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Titolo:
NOVEL POTENT AND M(2)-SELECTIVE ANTIMUSCARINIC COMPOUNDS WHICH PENETRATE THE BLOOD-BRAIN-BARRIER
Autore:
COHEN VI; JIN B; GITLER MS; DELACRUZ RA; BOULAY SF; SOOD VK; ZEEBERG BR; REBA RC;
Indirizzi:
GEORGE WASHINGTON UNIV,MED CTR,RADIOPHARMACEUT CHEM SECT WASHINGTON DC 20037 UNIV CHICAGO HOSP & CLIN,DEPT RADIOL,NUCL MED SECT CHICAGO IL 60637
Titolo Testata:
European journal of medicinal chemistry
fascicolo: 1, volume: 30, anno: 1995,
pagine: 61 - 69
SICI:
0223-5234(1995)30:1<61:NPAMAC>2.0.ZU;2-X
Fonte:
ISI
Lingua:
ENG
Soggetto:
RAT-BRAIN; ANTAGONISTS; RECEPTORS; SELECTIVITY;
Keywords:
M(2)-SELECTIVE ANTIMUSCARINIC AGENT; BLOOD-BRAIN BARRIER;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
14
Recensione:
Indirizzi per estratti:
Citazione:
V.I. Cohen et al., "NOVEL POTENT AND M(2)-SELECTIVE ANTIMUSCARINIC COMPOUNDS WHICH PENETRATE THE BLOOD-BRAIN-BARRIER", European journal of medicinal chemistry, 30(1), 1995, pp. 61-69

Abstract

A series of 10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-11-ones 1 wereprepared as potential m(2)-selective ligands. The binding affinities and selectivities of these compounds for the muscarinic cholinergic receptor subtypes were determined. The best m(2)-selective antimuscarinic agent studied was )butyl]-1-phenyl]acetyl]-10,11-dihydro-5H-dibenzo[1h (DIBD), which caused a significant reduction in (R,R)-3-quinuclidinyl-[I-125] -4-iodobenzilate ((R,R)-[I-125]-4IQNB) binding in brain regions known to contain a high percentage of m(2)-receptors. Thus DIED penetrates the blood-brain barrier and exhibits in vivo selectivity for the m, subtype. In contrast, neither DIBA,AF-DX 116, nor AQ-RA 741 caused a significant m(2)-selective reduction in (R,R)-[I-125]-4IQNB binding in the brain regions studied.

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Documento generato il 23/11/20 alle ore 21:45:40