Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


The Analgesic Activity of 8-(Trifluoromethyl)-1,2,3,4,5-benzopentathiepine- 6-amine and Its Hydrochloride

Author(s): Tatyana G. Tolstikova, Alla V. Pavlova, Ekaterina A. Morozova, Tatyana M. Khomenko, Konstantin P. Volcho, Nariman F. Salakhutdin.


8-(Trifluoromethyl)-1,2,3,4,5-benzopentathiepine-6-amine 1a and its hydrochloride revealed significant analgesic activity in the acetic acid-induced writhing test, and ED50 of the compound 1a was 0.66 mg/kg. In the hot plate pain test, the reliable analgesic activity was found in hydrochloride 1a*HCl, whereas the free base 1a proved to be inactive. Based on the results of the naloxone test, the analgesic effect of the compound 1a*HCl in both tests is mediated with the opioidergic system. Both the free base 1a and its hydrochloride did not show the anti-inflammatory activity. Replacement of the CF3 group for the fluorine atom resulted in complete loss of analgesic activity in the acetic acidinduced writhing test.

Keywords: renal impairment, antidepressants, fibromyalgia, anti-seizure drugs, Paroxetin, anticonvulsant, Analgesic Tests, Anti-Inflammatory Activity, acetic acid-induced writhing test, inflammatory agent

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Article Details

Year: 2012
Page: [513 - 516]
Pages: 4
DOI: 10.2174/157018012800389296
Price: $58