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Titolo:
AUTORADIOGRAPHIC EVIDENCE THAT 3-QUINUCLIDINYL-4-FLUOROBENZILATE (FQNB) DISPLAYS IN-VIVO SELECTIVITY FOR THE M2 SUBTYPE
Autore:
BOULAY SF; DOOD VK; RAYEQ MR; COHEN VI; ZEEBERG BR; REBA RC;
Indirizzi:
GEORGE WASHINGTON UNIV,MED CTR,SECT RADIOPHARMACEUT CHEM,WALTER G ROSS HALL,2300 EYE ST NW WASHINGTON DC 20037 UNIV CHICAGO,DEPT RADIOL,NUCL MED SECT CHICAGO IL 60637
Titolo Testata:
NeuroImage
fascicolo: 1, volume: 3, anno: 1996,
pagine: 35 - 39
SICI:
1053-8119(1996)3:1<35:AET3(>2.0.ZU;2-T
Fonte:
ISI
Lingua:
ENG
Soggetto:
MUSCARINIC ACETYLCHOLINE-RECEPTORS; ALZHEIMERS-DISEASE; RAT-BRAIN; POTENTIAL RADIOPHARMACEUTICALS; INVIVO; TOMOGRAPHY; BINDING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
28
Recensione:
Indirizzi per estratti:
Citazione:
S.F. Boulay et al., "AUTORADIOGRAPHIC EVIDENCE THAT 3-QUINUCLIDINYL-4-FLUOROBENZILATE (FQNB) DISPLAYS IN-VIVO SELECTIVITY FOR THE M2 SUBTYPE", NeuroImage, 3(1), 1996, pp. 35-39

Abstract

Alzheimer's disease (AD) involves selective loss of muscarinic m2, but not mi, subtype neuroreceptors in cortical and hippocampal regions of the human brain. Emission tomographic study of the loss of m2 receptors in AD is limited by the fact that there is currently no available ma-selective radioligand which can penetrate the blood-brain barrier. We now demonstrate the in vivo m2 selectivity of a fluorine derivativeof QNB (FQNB), by studying autoradiographically the in vivo inhibition of radioiodinated (R)-3-quinuclidinyl (S)-4-iodobenzilate ((R,S)-[I-125]IQNB) binding by unlabeled FQNB. In the absence of FQNB, (R,S)-[I-125]IQNB labels brain regions in proportion to the total muscarinic receptor concentration; in the presence of 30.0 nmol of racemic FQNB, (R,S)-[I-125]IQNB labeling in those brain regions containing predominantly the m2 subtype is reduced to background levels. We conclude that FQNB is ma-selective in vivo and that [F-18]FQNB or a closely related analogue may be of potential use in positron emission tomographic study of the loss of m2 receptors in AD. (C) 1996 Academic Press, Inc.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/11/20 alle ore 21:34:00