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. Author manuscript; available in PMC: 2022 Jul 8.
Published in final edited form as: J Med Chem. 2021 Jun 18;64(13):9271–9278. doi: 10.1021/acs.jmedchem.1c00512

Table 2.

C-terminal substitutions and their impact on the potency of RgIA-5474 on blocking human α9α10 nAChRs.

Analog Sequence IC50a (nM) 95% CI (nM)
RgIA-5624b GC(Pen)TDPRCRI3YQCYR 0.51 0.34–0.75
RgIA-5433 GC(Pen)TDPRCRI3YQCyr 2.1 1.4–3.2
RgIA-5474 GC(Pen)TDPRCRI3YQC(β3hY)R 0.0504 0.037–0.069
RgIA-5477 GC(Pen)TDPRCRI3YQC(β3hY)r 0.36 0.28–0.46
a

Data were collected by applying 100 μM ACh to Xenopus oocytes heterologously expressing the receptor. IC50 and 95% confidence intervals (CI) are expressed as the mean ± SEM from 3–5 separate oocytes. Ba2+ containing ND-96 buffer was utilized. Blue colored residues indicate changes introduced into the sequence in this series of analogs. Amino acid abbreviations: Pen, L-penicillamine; I3Y, 3-iodo-L-tyrosine; y, D-Tyr; r, D-Arg; β3hY, β3-homo tyrosine. The C-terminus of each peptide depicted in this table is a free carboxyl group;

b

Data was collected in Ca2+ containing ND-96 buffer. Concentration-response curves and the Hill slope values are shown in Figure S7 and Table S2.