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A potent and selective indole N-type calcium channel (Ca(v)2.2) blocker for the treatment of pain |
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| Authors: | 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 |
| Affiliation: | a Departments of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA b Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Rahway, NJ 07065, USA c Ion Channels, Merck Research Laboratories, Rahway, NJ 07065, USA d Pharmacology, Merck Research Laboratories, Rahway, NJ 07065, USA |
| Abstract: | 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. |
| Keywords: | Pain N-type calcium channel Cav2.2 blockers Indoles Chung model |
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