Chemical Name: N2-[4-(5,7-Difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-L-arginine methyl ester trifluoroacetate
Biological ActivityL-803,087 trifluoroacetate is a potent and selective somatostatin sst4 receptor agonist. Ki values are 0.7, 199, 4720, 1280 and 3880 nM for cloned human sst4, sst1, sst2, sst3 and sst5 receptors respectively. Facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice in vivo.
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Identification and characterization of subtype selective somatostatin receptor agonists.
Rohrer and Schaeffer
Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
Rohrer et al.
Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice.
Moneta et al.
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