L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, which is more than 280-fold more selective than other growth inhibitory receptors.L-803087 induced AMPA-mediated synaptic responses in the hippocampus in vitro, and in vivo increased seizures in alginate-induced seizure-busting mice.

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

L-803087对克隆人类sst1、sst2、sst3和sst5受体的Ki值分别为199、4720、1280和3880 nM[2]。L-803087具有与药效团上赖氨酸对应的二胺部分。然而，L-803087与药效团的芳香族和Trp取代基之间的关系并不明显。L-803087不抑制生长激素、胰岛素或胰高血糖素的分泌[2]。

在野生型小鼠中，L-803087（5 nmol）的给药平均使癫痫活动翻倍。有趣的是，这种效应被3 nmol Octreotide所阻断。在野生型小鼠海马切片中，Octreotide（2 μM）并不改变AMPA介导的突触反应，而L-803087（2 μM）的添加则会导致这种反应的增强[1]。