Analgesic and anticonvulsive activity new compounds with norbornene and adamantane fragments
| Autor: | H.T. Zlenko, L.I. Kasyan, H.A. Golodaeva, Vitaliy A. Palchikov, M.I. Stefanik |
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| Rok vydání: | 2011 |
| Předmět: | |
| Zdroj: | European Psychiatry. 26:1007-1007 |
| ISSN: | 1778-3585 0924-9338 |
| DOI: | 10.1016/s0924-9338(11)72712-2 |
| Popis: | IntroductionThe present work deals with analgesic and anticonvulsive activity of four novel aminoalcohols C-81, C-78, C-115 and C-120 synthesized on basic glycidylcamphorimide (Gly-CI), exo- and endo-aminomethylnorbornenes, aminoethyladamantan (remantadin) and aminoethylnorbornan (deitiforin).AimsSynthesis cage-like compounds with excellent analgesic and anticonvulsive activity. Methods: Experiments have been carried out on both genders adult white mice at the dozes of 1/10 LD50. Investigated substances were entered intraperitoneally. Preparations have been entered as a water suspension on TWEEN-40. Acute toxicity of compounds (LD50) has been measured by Litchfield & Wilcoxon method in Prozorovsky V.B. modification and amounts 370–1196 mg/kg.ResultsThe most toxic compound is aminoalcohol C-115 with adamantane fragment. Investigation of analgesic activity has been carried out by determination of pain threshold by thermal irritation method (hot plate) at 55°C. Anticonvulsive activity has been studied by corazole spasm test. The activity has been calculated in percentage in relation to control group of animals.ConclusionsAll aminoalcohols have shown analgesic and (except for compound C-81) anticonvulsive activity. For exo-aminoalcohol C-81 the most intense activity are analgesic (195.0%) and for endo-isomer C-78 - anticonvulsive activity (213.3%). Compounds C-115 and C-120 shows medium analgesic (67.1 and 58.5%) and anticonvulsive activity (13.4 and 67.5%). |
| Databáze: | OpenAIRE |
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