(R)-Etifoxine is an isomer, chemically isolated from Etifoxine (Stresam), an approved racemic drug (off patent) prescribed in Europe. (R)-Etifoxine was developed by Xytis Inc for treatment pain, mental disease, and central nervous system disorders. However future development has been discontinued.

GW0742, also known as GW610742, is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. GW0742 treatment has a prominent anti-inflammatory effect in 5XFAD mice and suggests that PPARδ agonists may have therapeutic utility in treating AD. GW0742 has the ability to improve glucose homeostasis in diabetic rats through activation of PPAR-δ. Therefore, PPAR-δ is a good target for the development of antidiabetic drugs in the future.

S-fluoxetine is an enantiomer of fluoxetine, a potent and selective inhibitor of the neuronal serotonin-uptake carrier and a clinically effective antidepressant. R-fluoxetine and S-fluoxetine enantiomers are nearly equipotent at blocking serotonin reuptake. In all biochemical and pharmacological studies, the eudismic ratio for the fluoxetine enantiomers is also near unity. A study examining the relative contributions of CYP enzymes to the metabolism of S-fluoxetine, and R-fluoxetine found dramatic differences. These data led to discovery programs between Lilly and Sepracor for the individual enantiomers. S-fluoxetine was studied in a phase 2 clinical trial for the prophylaxis of migraine, however, development was discontinued.

AK-7 is a brain penetrant selective SIRT2 inhibitor. AK-7 exerts neuroprotective properties in vitro and in vivo models of neurodegenerative diseases (Huntington’s, Parkinson’s and Alzheimer’s disease).

MG-132, also known as carbobenzoxy-Leu-Leu-leucinal, is a peptide aldehyde, which effectively blocks the proteolytic activity of the 26S proteasome complex. It also strongly inhibited calpain activity in vitro. MG-132 is used as a tool for perturbing the proteasome-regulated degradation of intracellular proteins.

Psoralidin (1) was first isolated from seeds of Psoralea corylifolia Linn. It was found to be an active ingredient of many Indian and Chinese traditional herbal medicines. Psoralidin exhibits a variety of biological activities like antineoplastic, antioxidant, antibacterial, antidepressant activities. Psoralidin inhibits protein tyrosine phosphatase 1B activity. Psoralidin may act as a estrogen receptor agonist. In addition psoralidin showed potent and noncompetitive inhibition against UDP- glucuronosyltransferase (UGT) or cytochrome p450 (CYP450) enzymes.

Sophoridine is a quinolizidine alkaloid isolated from traditional Chinese herbs, which exists in the stems and leafs of Leguminous plant Sophora alopecuroides L., Euchresta japonica Benth., and the roots of Sophora alopecuroides Ait. Sophoridine-induced synchronous oscillations in the hippocampus could elicit the generation and development of seizure. Accumulating evidence demonstrates remarkable pharmacological effects of Sophoridine, including anti-inflammatory, anti-virus and anti-cancer effects. Sophoridine is promising to be a novel, potent and selective antitumor drug candidate for pancreatic cancer. It was shown that sophoridine is able to suppress hepatocellular carcinoma in vitro and vivo. Sophoridine dose- and time-dependently blocks the RANKL-induced osteoclasts formation and the activation of ERK and c-Fos as well as the induction and nucleus translocation of NFATc1.

NNC 63-0532 is a potent non-peptide agonist for the KOR-3 (NOP receptor) (EC50 = 305 nM, Ki = 7.3 nM); about a 12-fold increase in selectivity over other receptors. NNC 63-0532 is an nociceptoid drug used in scientific research.

PD 176252 is a competitive antagonist of neuromedin-B preferring (BB1) and gastrin-releasing peptide preferring (BB2) receptors. PD176252 inhibited tumor growtn in preclinical model of lung cancer, and exhibited synergy with EGFR inhibitor in the model of head and neck cancer. PD176252 demonstrated anxiolytic properties in preclinical models.

PD 173212 is a potent, selective N-type voltage-gated Ca2+ channel blocker (IC50 = 36 nM), it possesses selectivity for non L-type Ca ÷2 channels versus neuronal Na ÷, K ÷, and L-type Ca ÷2 channels. PD 173212 demonstrated potent in vitro activity in the IMR-32 assay as well as in electrophysiology, and it was efficacious in the audiogenic seizure mouse model.