1220348-66-2Relevant academic research and scientific papers
Neuropathic pain-alleviating effects of pyrazole-conjugated arylsulfonamides as 5-HT6 receptor antagonists
Hong, Jin Ri,Choo, Hyunah,Nam, Ghilsoo
, p. 4146 - 4149 (2017/08/23)
A novel series of arylsulfonylaminomethyl-3-(1-phenyl-5-isopropyl)pyrazoles was evaluated for serotonin receptor subtype 6 (5-HT6R) antagonistic effects in vitro. We also investigated their neuropathic pain-alleviating effects in vivo using a rat spinal nerve ligation (SNL) model. Bicyclic aromatic sulfonamino groups, such as naphthalene and quinolin-substituted derivatives, showed good 5-HT6 inhibitory activity in vitro. Among them, selected compounds, 12 and 13, having 8-quinoylsulfonamino groups, showed potent neuropathic pain-alleviating effects in the rat model.
Synthesis and T-type calcium channel-blocking effects of aryl(1,5-disubstituted-pyrazol-3-yl)methyl sulfonamides for neuropathic pain treatment
Kim, Jung Hyun,Keum, Gyochang,Chung, Hesson,Nam, Ghilsoo
, p. 665 - 672 (2016/08/19)
A novel series of aryl(1,5-disubstituted pyrazol-3-yl)methyl sulfonamide derivatives was designed, synthesized, and evaluated for T-type calcium channel (α1Gand α1H) inhibitory activity. We identified several compounds, 9a, 9b, 9g, and 9h that displayed good T-type channel inhibitory potency with low hERG channel and CYP450 inhibition. Among them, 9a and 9b exhibited neuropathic pain alleviation effects in mechanical and cold allodynia induced in the SNL rat model. Compounds 9a and 9b displayed better efficacy than mibefradil and gabapentin against cold allodynia. In particular, compound 9a seemed to be valuable as shown fast acting performance in mechanical neuropathic pain model.
COMPOUNDS CAPABLE OF INHIBITING VOLTAGE GATED CALCIUM ION CHANNEL, AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME
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Paragraph 0270; 0271, (2015/12/12)
Disclosed herein are an N-(pyrazolylmethyl)arylsulfonamide derivative useful as a calcium ion channel blocker, a pharmaceutically acceptable salt thereof, and the medicinal use thereof as a therapeutic agent using its calcium ion channel blocking effect.
NOVEL 6-PYRAZOLYLAMIDO-3-SUBSTITUTED AZABICYCLO[3.1.0]HEXANE COMPOUNDS AS CALCIUM CHANNEL INHIBITORS
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Paragraph 0105; 0106; 0107, (2014/12/09)
The present invention relates to a 6-pyrazolylamido-3-substituted azabicyclo[3.1.0]hexane derivatives useful as calcium channel blockers, pharmaceutically acceptable salts thereof and medical use of the calcium channel inhibiting effect of the compounds for treatment of diseases.
NOVEL PYRAZOLYLMETHYLAMINE COMPOUNDS AS CALCIUM CHANNEL MODULATORS AND PREPARATION METHOD THEREOF
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Page/Page column 9, (2010/04/30)
The present invention relates to pyrazolylmethylamine-piperazine derivatives and their pharmaceutically acceptable salts effective as calcium channel modulators and a method of manufacturing the same. The present invention also relates to the medicinal us
