G protein-insensitive inwardly rectifying K+ channels are
resistant to bupivacaine inhibition. Oocytes were injected with the
cRNA for ROMK1, IRK1, R1G2(118–193), R1G2(97–168), or I1G2(96–189).
(a–d) Current responses were elicited by voltage steps
to +50 and −100 mV (VH = 0 mV) in the
absence and then presence of extracellular bupivacaine (500 μM, pH
7.5). (e) Fractional current remaining
(I/Io) shown for IRK1
(n = 4), ROMK1 (n = 5),
I1G2(96–189) (n = 5), R1G2(118–193)
(n = 5), and R1G2(97–168) (n =
5). (f) Western blot stained with
anti-Gβ G protein antibody. Pull-down assay was used to
measure the Gβ1γ7 binding to a
glutathione S-transferase fusion protein containing the
N- or C-terminal domain of GIRK1 in the absence (c) or
presence (b) of 500 μM bupivacaine.