N-oleoyldopamine is an endogenous lipid compound found in the mammalian brain. It has been found to be a capsaicin receptor (TRPV1) agonist. Activation of the capsaicin receptor induces glutamate release and paraventricular nucleus postsynaptic firing. N-oleoyldopamine has been reported to induce the influx of calcium in TRPV1-transfected HEK293 human embryonic kidney cells.

The potent, selective and orally active GPR119 agonist discovered at Arena Pharmaceuticals, Inc., AR231453 significantly increased insulin release in HIT-T15 cells (a hamster insulinoma-derived line with robust GPR119 expression) and in rodent islets. By contrast, no effect of this compound could be seen in islets isolated from GPR119-deficient mice, confirming that its effects were indeed mediated by GPR119.

A-844606 is a selective α7 nicotinic acetylcholine receptor (nAChR) partial agonist (EC50 values are 1.4 and 2.2 μM at human and rat receptors respectively). Displays no measurable effect on α4β2 nAChRs. Stimulates α7 nAChR-induced ERK1/2 phosphorylation in PC12 cells. A-844606 is being investigated as the drug potentially usefull in the treatment of cognition disorders.

A-796260 is a compound that acts as a potent and selective cannabinoid CB2 receptor agonist. The analgesic effects of A-796260 on activity-induced pain behavior were evaluated in a rat model, the results demonstrated that A-796260 may be a useful new pharmacological compound for further studying CB2 receptor pharmacology and for evaluating its role in the modulation of pain.

A-769662 stimulates partially purified rat liver AMPK with EC50 with 0.8 uM. A-769662 activates AMPK purified from multiple tissues and species in a dose-responsive manner with modest variations in observed EC50s. EC50s determined for A-769662 using partially purified AMPK extracts from rat heart, rat muscle, or human embryonic kidney cells (HEKs) are 2.2 uM, 1.9 uM, or 1.1 uM, respectively. A 4 hours treatment of primary rat hepatocytes with A-769662 dose-dependently increases ACC phosphorylation, which correlated inhibition of fatty acid synthesis with IC50 of 3.2 uM. A-769662 also inhibits fatty acid sythesis in mouse hepatocytes with IC50 with 3.6 uM. A-769662 activates AMPK both allosterically and by inhibiting dephosphorylation of AMPK on Thr-172, similar to the effects of AMP. A-769662 inhibits proteasomal function by an AMPK-independent mechanism. A-769662 affects the in vitro activity of purified 26S proteasomes but not the in vitro activity of purified 20S proteasomes. A-769662 has toxic effects on MEF cells. A recent research shows A-769662 inhibited cell proliferation and DNA synthesis.

Racemic phenibut (beta-phenyl-gamma-aminobutyric acid or 4-amino-3-phenylbutyric acid) is a neuropsychotropic drug that was discovered and introduced into clinical practice in Russia in the 1960s. In pharmacological tests of locomotor activity, antidepressant and pain effects, S-phenibut was inactive. In contrast, R-phenibut turned out to be two times more potent than racemic phenibut in most of the tests. Racemic phenibut and R-phenibut demonstrated an affinity for GABAB receptors, in contrast, S-phenibut was not able to bind receptors. Pharmacological activity of racemic phenibut relies on R-phenibut and this correlates to the binding affinity of enantiomers of phenibut to the GABAB receptor. Both S- and R-phenibut bind to the α2-δ subunit of voltage-dependent calcium channels and exert gabapentin-like anti-nociceptive effects. In addition S-isomer was found to be a substrate of gamma-aminobutyric acid aminotransferase, however, the R-isomer is a competitive inhibitor.

Hecogenin acetate is the acetylated form of Hecogenin, a naturally occurring sapogenin present in the leaves of plants from the Agave genus. It has been found to have antinociceptive activity in mice and has also been investigated as an anti-cancer agent in vitro. Hecogenin appears to exert its anticancer influence by modulating the ERK1/2 signal cascade and activates opioid receptors to influence nocioception.

Epiestradiol is an estradiol isomer with weak estrogenic activity.

1,25-dihydroxycalciferol (1,25-dihydroxyvitamin D2 or ercalcitriol) is a metabolite of vitamin D. It exerts antirachitic activity in animals. 1,25-dihydroxycalciferol and its analogs have antineoplastic actions in vitro.

D-kynurenine is metabolite of the amino acid D-tryptophan. D-kynurenine is an agonist for GPR109B (HM74), a putative G protein-coupled receptor. D-kynurenine elicits chemotactic responses in human neutrophils through GPR109B. D-amino acid oxidase can metabolize D-kynurenine to produce the fluorescent compound kynurenic acid.