Synthesis and receptor binding studies of 2-functionalized 1,4-benzodiazepine derivatives as potential metaclazepam-like antianxiety agents

M Anzini; A Cappelli; S Vomero; A Cagnotto; M Skorupska

Synthesis and receptor binding studies of 2-functionalized 1,4-benzodiazepine derivatives as potential metaclazepam-like antianxiety agents

Farmaco. 1993 Jul;48(7):897-905.

Authors

M Anzini¹, A Cappelli, S Vomero, A Cagnotto, M Skorupska

Affiliation

¹ Dipartimento Farmaco Chimico Tecnologico, Università Degli Studi di Siena, Italy.

PMID: 8104405

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

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
Rats
Receptors, GABA-A / drug effects
Receptors, GABA-A / metabolism*
Structure-Activity Relationship

Substances

Anti-Anxiety Agents
Receptors, GABA-A
Benzodiazepines
metaclazepam