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Titolo:
[H-3] QNB DISPLAYS IN-VIVO SELECTIVITY FOR THE M2 SUBTYPE
Autore:
GITLER MS; DELACRUZ R; ZEEBERG BR; REBA RC;
Indirizzi:
GEORGE WASHINGTON UNIV,MED CTR,DEPT RADIOL,RADIOPHARMACEUT CHEM SECT,ROOM 662 ROSS HALL WASHINGTON DC 20037 GEORGE WASHINGTON UNIV,MED CTR,DEPT RADIOL,RADIOPHARMACEUT CHEM SECT WASHINGTON DC 20037 UNIV CHICAGO HOSP & CLIN,DEPT RADIOL,NUCL MED SECT CHICAGO IL 60637
Titolo Testata:
Life sciences
fascicolo: 19, volume: 55, anno: 1994,
pagine: 1493 - 1508
SICI:
0024-3205(1994)55:19<1493:[QDISF>2.0.ZU;2-E
Fonte:
ISI
Lingua:
ENG
Soggetto:
MUSCARINIC RECEPTOR SUBTYPES; AF-DX 116; RAT-BRAIN; 3-QUINUCLIDINYL 4-IODOBENZILATE; AUTORADIOGRAPHIC DISTRIBUTION; ACETYLCHOLINE-RECEPTORS; DISSOCIATION KINETICS; ALZHEIMERS-DISEASE; BINDING; INVIVO;
Keywords:
EMISSION TOMOGRAPHIC NEURORECEPTOR; M2 MUSCARINIC NEURORECEPTOR SUBTYPE; [H-3] QNB;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
49
Recensione:
Indirizzi per estratti:
Citazione:
M.S. Gitler et al., "[H-3] QNB DISPLAYS IN-VIVO SELECTIVITY FOR THE M2 SUBTYPE", Life sciences, 55(19), 1994, pp. 1493-1508

Abstract

Alzheimer's disease (AD) involves selective loss of muscarinic m2, but not m1, subtype neuroreceptors in the posterior parietal cortex of the human brain. Emission tomographic study of the loss of m2 receptorsin AD is limited by the fact that there is currently no available m2-selective radioligand which can penetrate the blood-brain barrier. [H-3](R)-3-quinuclidinylbenzilate ([H-3]QNB) is commonly used for performing in vitro studies of the muscarinic acetylcholine receptor (mAChR),either with membrane homogenates or with autoradiographic slices, in which [H-3]QNB is nonsubtype-selective. We report here the results of in vivo studies, using both carrier-free and low specific activity [H-3]QNB, which show that [H-3]QNB exhibits a substantial in vivo m2-selectivity. Previously reported in vivo (R)-3-quinuclidinyl (R)-4-iodobenzilate ((R,R)-[I-125]IQNB) binding appears to be nonsubtype-selective. Apparently the bulky iodine substitution in the 4 position reduces the subtype selectivity of QNB. it is possible that a less bulky fluorine substitution might permit retention of the selectivity exhibited by QNB itself. We conclude that a suitably radiolabeled derivative of QNB, possibly labeled with F-18, may be of potential use in positron emission tomographic (PET) study of the loss of m2 receptors in AD.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/11/20 alle ore 21:35:49