Document Detail

A surface active benzodiazepine receptor ligand for potential probing membrane order of GABAA-receptor surroundings.
MedLine Citation:
PMID:  18698836     Owner:  NLM     Status:  MEDLINE    
A conjugable analogue of the benzodiazepine 5-(2-hydroxiphenyl)-7-nitro-benzo[ e][1,4]diazepin-2(3 H)-one N 1-substituted with an aliphatic chain (CNZ acyl derivative, CAd) was synthesized. CAd inhibited FNZ binding to GABA A-R with an inhibition binding constant K i = 176 nM and expanded a model membrane packed up to 13 mN/m when penetrating from the aqueous phase. CAd exhibited surface activity with a collapse pressure pi = 18.8 mN/m and minimal molecular area A min = 49 A (2)/molecule at the closest molecular packing, resulting in full and nonideal mixing with a phospholipid in a monolayer up to a molar fraction x congruent with 0.1, decreasing its surface potential and contributing with a dipole that pointed its positive end toward the air and reoriented at the interface upon compression. These findings suggested that CAd could be stabilized at the membrane-water interface with its CNZ moiety stacked at the GABA A-R while its acyl chain can be inserted into the membrane depth.
Anahí V Turina; Benjamín Caruso; Gloria I Yranzo; Elizabeth L Moyano; María A Perillo
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-08-13
Journal Detail:
Title:  Bioconjugate chemistry     Volume:  19     ISSN:  1520-4812     ISO Abbreviation:  Bioconjug. Chem.     Publication Date:  2008 Sep 
Date Detail:
Created Date:  2008-09-17     Completed Date:  2008-12-16     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9010319     Medline TA:  Bioconjug Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1888-95     Citation Subset:  IM    
Biofísica-Química, Departamento de Química, Facultad de Ciencias Exactas, Físicas y Naturales, Universidad Nacional de Córdoba, Av. Vélez Sarsfield 1611, 5016 Córdoba, Argentina.
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MeSH Terms
Benzodiazepines / chemical synthesis*,  metabolism*
Binding, Competitive
Cell Membrane / chemistry,  metabolism*
Lipid Bilayers / chemistry,  metabolism
Phospholipids / chemistry,  metabolism
Receptors, GABA-A / chemistry,  metabolism*
Surface Properties
Reg. No./Substance:
0/Ligands; 0/Lipid Bilayers; 0/Phospholipids; 0/Receptors, GABA-A; 12794-10-4/Benzodiazepines

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