Table 1.

Effect of compounds 4a-4h, 4o, 5a-5c, 9a, 14a-14h on TRPC6 channels

Compd	R1	R2	R3	TRPC6 IC50(?M)a
4a	MeNHCS	F	H	>130
4b	MeCO	F	H	>130
4c	Me(CH2)7CH=CH(CH2)7CO	F	H	NA
4d	BocNH(CH2)2CO	F	H	NA
4e		F	H	NA
4f		F	H	~100
4g	Ph2CHCO	F	H	~100
4h		F	H	NA
4o	EtOCO	F	H	4.7 ± 0.03b
5a	Boc	F	H	8.4 ± 1.1
5b	Boc	Cl	H	NA
5c	Boc	CF3	H	NA
14a	EtOCO	CF3	Me	1.0 ± 0.3
14b	Boc	NO2	Me	agonistc
14c		F	Me	NA
14d		F	Me	NA
14e		F	Me	NA
14f		F	Me	NA
14g		F	Me	NA

^aEffects on TRPC6 or IC₅₀ against activation by 10 μM 4o, estimated based on one experiment with triplicates.

^bEC₅₀ determined based on Ca²⁺ assay.

^cEC₅₀ cannot be accurately determined because of the self-fluorescence of the compound, NA: No activity.