Table 2.

Antagonist activity of N-acyl amides at TRPV1-4.

Antagonist activity
N-acyl amides (10 μ M mixtures)	TRPV1 (+ CAP)	TRPV2 (+ 2-APB)	TRPV3 (+ 2-APB)	TRPV4 (+ 4α-PDD)
N-acyl alanine	155.12 ± 10.33	267.43 ± 14.53	74.55 ± 4.34	87.46 ± 8.03
N-acyl aspartic acid	187.20 ± 11.78	251.09 ± 12.01	65.74 ± 13.38	83.25 ± 8.34
N-acyl beta-alanine	166.84 ± 13.52	239.05 ± 25.01	92.69 ± 9.95	91.59 ± 5.26
N-acyl GABA	87.22 ± 11.12	277.24 ± 22.89	163.03 ± 15.23	94.24 ± 5.71
N-acyl glycine	151.43 ± 10.3	255.01 ± 16.16	123.01 ± 10.80	85.11 ± 7.15
N-acyl isoleucine	185.08 ± 5.76	285.96 ± 30.44	62.73 ± 3.80	97.22 ± 5.46
N-acyl leucine	179.18 ± 13.56	235.66 ± 22.26	51.37 ± 3.10	80.25 ± 6.18
N-acyl methionine	158.93 ± 14.24	237.28 ± 18.32	65.15 ± 5.74	91.50 ± 9.87
N-acyl phenylalanine	180.70 ± 10.01	260.15 ± 28.61	75.64 ± 22.64	81.56 ± 4.54
N-acyl proline	95.98 ± 21.26	−34.61 ± 26.70	142.49 ± 6.48	94.16 ± 11.34
N-acyl serine	196.28 ± 6.53	234.06 ± 22.36	69.65 ± 5.10	94.83 ± 5.23
N-acyl threonine	197.53 ± 7.51	210.15 ± 17.10	81.18 ± 5.96	83.89 ± 7.96
N-acyl tryptophan	201.35 ± 3.26	263.71 ± 24.69	61.91 ± 6.13	−99.49 ± 38.83
N-acyl tyrosine	156.56 ± 15.15	−116.42 ± 13.94	58.78 ± 5.40	−124.36 ±, 22.53
N-acyl valine	174.62 ± 11.94	240.61 ± 26.79	39.73 ± 4.16	37.05 ± 7.37
DMSO	195.69 ± 16.42	253.67 ± 39.42	95.73 ± 7.01	93.92 ± 11.55
I-RTX (20 nM)	−22.15 ± 5.80
Rethenium red (30 μM)		64.83 ± 4.51	41.33 ± 3.75	−85.52 ±, 34.61

Far left column lists the N-acyl amide family or control compound that was used as the pre-incubated compounds for each screen. Challenge compounds are listed under the title of the TRPV-HEK expression system. Values shown are the data from the change in relative fluorescence units of Fura2AM from the 30 s baseline and represent the area of the curve of analysis of 190 s post injection of the positive control challenge compound. Those values in bold black are significantly different from those of the vehicle injection p ≤ 0.01.