Pharmacological profile of a potential anxiolytic : AP159, a new benzothieno-pyridine derivative

AP159 [N-cyclohexyl-1,2,3,4-tetrahydrobenzo(b)thieno(2,3c)pyridine]-3- carboamide,hydrochloride) showed clear anti-conflict activity in rats in the absence of effects on muscle relaxation, potentiation of anesthesia (in mice) or anticonvulsant activity (in mice). This anti-conflict effect was antago...

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Bibliographic Details
Published in:Psychopharmacologia 1991-08, Vol.104 (4), p.432-438
Main Authors: NAGATANI, T, YAMAMOTO, T, TAKAO, K, HASHIMOTO, S, KASAHARA, K, SUGIHARA, T, UEKI, S
Format: Article
Language:English
Subjects:
Aggression - drug effects
Animals
Anti-Anxiety Agents - pharmacology
Avoidance Learning - drug effects
Biological and medical sciences
Conflict (Psychology)
Drinking Behavior - drug effects
Ethanol - pharmacology
Flumazenil - pharmacology
Hydroxyindoleacetic Acid - metabolism
Male
Medical sciences
Mice
Mice, Inbred ICR
Mice, Inbred Strains
Motor Activity - drug effects
Muscle Relaxants, Central - pharmacology
Neuropharmacology
Pharmacology. Drug treatments
Postural Balance - drug effects
Psycholeptics: tranquillizer, neuroleptic
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Pyridines - pharmacology
Rats
Rats, Inbred Strains
Seizures - chemically induced
Seizures - prevention & control
Serotonin - metabolism
Thienopyridines
Thiopental - pharmacology
Thiophenes - pharmacology
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Summary:AP159 [N-cyclohexyl-1,2,3,4-tetrahydrobenzo(b)thieno(2,3c)pyridine]-3- carboamide,hydrochloride) showed clear anti-conflict activity in rats in the absence of effects on muscle relaxation, potentiation of anesthesia (in mice) or anticonvulsant activity (in mice). This anti-conflict effect was antagonized by treatment with Ro15-1788. By contrast with the deficits produced by diazepam, AP159 did not impair passive avoidance. The latter drug also improved scopolamine-induced amnesia in the same task. AP159 did not inhibit 3H-flunitrazepam binding, but potently inhibited 3H-8OH-DPAT binding. This compound increased serotonin and 5HIAA content of the midbrain raphe nuclei and of the amygdala centralis. AP159 has been shown to be a novel non-BZP anxiolytic agent with no side effects in laboratory animals; it could be a clinically effective anxiolytic agent.
ISSN:0033-3158
1432-2072
DOI:10.1007/bf02245645