CBiPES is a selective positive allosteric modulator of the metabotropic glutamate receptor group II subtype mGluR2. CBiPES attenuated a stress-induced hyperthermia and PCP-induced hyperlocomotor activity in the mouse model.

LY-300168 (GYKI-53655) is a negative allosteric AMPA modulator. It is used as a tool compound to study role of AMPA receptor in CNS functioning. Administration of LY-300168 demonstrated anxyolitic effects. GYKI-53655 produced a dose-dependent prolongation of survival time in the MgCl2 induced global ischaemia model.

LY-367385, a potent and selective antagonist of metabotropic glutamate 1a receptor (mGlu1a), which attenuated infarct size after transient focal cerebral ischemia.

LY235959 is the active isomer of the 6-substituted decahydroisoquinoline-3-carboxylic acid, LY274614. Both LY274614 and LY235959 have demonstrated potent NMDA receptor antagonist activity both in vivo and in-vitro. LY235959 has been shown to attenuate and reverse morphine tolerance as well as, attenuate opioid withdrawal and block c-fos mRNA induction in limbic areas. The attenuation of morphine tolerance occurs through the interaction of LY235959 with the NMDA receptor and not by producing opiate receptor changes. LY235959 is able to block NMDA receptor-induced hyperalgesia, as well as formalin-induced inflammatory pain, in rats. These antinociceptive effects of LY235959 were obtained at doses that did not produce motor impairment. LY235959 does not block the hyperalgesia produced by kainic acid (a non-NMDA glutamate receptor agonist) providing evidence of its selectivity for the NMDA receptor.

LY-320135 is a substituted benzofuran which is structurally distinct from the aminoalkylindole and pyrazole type cannabinoid antagonists, AM630 and SR141716A, respectively. LY-320135 is a potent and selective canniboid CB1 receptor antagonist/inverse agonist. LY-320135 is selective (~70 fold) over canniboid CB2 receptors. LY-320135 is widely used in research, particularly for elucidating the mechanisms by which many CB1 antagonists act as inverse agonists at higher doses. LY-320135 shows weak binding to both 5-HT2 (Ki = 6.4 uM) and muscarinic receptors (Ki = 2.1 uM).

LY294002 is a morpholine-containing chemical compound that is a potent inhibitor of numerous proteins, and a strong inhibitor of phosphoinositide 3-kinases (PI3Ks). It was previously under active development by Eli Lily and was tested in a number of clinical cancer trials including neuroblastomas and head and neck cancer. However, commercialization efforts have been discontinued, and LY294002 is now predominantly used as a research tool.

LY404187 (or LY-404,187) is a selective, potent and centrally active positive allosteric modulator of AMPA receptors. LY404187 preferentially acts at recombinant human homomeric GluR2 and GluR4 versus GluR1 and GluR3 AMPA receptors. This drug, developed by Eli Lilly and Company, is a member of biarylpropylsulfonamides. LY404187 has been shown to enhance performance in animal models of cognitive function requiring different mnemonic processes and may be therapeutically beneficial for treating cognitive deficits in a variety of disorders, particularly those that are associated with reduced glutamatergic signaling such as schizophrenia. In addition, LY404187 has been demonstrated to be efficacious in animal models of behavioral despair that possess considerable predictive validity for antidepressant activity and Parkinson's disease.

LY344864 is a selective 5-HT1F receptor agonist (EC50 = 3 nM). In a rat model of migraine, LY344864 inhibited neurogenic dural inflammation following i.v. and oral administration.

LY2033298 is a selective allosteric modulator for muscarinic acetylcholine M4 receptor. It exerts antipsychotic action in animal models. The compound is able to modulate circadian activity rhythms and morphine-induced conditioned place preference in rats.

LY94939 was discovered as a result of efforts to develop agents that inhibit the uptake of 5-HT from the synaptic cleft. A selected analogue of LY94939, the compound LY82816 (3-p-trifluoromethyl-phenoxyN-methyl-3-phenylpropylamine oxalate or (fluoxetine oxalate), which was a secondary amine (later named as fluoxetine oxalate), and its primary amine or N-demethylated compound (later named as norfluoxetine), were the most potent inhibitors of [3 H]-5-HT uptake in nerve endings, with Ki values of 0.07 uM. The first salt form of fluoxetine tested in serotonin reuptake assays in the early 1970s was the oxalate salt (LY82816); however, the marketed version is the hydrochloride salt (fluoxetine hydrochloride (LY110140), or Prozac.