| 中文名称 | N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE |
|---|---|
| 中文同义词 | |
| 英文名称 | N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE |
| 英文同义词 | L-803087 TFA |
| CAS号 | 1786412-46-1 |
| 分子式 | C27H30F5N5O5 |
| 分子量 | 599.549616 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1786412-46-1.mol |
| 结构式 | ![N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE 结构式](CAS/20180601/GIF/1786412-46-1.gif) |
N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE 性质
N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE 用途与合成方法
Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor)
L-803087 has
K
i
values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively.
L-803087 has a diamine moiety that maps to lysine on the phmacophore, but relation of this molecule to the aromatic and the Trp substituents of the phmacophore are not obvious. L-803087 does not inhibit secretion of growth hormone, insulin, or glucagon.
L-803087 (5 nmol) is doubled seizure activity in wild-type mice on average. Interestingly, this effect is blocked by 3 nmol Octreotide. In hippocampal slices from wild-type mice, Octreotide (2 μM) does not modify AMPA-mediated synaptic responses while facilitation occurred with L-803087 (2 μM).