"Remarkably, however, this single atom alteration in each of the KCNQ3 * subunits entirely abolishes retigabine activation of KCNQ3 * channels (XREF_FIG)."
"Retigabine activates mainly heteromeric Kv7.2 and Kv7.3 channels and as a result causes changes in resting membrane potential towards more negative levels (ie hyperpolarization)."
"Retigabine potentiation of KCNQ3 * channels was retained with F 3 -Trp substitution at Trp265 (XREF_FIG), a substitution that still potently diminishes the negative electrostatic potential on the face of the side chain (XREF_FIG), indicating that a cation-pi interaction of Trp265 with retigabine or some other entity (perhaps another channel residue) is not required for retigabine effects."
"The M-type current was activated by 1) 10 muM retigabine, an opener of all KCNQ channels except KCNQ1, 2) 10 muM zinc pyrithione, which augments all KCNQ channels except KCNQ3, and 3) 50 muM N-ethylmaleimide, which activates KCNQ2, KCNQ4, and KCNQ5, but not KCNQ1 or KCNQ3, channels."
"Recently, Wickenden et al. (2001) have also shown that retigabine can activate the KCNQ5 and KCNQ3 heteromer expressed in CHO cells."
"Moreover, KCNQ3 and KCNQ5 channels are potently activated by the anticonvulsant retigabine (Wickenden et al., 2001)."
No evidence text available