产品描述
L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM, which is >280-fold higher than other somatostatin receptors.
体外活性
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 has Ki values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively.
体内活性
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).
Cas No.
217480-26-7
分子式
C25H29F2N5O3
分子量
485.53
别名
L-803087
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
