CGS -21680 is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor. In an isolated perfused working rat heart model, CGS -21680 effectively increases coronary flow with an ED25 value of 1.8 nM. CGS-21680 binds adenosine A2 receptor with high affinity (Kd = 15.5 nM). Novartis originated CGS- 21680 in Switzerland and discontinued its development later.

Saikosaponin D is a triterpene saponin found in Bupleurum that exhibits antioxidative, immunomodulatory, anti-fibrotic, anti-angiogenic, anticancer, and chemopreventive activities. Saikosaponin D increases activity of superoxide dismutase, catalase, and glutathione peroxidase and decreases activity of malondialdehyde in cellular models of oxidative damage. In other in vitro models, saikosaponin D increases secretion of IL-12, maturation of dendritic cells, and proliferation of lymphocytes. Saikosaponin D inhibits SERCA, increasing intracellular Ca2+ and inducing autophagy. In vivo, this compound decreases severity of fibrosis. In embryos, saikosaponin D decreases microvessel formation. Additionally, this compound decreases tumor formation in DEN-treated animal models and suppresses expression of CEBP-β and COX-2. Saikosaponin D also induces apoptosis and activation of caspases 3 and 7 in hepatocellular carcinoma cells. Saikosaponin D is a Glucocorticoid receptor agonist. It is a COX-2 and iNOS inhibitor.

RP-67580 selectively inhibits the binding of substance-P to Neurokinin Receptor-1 and does not show meaningful antagonistic activity against NK2 and NK3. Preclinical trials had been conducted and discontinued in France for the potential treatment of inflammation and pain. RP-67580 has not been used in human trials.

RO 15-4513 is a high-affinity benzodiazepine ligand which acts as a partial inverse agonist at recombinant diazepam-sensitive (DS) benzodiazepine α1-, α2-, α3- and α5-GABAA receptors, developed by Hoffmann–La Roche in the 1980s. Ro 15-4513 reverses the sedating and anticonflict effects of alcohol, and can, therefore, be used as an antidote to the acute impairment caused by alcohol. In non-food or fluid-deprived rats, orally self-administering 10% alcohol in an operant situation, Ro 15-4513 resulted in a dose-dependent suppression of alcohol intake. The use of Ro 15-4513 would appear to be limited by the fact that the compound is proconvulsant. Ro 15-4513 has been found to induce seizures in mice undergoing ethanol withdrawal. However, it is a potentially powerful tool with which to investigate the neuropsychopharmacology of alcohol. Labelling Ro15-4513 with carbon-11 leads to the possibility of its use in PET imaging of the brain. The specificity of the compound to a small number of GABA receptor sub-types leads to the generation, with accurate modeling, of detailed images with well-defined limbic and cortical structures. These images can be useful in quantitatively analyzing conditions such as addiction, that is known to be, at least in part, associated with the GABAergic system.

1-(5-iodonaphthalene-1-sulfonyl)-1H-hexahydro-1,4-diazepine (ML-7) is an inhibitor of myosin light chain kinase (MLCK). It is widely used to study MLCK signaling both in vitro and in vivo.

LY-165163 is a partial agonist of serotonin receptors 5-HT1A and 5-HT1D. It exhibits marked activity at both pre- and postsynaptic dopaminergic D2 (D3 and D1) receptors. LY-165163 caused a significant and dose-dependent hypothermia in rats. As a 5-HT1D receptor agonist, LY-165163 was proposed for the ocular pain treatment.

Сalpeptin is useful cell-penetrative calpain inhibitor. Calpeptin inhibits the cell growth of ER (estrogen receptor) positive breast cancer cells, such as MCF-7, T-47D, and ZR-75-1 in the presence of Estradiol. Studies in rodent and cell culture models of Parkinson's disease suggest that treatment with calpain inhibitor calpeptin can prevent neuronal death and restore functions. The combination of histone deacetylase inhibitors and calpeptin inhibited the growth of two distinctly different types of breast cancer cells and could have wide clinical applications. Calpeptin is a promising antitumor agent for pancreatic cancer.

KN-62 (1-[N,O-Bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazine) is an inhibitor of Ca2+/calmodulin-dependent protein kinase II (Ca2+/CaM kinase II). In addition, it acts as an antagonist of the P2X7 receptor.

Himbacine is a complex piperidine alkaloid isolated from the bark of Galbulimima baccata, a species that belongs to the magnolia family. Himbacine appears to be a potent muscarinic antagonist that displays selectivity for M2 or M4 receptors, as compared to M1 or M3 receptors. Vorapaxar (SCH 530348) is a non-peptide himbacine analogue that has been developed for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction or peripheral arterial disease. Vorapaxar is a platelet inhibitor that potently and selectively inhibits thrombin-mediated platelet activation without interfering with thrombin-mediated cleavage of fibrinogen via antagonism of the platelet proteinase-activated receptor PAR1.

B-HT 958 (2-amino-6-(p-chlorobenzyl)-4H-5,6,7,8-tetrahydrothiazolo[5,4-d]az epine), a compound chemically related to clonidine-like drugs of the azepine type, exerts a strong agonistic effect on brain dopamine autoreceptors. B-HT 958 is a partial agonist at peripheral alpha 2-adrenoceptors. In doses of about 1 mg/kg and with low frequency sympathetic stimulation (less than 6.4 Hz) it acts presynaptically as agonist; in this dose the drug acts postsynaptically mainly as antagonist.