Abstract
The voltage-dependent N-type calcium channel (Cav2.2), which is distributed in the nerve endings of the central and peripheral nerves, is known to be strongly associated with the pathological processes of cerebral ischemia and neuropathic pain. Ziconotide, the chemically synthesized version of the 25-residue peptide marine toxin ω-conotoxin MVIIA, has been approved as an analgesic drug for severe chronic pain treatment. A blockade of N-type calcium channels has been suggested for reducing the neuronal injury occurring from ischemia/reperfusion events. Therefore, many efforts have been made to develop systemically available small-molecule N-type calcium channel blockers thus far. This review focuses on the latest updates concerning small-molecule N-type calcium channel blockers as potential candidates for the next generation of therapeutics for neuropathic pain and ischemic stroke. The pharmacological advantages of N-type calcium channel blockers in these pathological states are also described.
Keywords: N-type calcium channel blockers, neuropathic pain, neuroprotection, small molecule, review
Current Topics in Medicinal Chemistry
Title: Recent Updates of N-Type Calcium Channel Blockers with Therapeutic Potential for Neuropathic Pain and Stroke
Volume: 9 Issue: 4
Author(s): Takashi Yamamoto and Akira Takahara
Affiliation:
Keywords: N-type calcium channel blockers, neuropathic pain, neuroprotection, small molecule, review
Abstract: The voltage-dependent N-type calcium channel (Cav2.2), which is distributed in the nerve endings of the central and peripheral nerves, is known to be strongly associated with the pathological processes of cerebral ischemia and neuropathic pain. Ziconotide, the chemically synthesized version of the 25-residue peptide marine toxin ω-conotoxin MVIIA, has been approved as an analgesic drug for severe chronic pain treatment. A blockade of N-type calcium channels has been suggested for reducing the neuronal injury occurring from ischemia/reperfusion events. Therefore, many efforts have been made to develop systemically available small-molecule N-type calcium channel blockers thus far. This review focuses on the latest updates concerning small-molecule N-type calcium channel blockers as potential candidates for the next generation of therapeutics for neuropathic pain and ischemic stroke. The pharmacological advantages of N-type calcium channel blockers in these pathological states are also described.
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Cite this article as:
Yamamoto Takashi and Takahara Akira, Recent Updates of N-Type Calcium Channel Blockers with Therapeutic Potential for Neuropathic Pain and Stroke, Current Topics in Medicinal Chemistry 2009; 9 (4) . https://dx.doi.org/10.2174/156802609788317838
DOI https://dx.doi.org/10.2174/156802609788317838 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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