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Biological properties of the benzodiazepine amidine derivative L-740,093, a cholecystokinin-B/gastrin receptor antagonist with high affinity in vitro and high potency in vivo.

Abstract:

A novel series of 5-amino-1,4-benzodiazepin-2-one derivatives (amidines), which contain a cationic solubilizing group and which are antagonists for the cholecystokinin (CCK)-B receptor, have been identified. Optimization of this series led to the identification of an azabicyclononane amidine, L-740,093 [N-[(3R)-5-(3-azabicyclo[3.2.2]nonan-3-yl)-2,3-dihydro-1-methyl-2- oxo- 1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)urea], that bound with high affinity of CCK-B receptors from guinea pig cer...

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Publication status:
Published

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Journal:
Molecular pharmacology
Volume:
46
Issue:
5
Pages:
943-948
Publication date:
1994-11-01
EISSN:
1521-0111
ISSN:
0026-895X
Source identifiers:
18030
Language:
English
Keywords:
Pubs id:
pubs:18030
UUID:
uuid:d724b063-2a42-4857-adb3-3a69f8d30bc5
Local pid:
pubs:18030
Deposit date:
2012-12-19

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