1786412-46-1
1786412-46-1 structure
- Name: L-803,087 trifluoroacetate
- Chemical Name: L-803087 TFA
- CAS Number: 1786412-46-1
- Molecular Formula: C27H30F5N5O5
- Molecular Weight: 599.55
- Catalog: Signaling Pathways GPCR/G Protein Somatostatin Receptor
- Create Date: 2020-08-07 16:24:37
- Modify Date: 2024-01-22 14:34:47
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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].
| Name | L-803087 TFA |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
Ki: 0.7 nM (sst4 receptor), 199 nM (sst1 receptor), 4720 nM (sst2 receptor), 1280 nM (sst3 receptor) and 3880 nM (sst5 receptor)[1] |
| In Vitro | L-803087 has Ki values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively[1]. 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[1]. |
| 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 |
| Molecular Formula | C27H30F5N5O5 |
|---|---|
| Molecular Weight | 599.55 |