PNU-142633 is selective 5HT1D partial agonist, developed by Pharmacia & Upjohn, Inc. It failed in phase II clinical trials against acute migraine, and its development was discontinued.

GW-9508 is a small-molecule agonist of the fatty acid receptors GPR40 and GPR120. GW-9508 exerts wide-range activity in animal models: anti-depressant, anti-inflammatory, anti-diabetic and analgetic actions.

E-2012 is a gamma secretase modulator that is being evaluated as a potential new treatment for Alzheimer's disease. E-2012, a new chemical entity discovered by Eisai, has shown some potential in non-clinical studies to reduce the production of beta-amyloid Abeta 40/42 by modulating the function of gamma-secretase without interfering with the Notch-processing.

(R)-SKF-83959 (MCL 202) is enantiomer of D1 receptor agonist SKF-83959. (R)-SKF-83959 is reported to be a functionally selective dopamine D1 and D5 receptors ligand with much lower affinity to dopamine D2 and D3 receptors. (R)-SKF-83959 like SKF-83959, produced dose related effects on overt behavior (eye blinking) and schedule-controlled performance in squirrel monkeys. (R)-SKF-83959 increases in eye blinking and decreases in rates of fixed-ratio responding. In contrast to the effects of its S-(-) enantiomer, was relatively devoid of behavioral activity up to doses that were approximately 10-fold greater than (R)-SKF-83959. Pretreatment with the selective D1- like receptor antagonist SCH 39166 dose-dependently antagonized increases in eye blinking produced by (R)-SKF-83959, confirming the involvement of D1 mechanisms in its effects.

N-(1-amino-3,3-dimethyl-1-oxobutan-2-yl)-1-(4-fluorobenzyl)-1H-indazole-3-carboxamide [ADB-FUBINACA] is a synthetic cannabinoid, a Schedule I drug. ADB-FUBINACA acts as a high potency agonist of cannabinoid CB1 receptor. The compound considered to be a component of illicit smoking mixtures "spice".

4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862) is an 1-arylpyrazole class of sigma-1 receptor antagonist. Formalin-induced nociception (both phases), capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity were dose-dependently inhibited by systemic administration of S1RA. Occupancy of sigma-1 receptors in the CNS was significantly correlated with the antinociceptive effects. As a mechanistic correlate, electrophysiological recordings demonstrated that pharmacological antagonism of sigma-1 receptors attenuated the wind-up responses in spinal cords sensitized by repetitive nociceptive stimulation. Esteve is developing E 52862 for the treatment of several pain indications, including diabetic neuropathies, chemotherapy-induced neuropathic pain, postherpetic neuralgia, postoperative pain. Phase II development of this first-in-class agent is underway in Romania, Spain and Greece.

Tetrahydro-4-Methylene-2-octyl-5-oxo-3-furancarboxylic acid or C75 is an inhibitor of fatty acid synthase. Additionally, C75 increased fatty acid oxidation and ATP levels by increasing carnitine palmitoyltransferase I (CPT I) activity. Unlike the activation produced by C75, the CoA derivative is a potent competitive inhibitor that binds tightly but reversibly to CPT I. C75 exerts antitumor and anti-obese potential. C75 has two enantiomers: (-)-C75 inhibits FAS activity in vitro and has a cytotoxic effect on tumor cell lines, without affecting food consumption, (+)-C75 inhibits CPT1 and its administration produces anorexia, suggesting that central inhibition of CPT1 is essential for the anorectic effect of C75.

Tubacin is a highly potent and selective, reversible, cell-permeable inhibitor of HDAC6 with an IC50 value of 4 nM. Tubacin inhibits α- tubulin deacetylation in mammalian cells. Tubacin is specific for the tubulin deacetylase activity of HDAC6. The effects of tubacin has been studied in hematologic malignancies, such as multiple myeloma and leukemia cell lines. Overexpression of HDAC6 in primary lymphocytes and T cell lines increase cell migration in response to cytokines. Knockdown of HDAC6 in T cells decreased chemotactic mobility independent of its enzymatic activity. Furthermore, treatment of multiple myeloma cells with tubacin resulted in decreased cell growth at an IC50 of 2–5uM. In terms of toxicity to normal bone marrow and blood cells, treatment of peripheral blood mononuclear cells (PBMC) and bone marrow progenitor cells (BMPC) with tubacin (5uM) for 12 hours showed that constitutive expression of HDAC6 is higher in BMPCs than PBMCs. Furthermore, acetylation of α-tubulin was markedly enhanced by tubacin in BMPCs but not in PBMCs. Bortezomib and tubacin together induced synergistic antitumor activity in multiple myeloma cells and primary bone marrow plasma cells. Published data therefore provide support for combined therapy in clinical trials for patients with multiple myeloma.

Gomisin N is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. In vitro assays demonstrated that Gomisin N could inhibit TGF-β induced epithelial-mesenchymal transition of 4T1 cells and of primary human breast cancer cells. Gomisin N could maintain membrane stability of rat hepatocytes under oxidative stress. Gomisin N can reduce inflammation, inhibit apoptosis, and improve cardiac function after ischemic injury. It represents a potential novel therapeutic approach for treatment of ischemic heart disease. Gomisin N produced beneficial sedative and hypnotic bioactivity, which might be mediated by the modification of the serotonergic and GABAergic system.

A-834735 is a drug developed by Abbott Laboratories, acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors.