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. Author manuscript; available in PMC: 2013 Oct 11.

Published in final edited form as: J Med Chem. 2012 Sep 20;55(19):8392–8408. doi: 10.1021/jm300780p

Table 1.

In vitro hTRPV1 Antagonistic Activities for 2-Acylic Amino Derivatives



	R	K_i [CAP] (nM)	IC₅₀ [pH] (nM)		R	K_i [CAP] (nM)	IC₅₀ [pH] (nM)
1		26	NE	21		14	140
2		20	1210	22		15.8	203
3		4.4	NE	23		65.7	414
4		1.2	116	24		WE	WE
12	H	WE	NE	25		NE	NE
13		9.1	293	26		WE	WE
14		20.4	260	27		19.1	2390
15		27.2	1130	28		3.5	148
16		19.3	1140	29		0.2	14.7
17		59.6	1400	30		0.6	10.5
18		39.2	WE	31		0.8	21.3
19		WE	WE	32		0.9	57.4
20		39.3	1160