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Table 3
In vitro functional potencies of selected tetrahydroquinoline TRPV1 antagonists in human TRPV1 Ca+ influx assay and their CYP3A4 inhibition
R2
O
N
8
HN
N
H
R1
5
7
N
6
N
H
a
Compd
R1
R2
hTRPV1 IC50 (nM)
CYP3A4 % inhibitionb
11a
11b
11c
11d
11e
11f
11g
11h
11i
H
7-F
Methyl
Methyl
Methyl
Methyl
Methyl
Methyl
Methyl
Benzyl
Benzyl
Benzyl
Benzyl
215
34
7
65
66
47
7-CF3
8-tBu
7-tBu
6-tBu
6-OMe
H
6
115
853
1380
70
59
94
6-F
66
11j
11k
11l
6-tBu
6-OMe
6-OMe
8-Cl
121
160
196
11
97
93
Cyclohexylmethyl
3-Methylbutyl
11m
a
All values are means SEM of at least three separate experiments.
At 10 lM.
b
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