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Benzothiophenes as potent analgesics against neuropathic pain

Yadav, S and Dwivedi, VK and Gupta, S and Surolia, A (2019) Benzothiophenes as potent analgesics against neuropathic pain. [Book Chapter]

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Official URL: https://doi.org/10.1007/978-981-13-3065-0_17


Neuropathic pain arises because of neuronal injury. Unlike inflammatory pain which can be managed by classical nonsteroid anti-inflammatory drugs (NSAIDs), neuropathic pain is difficult to treat. The classical NSAIDs work through inhibition of cyclooxygenase 2 (COX2) enzyme. However, COX2 inhibitors are insufficient to treat neuropathic pain. Hence, it becomes important to explore for novel molecules acting through cell surface molecules like ion channels, for the treatment of neuropathic pain. We investigated multiple bromobenzothiophene carboxamides for their efficacy against neuropathic pain. Interestingly, AS6 was found to be very effective in treating neuropathic pain through inhibition of Kv4.3 ion channel. AS6 also reduced the COX2 overexpression associated with neuropathic pain. These results as well as results from our previous study indicate that AS6 can be a potent antinociceptive agent against both inflammatory and neuropathic pain.

Item Type: Book Chapter
Publication: Advances in Experimental Medicine and Biology
Series.: Advances in Experimental Medicine and Biology
Publisher: Springer New York LLC
Additional Information: The copyright for this article belongs to the Springer New York LLC.
Keywords: 3 bromo n (2 phenylethyl) benzobthiophene; 3 bromo n (4 fluorobenzyl) benzobthiophene 2 carboxamide; 3 bromo n (4 fluorobenzyl) n (prop 2 en 1 yl) benzobthiophene 2 carboxamide; 3 bromo n 4 (trifluoromethyl)benzyl benzobthiophene 2 carboxamide; analgesic agent; benzothiophene derivative; cyclooxygenase 2; indometacin; morphine; n benzyl 3 bromobenzobthiophene 2 carboxamide; potassium channel; potassium channel Kv4.3; unclassified drug; analgesic agent; benzothiophene; cyclooxygenase 2; cyclooxygenase 2 inhibitor; PTGS2 protein, human; thiophene derivative, analgesic activity; animal experiment; animal model; animal tissue; controlled study; drug efficacy; drug mechanism; human; human cell; inflammatory pain; male; neuropathic pain; nonhuman; priority journal; rat; inflammation; metabolism; neuralgia, Analgesics; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Humans; Inflammation; Neuralgia; Thiophenes
Department/Centre: Division of Biological Sciences > Molecular Biophysics Unit
Date Deposited: 18 Aug 2022 06:44
Last Modified: 18 Aug 2022 06:44
URI: https://eprints.iisc.ac.in/id/eprint/75960

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