Synthesis and anxiolytic activity of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines
- 1 May 1981
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 24 (5) , 592-600
- https://doi.org/10.1021/jm00137a020
Abstract
The synthesis of a series of 6-(substituted-phenyl)-1,2,4-triazolo[4,3-b]pyridazines (VIII) is reported. Some of these derivatives show activity in tests predictive of anxiolytic activity [protection against pentylenetetrazole-induced convulsions; thirsty rat conflict procedure]. They also represent a new class of compound which inhibits [3H]diazepam binding. Structure-activity correlations, and the ability of structures VIII to inhibit [3H]diazepam binding (in vitro), are discussed.This publication has 20 references indexed in Scilit:
- Rapid Changes in Brain Benzodiazepine Receptors After Experimental SeizuresScience, 1978
- Identification of inosine and hypoxanthine as endogenous inhibitors of [3H] diazepam binding in the central nervous systemLife Sciences, 1978
- Novel anxiolytic agents derived from .alpha.-amino-.alpha.-phenyl-o-tolyl-4H-triazoles and -imidazolesJournal of Medicinal Chemistry, 1978
- Benzodiazepine binding in human brain: Characterization using [3H] flunitrazepamLife Sciences, 1978
- Biochemical identification of the site of action of benzodiazepines in human brain by 3H-diazepam bindingLife Sciences, 1978
- Central nervous system depressants. 14. As‐triazino‐1,4‐benzodiazepinesJournal of Heterocyclic Chemistry, 1977
- Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding.Proceedings of the National Academy of Sciences, 1977
- Diazepines. IV. Synthesis and biological action of 6-phenyl-4H-imidazo[1,2-a][1,5]benzodiazepin-5(6H)-ones.CHEMICAL & PHARMACEUTICAL BULLETIN, 1977
- Conversion of N-alkylaminobenzophenones to benzodiazepines in vivoJournal of Medicinal Chemistry, 1976
- Synthesis and pharmacology of novel anxiolytic agents derived from 2-[(dialkylamino)methyl-4H-triazol-4-yl]benzophenones and related heterocyclic benzophenonesJournal of Medicinal Chemistry, 1976