IndraLab

Statements

Pimozide inhibits KCNH2. 13 / 25
5 3 4 | 13
reach
"To confirm whether pimozide inhibits hERG channels from within the cells, we also investigated changes in hERG currents using a patch-clamp technique.Pimozide and elacridar were purchased from Santa C[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
36181876
reach
"To investigate whether or not pimozide inhibits hERG channels inside the cells, pimozide was dissolved in the intracellular solution at concentrations of 2, 10, and 100 nM."
36181876
reach
"20 , 21 However, a specific report on the mode of hERG channel inhibition by pimozide from within the cell is lacking."
36181876
reach
"These results suggest that pimozide inhibits the hERG channel from within the cell."
36181876
reach
"If pimozide inhibits hERG channels from inside the cell, then coexisting P-gp inhibitors may increase the risk of QT prolongation by increasing the uptake of pimozide into cardiomyocytes and enhancing[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
36181876
reach
"Subsequent studies have generally agreed with this conclusion.As well as the effects noted above, pimozide also displays actions as an antagonist, inverse agonist, and channel blocker, with relatively lower affinities, at α-adrenergic, muscarinic cholinergic, and histamine receptors and calcium and sodium channels.Like many other antipsychotics, but more strongly than most, pimozide also inhibits the hERG (human ether-a-go-go-related) K+ channel [28]."
36552037
reach
"Pimozide also inhibits hERG (human Ether-a-go-go-related) K + -Channel (Kongsamut et al., 2002)."
29958636
reach
"In this investigation, four out of nine hearts developed arrhythmia under hypokalemic conditions, thus supporting the notion that hypokalemia is indeed a risk factor for developing arrhythmia.In addit[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
16507347
reach
"The IC 50 value for pimozide block of peak HERG tail currents measured 18.1 nM (13.7-23.9 nM, 95% C.L., Fig. 1B)."
10762666
reach
"These results suggest that pimozide inhibits HERG with high affinity and is selective for this channel relative to other human cardiac K + channels.Pimozide has been shown to prolong the QT interval a[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
10762666
reach
"Pimozide and sertindole, for example, have previously been shown to block HERG in the low nanomolar range (Rampe et al., 1998; Kang et al., 2000)."
12176106
reach
"However, with up to 5 muM testosterone and up to 12 hr of incubation, enough oocytes with acceptable membrane properties (input resistance of no less than 2 x 10 5 Omega at -80 mV) were available.Appl[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
11377395
reach
"The IC 50 values for these compounds generally varied by about three-fold when compared between the two laboratories ( Table 2 b), with the exception of the potent HERG blocker pimozide where an appro[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
16843688