SYNTHESIS AND RECEPTOR-BINDING STUDIES OF 2-FUNCTIONALIZED 1,4-BENZODIAZEPINE DERIVATIVES AS POTENTIAL METACLAZEPAM-LIKE ANTIANXIETY AGENTS

The synthesis of 7-chloro-2,3-dihydro-2-(2-methoxyethyl)-1-methyl-5-phenyl-1H-1,4-benzodiazepine (2) is described. While the metaclazepam-like compound 2 showed an affinity for benzodiazepine receptor central type (CBZRs) comparable to that of metaclazepam (1a), its intermediates bearing the exocycl...

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Bibliographic Details
Published inFarmaco (Società chimica italiana : 1989) Vol. 48; no. 7; pp. 897 - 905
Main Authors ANZINI, M, CAPPELLI, A, VOMERO, S, CAGNOTTO, A, SKORUPSKA, M
Format Journal Article
LanguageEnglish
Published ROME Soc Chimica Italiana 01.07.1993
Subjects
Animals
Anti-Anxiety Agents - chemical synthesis
Anti-Anxiety Agents - metabolism
Anti-Anxiety Agents - pharmacology
Benzodiazepines - chemical synthesis
Benzodiazepines - metabolism
Benzodiazepines - pharmacology
Brain Chemistry - drug effects
In Vitro Techniques
Life Sciences & Biomedicine
Pharmacology & Pharmacy
Rats
Receptors, GABA-A - drug effects
Receptors, GABA-A - metabolism
Science & Technology
Structure-Activity Relationship
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Summary:The synthesis of 7-chloro-2,3-dihydro-2-(2-methoxyethyl)-1-methyl-5-phenyl-1H-1,4-benzodiazepine (2) is described. While the metaclazepam-like compound 2 showed an affinity for benzodiazepine receptor central type (CBZRs) comparable to that of metaclazepam (1a), its intermediates bearing the exocyclic double bond resulted more active.
ISSN:0014-827X