| Identification | Back Directory | [Name]
N2-[4-(5,7-DIFLUORO-2-PHENYL-1H-INDOL-3-YL)-1-OXOBUTYL]-L-ARGININE METHYL ESTER TRIFLUOROACETATE | [CAS]
1786412-46-1 | [Synonyms]
L-803087 TFA | [Molecular Formula]
C27H30F5N5O5 | [MDL Number]
MFCD09037334 | [MOL File]
1786412-46-1.mol | [Molecular Weight]
599.55 |
| Hazard Information | Back Directory | [Uses]
L-803087 TFA is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 TFA is >280-fold more selective for sst4 receptor than other somatostatin receptors. L-803087 TFA facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2]. | [in vivo]
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)[2]. | [References]
[1] Rohrer SP, et al. Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40. DOI:10.1126/science.282.5389.737
[2] Moneta D, et al. Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice. Eur J Neurosci. 2002 Sep;16(5):843-9. DOI:10.1046/j.1460-9568.2002.02146.x |
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