Evidence 1
Activity
Activity
Neurotoxin
FUNCTION: Omega-conotoxins act at presynaptic membranes, they bind and block voltage-gated calcium channels (Cav). This peptide reversibly and selectively inhibits Cav2.2/CACNA1B (IC(50)=11.5 nM) voltage-gated calcium channels. Channel time recovery after toxin exposure is short (about 50 seconds). In vivo, it effectively and dose-dependently reduces nociceptive behavior in the formalin test and in neuropathic pain models, and reduces mechanical and thermal allodynia in the tail nerve injury rat model. It also shows significant analgesic effects on writhing in mouse neurotransmitter- and cytokine-induced pain models, though it has no effect on acute thermal pain and interferon-gamma-induced pain. It also depresses blood pressure immediately after administration, but pressure recovers relatively quickly and completely. {ECO:0000269|PubMed:21172037}.
Target
voltage-gated calcium channel (Cav)
Source & Reference
NA
UniProtKB/Swiss-Prot Tox-Prot
Other
Conus fulmen (Thunderbolt cone) (Chelyconus fulmen)
Neurotoxin
Presynaptic neurotoxin
Calcium channel impairing toxin
Ion channel impairing toxin
Voltage-gated calcium channel impairing toxin
Omega-conotoxins act at presynaptic membranes, they bind and block voltage-gated calcium channels (Cav). This peptide reversibly and selectively inhibits Cav2.2/CACNA1B (IC(50)=11.5 nM) voltage-gated calcium channels.
Conotoxin FVIA
cone snail
Conotoxin O1 superfamily
Evidence at protein level
Amidation
Calcium channel impairing toxin
Disulfide bond
Ion channel impairing toxin
Knottin
Neurotoxin
Presynaptic neurotoxin
Secreted
Toxin
Voltage-gated calcium channel impairing toxin
TISSUE SPECIFICITY: Expressed by the venom duct. {ECO:0000305|PubMed:21172037}.