TABLE 2

Clinical potential and representative sequences of major conotoxin classes defined by pharmacology

Cysteines involved in disulfide bonds (underlined) connect in discrete overlapping patterns depending on sequence (see Tables 4, 5, 79, and 11).

ClassMode of ActionNameSequenceClinical Potential
ωCav2.2 inhibitorMVIIACKGKGAKCSRLMYDCCTGSCRSGKC*Pain (intrathecal; phase IV)
μNav inhibitorSIIIAZNCCNGGCSSKWCRDHARCC*Pain (intravenous)
μONav1.8 inhibitorMrVIBACSKKWEYCIVPIIGFIYCCPGLICGPFVCVPain (intrathecal/intravenous)
δNav enhancerEVIADDCIKOYGFCSLPILKNGLCCSGACVGVCADL*?
κKv inhibitorPVIIACRIONQKCFQHLDDCCSRKCNNRFNKCVCardiac reperfusion
χNET inhibitorXen2174ZGVCCGYKLCHOCPain (intrathecal; phase II)
αnAChR inhibitorVc1.1GCCSDPRCNYDHPEIC*Pain (intravenous)a
σ5HT3 receptorGVIIIAGCTRTCGGOKCTGTCTCTNSSKCGCRYNVHPSGBGCGCACS*?
ρα1-Adrenoceptor inhibitorTIAFNWRCCLIPACRRNHKKFC*Cardiovascular/BPH
ConantokinNMDA-R antagonistCon-GGEγγLQγNQγLIRγKSNPain/epilepsy (intrathecal)a
ConopressinVasopressin-R agonistCono-GCFIRNCPKG*Cardiovascular/mood
ContulakinNeurotensin-R agonistCont-GZSEEGGSNAtKKPYIlLPain (intrathecal)a
  • * , C-terminal amidation.

  • a Clinical development suspended.