Terfenadine is a potent open-channel blocker of hERG with a mean IC50 of 204 nM.
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Terfenadine is a potent open-channel blocker of hERG with a mean IC50 of 204 nM[3]. Terfenadine inhibited Kir2.3 channels with a strikingly greater potency (IC50 = 1.06 ± 0.11 μmol L-1) compared to Kir2.1 channels (IC50 = 27.8 ± 4.8 μmol L-1). The Kir2.3(I213L) mutant, possessing a larger affinity for phosphatidylinositol 4,5-bisphosphate (PIP2) than the wild-type Kir2.3, was less sensitive to terfenadine inhibition (IC50 = 13.0 ± 2.9 μmol L-1). Additionally, the PIP2 intracellular application had largely reduced the inhibition of Kir2.1 channels by terfenadine[4]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca(2+) homeostasis. Terfenadine induced autophagy, that can promote apoptosis[5]. Terfenadine combined with EPI (epirubicin) synergistically inhibits the growth and metastatic processes of resistant cells both in vitro and in vivo[6].
United States, Utah
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George E Wahlen VA Medical Center
Recruiting
Salt Lake City, Utah, United States, 84132
Contact: Russell Richardson, Ph.D. 801-582-1565 r.richardson@hsc.utah.edu
Contact: Ashley Nelson, MD 801-582-1565 ext 4127 ash.nelson@hsc.utah.edu 收起 <<
United States, Utah
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George E Wahlen VA Medical Center
Recruiting
Salt Lake City, Utah, United States, 84132
Contact: Russell Richardson, Ph.D. 801-582-1565 r.richardson@hsc.utah.edu
Contact: Ashley Nelson, MD 801-582-1565 ext 4127 ash.nelson@hsc.utah.edu 收起 <<
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Koganei-Shi, Japan
Investigational Site Number 392003
Osaka-Shi, Japan
Investigational Site Number 392001
Shinjuku-Ku, Japan 收起 <<
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GSK Investigational Site
Austin, Texas, United States, 78731
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Austin, Texas, United States, 78750
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Kerrville, Texas, United States, 78028
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New Braunfels, Texas, United States, 78130
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San Antonio, Texas, United States, 78205
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North Carolina Clinical and Translational Research Center
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Madrid, Spain, 28046
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Madrid, Spain, 28050
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Silicon Valley Gastroenterology 2490 Hospital Dr. Suite 211
Recruiting
Mountain View, California, United States, 94040
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