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N-type calcium channel blockers in pain and stroke

journal contribution
posted on 2023-06-08, 19:29 authored by Brian Cox, Jane C Denyer
N-type calcium channels are located at presynaptic termini throughout the central nervous system (CNS), where they play a key role in the regulation of neurotransmitter release. In the pain pathway, N-type calcium channels in the spinal cord directly mediate spinal transmission of pain signals from the periphery to the CNS. In cerebral ischaemia, neuronal injury is also, in part, mediated through the activity of N-type calcium channels. The recent development of a selective N-type calcium channel blocking peptide, SNX-111 (Ziconotide, Neurex Corp., USA) has shown unequivocally that the N-type calcium channel is an important drug target for both analgesia and neuroprotection. SNX-111 is now in late stage clinical development for the treatment of various acute and chronic pain states, brain damage following cerebral ischaemia, closed head trauma and coronary artery bypass surgery. Over the last decade, the search for a selective small molecule blocker of N-type channels has been intense and has resulted in the discovery of a number of promising compounds, although none so far have been reported to have entered clinical trials.

History

Publication status

  • Published

Journal

Expert Opinion on Therapeutic Patents

ISSN

1354-3776

Publisher

Informa Healthcare

Issue

10

Volume

8

Page range

1237-1250

Department affiliated with

  • Chemistry Publications

Full text available

  • No

Peer reviewed?

  • Yes

Legacy Posted Date

2015-01-12

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