Literature DB >> 7870872

Neuropharmacology of a new potential anxiolytic compound, F 2692, 1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine. 1. Acute and in vitro effects.

M B Assié1, P Chopin, A Stenger, C Palmier, M Briley.   

Abstract

F 2692 [1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine] exhibited dose-dependent "anxiolytic" properties in the elevated plus-maze and the punished drinking tests in rats. It was also active in the two-compartment test in mice. The "anxiolytic" effects were antagonised by the benzodiazepine antagonists, flumazenil and ZK 93426. The compound exhibited anticonvulsant, sedative, myorelaxant and amnesic effects at doses 3-30 times higher than those required for "anxiolytic" activity. F 2692 has a very low affinity for benzodiazepine binding sites in vitro and in vivo (about 1000 and 160 fold lower than diazepam respectively). In addition it displayed no affinity for GABAA, alpha 2-adrenergic, 5-HT1A or 5-HT2 receptors. These data suggest that F 2692 may be a potential anxiolytic compound with an unusual mechanism of action.

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Year:  1993        PMID: 7870872     DOI: 10.1007/bf02246945

Source DB:  PubMed          Journal:  Psychopharmacology (Berl)        ISSN: 0033-3158            Impact factor:   4.530


  31 in total

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Journal:  Brain Res       Date:  1978-06-09       Impact factor: 3.252

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Authors:  P Chopin; M Briley
Journal:  J Pharm Pharmacol       Date:  1990-05       Impact factor: 3.765

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Journal:  Pharmacol Biochem Behav       Date:  1985-10       Impact factor: 3.533

5.  Validation of open:closed arm entries in an elevated plus-maze as a measure of anxiety in the rat.

Authors:  S Pellow; P Chopin; S E File; M Briley
Journal:  J Neurosci Methods       Date:  1985-08       Impact factor: 2.390

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Authors:  W Haefely; J R Martin; P Schoch
Journal:  Trends Pharmacol Sci       Date:  1990-11       Impact factor: 14.819

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Authors:  D P Taylor
Journal:  FASEB J       Date:  1988-06       Impact factor: 5.191

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Authors:  P P Roy-Byrne; D Hommer
Journal:  Am J Med       Date:  1988-06       Impact factor: 4.965

9.  Effects of prolonged administration of milnacipran, a new antidepressant, on receptors and monoamine uptake in the brain of the rat.

Authors:  M B Assie; M Charveron; C Palmier; C Puozzo; C Moret; M Briley
Journal:  Neuropharmacology       Date:  1992-02       Impact factor: 5.250

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Journal:  Pharmacol Biochem Behav       Date:  1980-08       Impact factor: 3.533

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  3 in total

1.  The benzodiazepine antagonist flumazenil blocks the effects of CCK receptor agonists and antagonists in the elevated plus-maze.

Authors:  P Chopin; M Briley
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

2.  Neuropharmacology of a new potential anxiolytic compound, F 2692, 1-(3'-trifluoromethyl phenyl) 1, 4-dihydro 3-amino 4-oxo 6-methyl pyridazine. 2. Evaluation of its tolerance and dependence producing potential and of its effects on benzodiazepine withdrawal in the elevated plus-maze test in rats.

Authors:  P Chopin; M B Assié; M Briley
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

3.  The GABAA-Benzodiazepine Receptor Antagonist Flumazenil Abolishes the Anxiolytic Effects of the Active Constituents of Crocus sativus L. Crocins in Rats.

Authors:  Nikolaos Pitsikas; Petros A Tarantilis
Journal:  Molecules       Date:  2020-11-30       Impact factor: 4.411

  3 in total

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