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. Author manuscript; available in PMC: 2018 Jun 8.
Published in final edited form as: J Med Chem. 2017 Apr 28;60(11):4680–4692. doi: 10.1021/acs.jmedchem.7b00304

Table 1.

Structures of Compounds 4a–4p and Their Effects on TRPC6 and TRPC4

graphic file with name nihms922087u2.jpg
Compound R1 R3 R4 TRPC6 EC50(μM)a TRPC4β+MOR IC50(μM)b
4a H F graphic file with name nihms922087t1.jpg 12.3±1.2 ~10
4b Me F graphic file with name nihms922087t2.jpg NA NA
4c Me F graphic file with name nihms922087t3.jpg NA NA
4d Me F graphic file with name nihms922087t4.jpg NA NA
4e Me NO2 graphic file with name nihms922087t5.jpg NA NA
4f Me NO2 graphic file with name nihms922087t6.jpg NA NA
4g Me NO2 CO2Et ~8c NA
4h Me F Boc NA NA
4i H NO2 CO2Et ~2c NA
4j H F graphic file with name nihms922087t3.jpg 28.8±8.3 ~35
4k H F graphic file with name nihms922087t4.jpg NA NA
41 H Cl Boc NA NA
4m H Cl Cbz 7.79±0.05 NA
4n H CF3 CO2Et 1.39±0.01 NA
4o H F CO2Et 4.66±0.03 NA
4p H F Cbz 3.91±0.02 NA
a

EC50 determined based on Ca2+ assay.

b

IC50 against that activated by 1 μM DAMGO, estimated based on one experiment with triplicates;

c

Estimated value because of the self-fluorescence of the compound.

NA: No activity.