Sergolexole [LY 281067] is an ergoline ester similar in structure to amesergide [LY 237733], with potent and highly selective antagonist activity at serotonin 2. The preclinical pharmacologic activity of LY 281067 shows it to be a potent and highly selective serotonergic (5-HT2) receptor antagonist. Based upon binding studies with 5-HT2 receptors in brain cortical membranes and block of 5-HT-induced contractions in the rat jugular vein, LY 281067 showed high affinity at 5-HT2 receptors with a dissociation constant of approximately 1 nM. LY 281067 was a highly selective 5-HT2 receptor antagonist without appreciably binding to 5-HT1, D1 or D2 receptors or interacting with histamine (H1), cholinergic, beta adrenergic or alpha-1 adrenergic receptors in smooth muscle. LY 281067 had modest affinity at alpha-2 receptors with a dissociation constant of approximately 100 nM. Oral bioavailability of LY 281067 in spontaneously hypertensive rats was excellent with an oral to i.v. dose ratio approximating 4. Sergolexole was undergoing phase II clinical trials with Eli Lilly in the USA as a potential treatment for migraine and anxiety, but development of this compound, but development of this compound has been discontinued.

TGF-B-recpotor inhibitor (dihydropyrrolopyrazole, 13) is one of the series of optimized, bioavailable dihydropyrrolopyrazole TGF-beta receptor type I inhibitors synthesized at Ely Lilly and is an investigational antitumor agent.

TGF-B-recpotor inhibitor (dihydropyrrolopyrazole, 13) is one of the series of optimized, bioavailable dihydropyrrolopyrazole TGF-beta receptor type I inhibitors synthesized at Ely Lilly and is an investigational antitumor agent.

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.

N-(4-(2-Methoxyphenoxy)-phenyl-N-(2,2,2-trifluoroethylsulfonyl)-pyrid-3-ylmethylamine (LY487379) is a selective positive allosteric modulator at metabotropic glutamate subtype 2 receptors (mGluR2). The compound exerts antipsychotic and anxiolytic actions.

LY-272015 is an antagonist at serotonin 5-HT2B receptor. LY-272015 exerts antihypertensive action in animal models.

5-(2-Aminopropyl)benzofuran (5-APB) is an empathogenic psychoactive compound of the substituted benzofuran, substituted amphetamine and substituted phenethylamine classes. 5-(2-Aminopropyl)benzofuran is a serotonin–norepinephrine–dopamine reuptake inhibitor and serotonin–norepinephrine–dopamine releasing agent. The toxicity and long-term health effects of recreational 5-APB use do not seem to have been studied in any scientific context and the exact toxic dosage is unknown/ 5-(2-Aminopropyl)benzofuran 's high affinity for the 5-HT2b receptor makes it likely that 5-APB would be cardiotoxic with long-term use, as seen in other 5-HT2B agonists such as fenfluramine and MDMA.

Catharanthine is a terpene indole alkaloid produced by the medicinal plant Catharanthus roseus. Catharanthine is derived from strictosidine, but the exact mechanism by which this happens is currently unknown. Catharanthine is one of the two precursors that form vinblastine, the other being vindoline.

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.

Selective, potent, orally bioavailable full 5-HT1A antagonist. S-(+)-enantiomer of (±)-LY426965 is more active in comparison with its opposite enantiomer (R)-(-)-LY 426965. LY426965 completely reversed the effects of nicotine withdrawal on the auditory startle reflex in rats. In microdialysis experiments, LY426965, when administered with fluoxetine, significantly increased extracellular levels of serotonin above those achievable with fluoxetine alone. In electrophysiological studies, the administration of LY426965 both blocked and reversed the effects of fluoxetine on 5-HT neuronal activity. Preclinical results indicate that LY426965 may have clinical use as a pharmacotherapy for smoking cessation and depression and related disorders.