- A potent and selective indole N-type calcium channel (Cav2.2) blocker for the treatment of pain
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N-type calcium channels (Cav2.2) have been shown to play a critical role in pain. A series of low molecular weight 2-aryl indoles were identified as potent Cav2.2 blockers with good in vitro and in vivo potency.
- Tyagarajan, Sriram,Chakravarty, Prasun K.,Park, Min,Zhou, Bishan,Herrington, James B.,Ratliff, Kevin,Bugianesi, Randall M.,Williams, Brande,Haedo, Rodolfo J.,Swensen, Andrew M.,Warren, Vivien A.,Smith, McHardy,Garcia, Maria,Kaczorowski, Gregory J.,McManus, Owen B.,Lyons, Kathryn A.,Li, Xiaohua,Madeira, Maria,Karanam, Bindhu,Green, Mitchell,Forrest, Michael J.,Abbadie, Catherine,McGowan, Erin,Mistry, Shruti,Jochnowitz, Nina,Duffy, Joseph L.
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scheme or table
p. 869 - 873
(2011/03/18)
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- 2-SUBSTITUTED INDOLE DERIVATIVES AS CALCIUM CHANNEL BLOCKERS
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2-Substituted indole derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
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Page/Page column 42-43
(2008/12/08)
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