivity fornAChRs and may deserve further investigation asa possible PET radiotracer. (C) 1998 Elsevier Science Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 29/09/20 alle ore 00:38:16