α-ConotoxinBuIAhasbeenidentifiedwithinthevenomofthemarinesnailConusBullatus. α-ConotoxinBuIAisapotentblockerofneuronalnicotinicacetylcholinereceptorswithinterestingselectivitypropertiesamongisoforms.Inparticular,itdiscriminatesbestratα6-subunitcontainingneuronalAChRoverα4-containingreceptorswithrespectiveIC50valuesof0.25nMforα6/α3β2chimerasand10µMforα4β2.However,thelevelofdiscriminationismainlyβ-isoformdependentbecausethekineticsofunblockaredependentontheβ-subunittype.NeuronalAChRscontainingβ4ratherthanβ2haveaveryslowoffrateforα-ConotoxinBuIA.ThisistruealsoforhumanAChRs.Asaresult,theIC50valuesforα3β2andα3β4are,respectively,5.7nMand27nMandtheirKoff,respectively,0.65min-1and0.011min-1.α-ConotoxinBuIA canthusbeadvantageouslyusedtodiscriminatebetweena-isoformsandalsobetweenβ2andβ4isoforms.
Description:
AAsequence:GCCSTPPCAVLYC-NH2
Disulfidebonds:Cys2-Cys8;Cys3-Cys13
Formula:C54H82N14O16S4
Appearance:Whitelyophilizedsolid
MolecularWeight: 1311.59g/mol
Source:Synthetic
Counterion:TFAsalts
Solubility:Waterorsalinebuffer