L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors. L-803087 induces AMPA-mediated synaptic responses in the hippocampus in vitro and increases seizures in alginate-induced seizure-busting mice in vivo.

SST5 receptor:3880 nM (ki), SST3 receptor:1280 nM (ki), SST4 receptor:0.7 nM (ki), SST1 receptor:199 nM (ki), SST2 receptor:4720 nM (ki)

L-803087 has Ki values of 199, 4720, 1280, and 3880 nM for cloned human sst1, sst2, sst3, and sst5 receptors, respectively[2].
The molecule L-803087 features a diamine moiety mapping to lysine on the pharmacophore. However, the relationship of this molecule to the aromatic and Trp substituents of the pharmacophore is not apparent. L-803087 does not inhibit the secretion of growth hormone, insulin, or glucagon[2].

In wild-type mice, the administration of L-803087 (5 nmol) on average doubles seizure activity. 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, whereas facilitation occurs with L-803087 (2 μM)[1].