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

Journal Letters in Drug Design and Discovery
ISSN: 1570-1808 , E-ISSN: 1875-628X
Output data Year: 2012, Volume: 9, Number: 5, Pages: 513-516 Pages count : 4 DOI: 10.2174/157018012800389296
Tags Analgesic activity; Benzopentathiepine; Acetic acid-induced writhing test; Hot plate test; Opioidergic system
Authors Tolstikova Tatyana G. 1 , Pavlova Alla V. 1 , Morozova Ekaterina A. 1 , Khomenko Tatyana M. 1 , Volcho Konstantin P. 1 , Salakhutdinov Nariman F. 1
Affiliations
1 N.N.Vorozhtsov Novosibirsk Institute of Organic Chemistry, Siberian Branch, Russian Academy of Sciences, Lavrentiev av., 9, 630090 Novosibirsk, Russian Federation

Abstract: 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 acid-induced writhing test.
Cite: Tolstikova T.G. , Pavlova A.V. , Morozova E.A. , Khomenko T.M. , Volcho K.P. , Salakhutdinov N.F.
The Analgesic Activity of 8-(Trifluoromethyl)-1,2,3,4,5-benzopentathiepine-6-amine and Its Hydrochloride
Letters in Drug Design and Discovery. 2012. V.9. N5. P.513-516. DOI: 10.2174/157018012800389296 WOS Scopus РИНЦ
Dates:
Published print: Apr 26, 2012
Identifiers:
Web of science WOS:000308667300010
Scopus 2-s2.0-84860762141
Elibrary 17984830
OpenAlex W2735543072
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