- TOLPERISONE ANALOGS AND METHODS OF USE
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The present invention is, in part, directed to tolperisone analogs (e.g., compounds of formula (I), (I-a), (I-b), (II), (Il-a), (III), (Ill-a), (ΙΙΙ-b), (III-c), (IV), (IV-a), (V), or (V-a)) and methods of use thereof for the treatment of various conditions including elevated muscle tone and tension (e.g., spasticity, muscle spasm). In one aspect, the tolperisone analogs disclosed herein have an additional substituent at the α-position, which blocks the generation of a β- elimination product.
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Page/Page column 28
(2019/10/29)
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- Synthesis of 3H-tolperisone
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Tolperisone has been tritiated to 50 Ci/mmol specific activity in order to use this compound in the study of muscle relaxant binding. Of the two reaction pathways investigated, hydrogenolytic exchange of aromatic bromine is favored over hydrogenation of a double bond.
- Dietrich, Axel,Fels, Gregor
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p. 1125 - 1134
(2007/10/03)
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