Tricyclics with analgesic and antidepressant activity. 2. [[(Alkylamino)ethyl]thio]dibenzo[b,f]thiepins and 10,11-dihydro derivatives
| Autor: | T. C. Spaulding, Harry M. Geyer, James A. Profitt, Vernon B. Anderson, Helen H. Ong, J. C. Wilker |
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| Rok vydání: | 1982 |
| Předmět: |
Dibenzothiepins
Male Apomorphine Chemical Phenomena Stereochemistry Analgesic Thio Physical dependence (+)-Naloxone Antidepressive Agents Tricyclic 5-Hydroxytryptophan Drug Discovery Benzoquinones medicine Animals Blepharoptosis Humans Analgesics Chemistry Quinones Rats Amphetamine Molecular Medicine Antidepressant Stereotyped Behavior medicine.symptom Antipsychotic Agents |
| Zdroj: | Journal of Medicinal Chemistry. 25:1150-1153 |
| ISSN: | 1520-4804 0022-2623 |
| Popis: | A series of [[(alkylamino)ethyl]thio]dibenz[b,f]oxepins (I) and their 10,11-dihydro derivatives (II) was synthesized and subjected to broad analgesic/CNS screening. Several analogues of both types, carrying small N-substituents and frequently a nuclear fluorine function, have been found to possess potent analgesic activity in the phenylquinone writhing assay (PQW) and the tail-flick test in mice. Many of these compounds also exhibited significant activity in antagonizing tetrabenazine-induced ptosis, as exemplified by 10b, 16b, and 18b. Results from the mouse jumping test indicated low physical dependence potential for these compounds, and further evidence for a nonnarcotic profile was provided by the absence of significant naloxone interactions with the tail-flick response. Compound 10b did not produce tolerance in mice following chronic administration in the PQW screen. |
| Databáze: | OpenAIRE |
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