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. Author manuscript; available in PMC: 2014 Feb 1.
Published in final edited form as: J Cardiovasc Pharmacol. 2013 Feb;61(2):113–119. doi: 10.1097/FJC.0b013e318279ba42

Table 2. Data summary for TRPV4 antagonists (a).

Antagonist Potency
(IC50, μM)
Species Cross-reactivity
RN-1734 2.3
5.9
3.2
human
mouse
rat
---
RN-9893 <0.12
<0.06
<0.12
human
mouse
rat
---
HC-067047 0.048
0.017
0.133
human
mouse
rat
inhibits TRPM8, HERG
at submicromolar
Ruthenium Red <0.086-1
<0.21-1
<0.2-0.33
human
mouse
rat
inhibits all TRPVs,
TRPM6, TRPM8,
TRPA1, RyR1-3
Capsazepine 18.6
13.5
human
rat
Inhibits TRPV1, TRPM8
Citral 32 mouse Inhibits TRPA1,
activates TRPV1,
TRPV3, TRPM8
(a)

modified from 89, 90