Selective antagonist of N-type voltage sensitive calcium channels (VSCC). Blocks neurotransmitter release by preventing depolarization-induced calcium influx. Synthetic, 25-residue peptide corresponding to one of the conotoxins, q.v., derived from the venom of the marine cone snail, Conus magus L. Synthesis: B. M. Olivera et al., Biochemistry 26, 2086 (1987). Structure-activity study: L. Nadasdi et al., ibid. 34, 8076 (1995). Binding study and use as biochemical tool: R. Kristipati et al., Mol. Cell. Neurosci. 5, 219 (1994). NMR studies: L. K. MacLachlan et al., Methods Mol. Biol. 60, 337 (1997). Radioimmunoassay: C. M. Barksdale et al., J. Clin. Ligand Assay 19, 229 (1996). Clinical pharmacology: D. McGuire et al., J. Cardiovasc. Pharmacol. 30, 400 (1997). Clinical trial in pain relief from cancer or AIDS: P. S. Staats et al., J. Am. Med. Assoc. 291, 63 (2004).
Analgesic; neuroprotective.
Neuroprotective; Analgesic; Non-opioids