{"refrec":{"BRefID":289050,"RR":"<b>Tranberg, C.E.; Yang, A.; Vetter, I.; McArthur, J.R.; Baell, J.B.; Lewis, R.J.; Tuck, K.L.; Duggan, P.J.</b> (2012). ω-conotoxin GVIA mimetics that bind and inhibit neuronal Ca<sub>v</sub>2.2 ion channels. <i>Mar. Drugs 10(10)</i>: 2349-2368. <a href=\"https://dx.doi.org/10.3390/md10102349\" target=\"_blank\">https://dx.doi.org/10.3390/md10102349</a>","BEntID":281087,"PublicFlag":1,"CheckedFlag":1,"wosflag":1,"vabbflag":null,"RefStringPartII":". <i>Mar. Drugs 10(10)</i>: 2349-2368. <a href=\"https://dx.doi.org/10.3390/md10102349\" target=\"_blank\">https://dx.doi.org/10.3390/md10102349</a>","DocTypID":8,"DocType":"Journal article","MarineFlag":1,"FreshFlag":0,"BrackishFlag":0,"TerrestrialFlag":0,"Authorstring":"Tranberg, C.E.; Yang, A.; Vetter, I.; McArthur, J.R.; Baell, J.B.; Lewis, R.J.; Tuck, K.L.; Duggan, P.J.","OrigTitleTranslFlag":0,"Authorstringtrunc":"Tranberg, C.E. <i>et al.</i>","Englishabstract":"The neuronal voltage-gated N-type calcium channel (Ca<sub>v</sub>2.2) is a validated target for the treatment of neuropathic pain. A small library of anthranilamide-derived ω-Conotoxin GVIA mimetics bearing the diphenylmethylpiperazine moiety were prepared and tested using three experimental measures of calcium channel blockade. These consisted of a <sup>125</sup>I-ω-conotoxin GVIA displacement assay, a fluorescence-based calcium response assay with SH-SY5Y neuroblastoma cells, and a whole-cell patch clamp electrophysiology assay with HEK293 cells stably expressing human Ca<sub>v</sub>2.2 channels. A subset of compounds were active in all three assays. 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