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Titolo:
CHARACTERIZATION OF IN-VIVO BRAIN MUSCARINIC ACETYLCHOLINE-RECEPTOR SUBTYPE SELECTIVITY BY COMPETITION STUDIES AGAINST (R,S)-[I-125]IQNB
Autore:
GITLER MS; BOULAY SF; SOOD VK; MCPHERSON DW; KNAP FF; 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 OAK RIDGE NATL LAB,DIV HLTH SCI RES,NUCL MED GRP OAK RIDGE TN 37831 UNIV CHICAGO HOSP,DEPT RADIOL,NUCL MED SECT CHICAGO IL 60637
Titolo Testata:
Brain research
fascicolo: 1-2, volume: 687, anno: 1995,
pagine: 71 - 78
SICI:
0006-8993(1995)687:1-2<71:COIBMA>2.0.ZU;2-Y
Fonte:
ISI
Lingua:
ENG
Soggetto:
EMISSION COMPUTED-TOMOGRAPHY; RAT-BRAIN; ALZHEIMERS-DISEASE; 3-QUINUCLIDINYL 4-IODOBENZILATE; POTENTIAL RADIOPHARMACEUTICALS; INVIVO; BINDING; RADIOLIGAND; LIGAND;
Keywords:
ALZHEIMERS; MUSCARINIC RECEPTOR; M2 SUBTYPE; RADIOLIGAND; BRAIN IMAGING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
31
Recensione:
Indirizzi per estratti:
Citazione:
M.S. Gitler et al., "CHARACTERIZATION OF IN-VIVO BRAIN MUSCARINIC ACETYLCHOLINE-RECEPTOR SUBTYPE SELECTIVITY BY COMPETITION STUDIES AGAINST (R,S)-[I-125]IQNB", Brain research, 687(1-2), 1995, pp. 71-78

Abstract

We have studied the in vivo rat brain muscarinic acetylcholine receptor (mAChR) m2 subtype selectivities of three quinuclidine derivatives:(R)-3-quinuclidinyl benzilate (QNB), E-(+,+)-1-azabicyclo[2,2,2]oct-3-yl y-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate (E-(+, +)-IQNP), and E-(+, -)-1-azabicyclo[2.2.2]oct-3-yl y-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate (E-(+,-) IQNP), and two tricyclic ring compounds: ]-10,11-dihyro-5H-dibenzo[b,e][1,4]diazepin-11-one (DIBD) and iisobutylamino)butyl-1-phenyl]acetyl]-5,11-dihydro -6H-pyrido[2,3-b][1,4]benzodiazepin-6-one (PBID), by correlating the regional inhibition of (R,S)-[I-125]IQNB with the regional composition of the m1-m4 subtypes. Subtle effects are demonstrated after reduction of the between-animal variability by normalization to corpus striatum. Substantial in vivo m2-selectivity is exhibited by QNB and DIBD, modest in vivo m2-selectivity is exhibited by E-(+, +)-IQNP, and little or no in vivo m2-selectivity is exhibited by PBID and E-(+, -)-IQNP. Surprisingly, the in vivem2-selectivity is not correlated with the in vitro m2selectivity. Forexample, QNB, which appears to be the most strongly in vivo m2-selective compound, exhibits negligible in vitro m2-selectivity. These examples indicate that a strategy which includes only preliminary in vitro screening may very well preclude the discovery of a novel compound which would prove useful in vivo.

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Documento generato il 27/11/20 alle ore 05:54:27