α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach[1][2].
The α-Conotoxin Vc1.1 is first discovered using a PCR screen of cDNAs from the venom ducts of Conus victoriae. α-Conotoxin Vc1.1 inhibits nicotine-evoked membrane currents in isolated bovine chromaffin cells in a concentration-dependent manner and preferentially targets peripheral nAChR subtypes over central subtypes. The three-dimensional structure of Vc1.1 comprises a small alpha-helix spanning residues Pro6 to Asp11 and is braced by the I-III, II-IV disulfide connectivity seen in other alpha-conotoxins. The cysteine spacing within the sequence of α-Conotoxin Vc1.1 suggests that it is a member of the 4/7 subclass of α-conotoxins, which includes the extensively studied conotoxins MII, EpI and PnIB[1].
α-Conotoxin Vc1.1 (0.18-18 μg/μL; intramuscular injection; daily; for 7 days; male Sprague-Dawley rats) treatment suppresses pain behaviors and also accelerates functional recovery of injured neurons in CCI rats[1].
References:
[1]. Richard J Clark, et al. The Synthesis, Structural Characterization, and Receptor Specificity of the Alpha-Conotoxin Vc1.1. J Biol Chem. 2006 Aug 11;281(32):23254-63.
[2]. Narmatha Satkunanathan, et al. Alpha-conotoxin Vc1.1 Alleviates Neuropathic Pain and Accelerates Functional Recovery of Injured Neurones. Brain Res. 2005 Oct 19;1059(2):149-58.