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. 2020 Dec 9;11(6):1412–1433. doi: 10.1016/j.apsb.2020.12.003

Table 2.

Pharmacology of CaCC ANO1/TMEM16A Activators.

Activator Structure EC50 (μmol/L) Test assay Selectivity Effect Ref.
Eact Image 25 3 hANO1-FRT TRPV1 (+)
TRPV4 (+)
[Ca2+]i (+)
ANO6 (+)
Pain,
Smooth muscle
contraction
66,109, 110, 111
Fact Image 26 6 hANO1-FRT NR NR 109
INO-4995 Image 27 NR hANO1-HEK293 NR NR 112
Resveratrol Image 28 48 mANO1-HEK293T NR Smooth muscle
contraction
113
GRb1 Image 29 38.4 mANO1-HEK293 NR Smooth muscle
contraction
114
Cinnamaldehyde Image 30 9.7 ANO1-HEK293 NR Smooth muscle
contraction
66
Chitosan oligosaccharides Image 31 74.5 μg/mL mANO1-HEK293 NR Smooth muscle
contraction
115
ETX001 NR 116 nmol/L hANO1-FRT
sANO1-CHO
[Ca2+]i (/) Anti-CF 116
Melittin C131H229N39O31 0.5–2 hANO1-HEK293 ANO6 (+)
PLA2 (+)
Phospholipid
scrambling
through ANO6 but
not ANO1
66,117

+, activation effect; /, no effect; NR, no report.