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Titolo:
IN-VIVO COMPETITION STUDIES OF Z-(-,-)-[I-125]IQNP AGAINST 3-QUINUCLIDINYL 2-(5-BROMOTHIENYL)-2-THIENYLGLYCOLATE (BRQNT) DEMONSTRATING IN-VIVO M2 MUSCARINIC SUBTYPE SELECTIVITY FOR BRQNT
Autore:
COHEN VI; ZEEBERG BR; BOULAY SF; SOOD VK; RAYEQ MR; DANESH RA; MCPHERSON DW; REBA RC;
Indirizzi:
GEORGE WASHINGTON UNIV,MED CTR,SECT RADIOPHARMACEUT CHEM,WALTER G ROSS HALL,2300 EYE ST NW WASHINGTON DC 20037 OAK RIDGE NATL LAB,NUCL MED GRP OAK RIDGE TN 37831 UNIV CHICAGO,DEPT RADIOL,NUCL MED SECT CHICAGO IL 60637
Titolo Testata:
Journal of molecular neuroscience
fascicolo: 1, volume: 11, anno: 1998,
pagine: 1 - 9
SICI:
0895-8696(1998)11:1<1:ICSOZA>2.0.ZU;2-1
Fonte:
ISI
Lingua:
ENG
Soggetto:
IODINE-125-LABELED 1-AZABICYCLO)2.2.2>OCT-3-YL ALPHA-HYDROXY-ALPHA-(1-IODO-1-PRO; EMISSION COMPUTED-TOMOGRAPHY; AUTORADIOGRAPHIC EVIDENCE; ALZHEIMERS-DISEASE; RAT-BRAIN; CHOLINERGIC RECEPTORS; ACETYLCHOLINE-RECEPTORS; ISOMERS; INVIVO; BINDING;
Keywords:
ALZHEIMERS DISEASE; MUSCARINIC SUBTYPE NEURORECEPTORS; PET; SPECT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
33
Recensione:
Indirizzi per estratti:
Citazione:
V.I. Cohen et al., "IN-VIVO COMPETITION STUDIES OF Z-(-,-)-[I-125]IQNP AGAINST 3-QUINUCLIDINYL 2-(5-BROMOTHIENYL)-2-THIENYLGLYCOLATE (BRQNT) DEMONSTRATING IN-VIVO M2 MUSCARINIC SUBTYPE SELECTIVITY FOR BRQNT", Journal of molecular neuroscience, 11(1), 1998, pp. 1-9

Abstract

Alzheimer's disease (AD) involves selective loss of muscarinic m2, but not m1, subtype neuroreceptors in cortical and hippocampal regions of the human brain. Until recently, emission tomographic study of the loss of m2 receptors in AD has been limited by the absence of availablem2-selective radioligands that can penetrate the blood-brain barrier. We now demonstrate the in vivo m2 selectivity of an analog of (R)-QNB, 3-quinuclidinyl 2-(5-bromothienyl)-2-thienylglycolate (BrQNT), by dissection and autoradiographic studies of the in vivo inhibition of radioiodinated Z-1-azabicyclo [2.2.2]oct-3-yl hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenyl- acetate (Z-(-,-)-[I-125]IQNP) binding by unlabeled BrQNT in rat brain. In the absence of BrQNT, Z-(-,-)[I-125]IQNP labels brain regions containing muscarinic receptors, with an enhanced selectivity for the m2 subtype. In the presence of 60-180 nmol of co-injected racemic BrQNT, Z-(-,-)-[I-125]IQNP labeling in those brain regions containing predominantly m2 subtype is reduced to background levels, while levels of radioactivity in areas not enriched in the m2 subtype do not significantly decrease. We conclude that BrQNT is m2-selective in vivo, and that [Br-76]BrQNT, or a radiofluorinated analog, may be of potential use in positron emission tomographic (PET) study of the loss of m2 receptors in AD. In addition, a radioiodinated analog maybe of potential use in single photon emission tomographic (SPECT) studies.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/11/20 alle ore 20:02:15