BI-D1870 is a small molecule, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC(50) of 10-30 nM, but does not significantly inhibit ten other AGC kinase members and over 40 other protein kinases tested at 100-fold higher concentrations. BI-D1870 is cell permeant and prevents the RSK-mediated phorbol ester- and EGF (epidermal growth factor)-induced phosphorylation of glycogen synthase kinase-3beta and LKB1 in human embryonic kidney 293 cells and Rat-2 cells. BI-D1870 exhibited a dose-responsive antiproliferative effect on OSCC cells with relative sparing of normal human oral keratinocytes. The compound inhibited the downstream RSK target YB-1 and caused apoptosis. In addition, BI-D1870 also induced G2/M arrest by modulating the expression of p21 and other cell cycle regulators. BI-D1870 may be of useful in oral squamous cell carcinoma therapy. BI-D1870 has being shown to ameliorate experimental autoimmune encephalomyelitis in mice. BI-D1870 administration protected mice from EAE by reducing the infiltration of TH1 and TH17 cells into the CNS and decreasing mRNA levels of Ccr6 in TH17 cells. These results suggest that RSK inhibition is a promising strategy for the treatment of MS.

alpha-yohmbine (aka rauwloscine) is a diastereomer of yohimbine and shares many of the same properties. Rauwolscine acts as an alpha-2-adrenergic antagonist and is therefore used as an unregulated nutritional supplement for fat-burning and CNS stimulation. Rauwolscine is also an antagonist of the HT2B receptor and has been investigated for the potential to mitigate blood vessel spasms.

a-Acetylbutyrolacone was used as an intermediate for the development of the non-nucleoside human immunodeficiency virus inhibitors and for the synthesis of antitumor agent which has thymidylate synthase (TS) and dihydrofolate reductase (DHFR) properties. Moreover, it has been characterized for use as a fluorogenic reagent for the spectrofluorimetric determination of primary amines.

PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.

6-alpha-Naloxol is active metabolite of naloxone. 6-alpha-Naloxol was shown to be neutral antagonist at the mu receptor in vitro, with no affect on cAMP levels or GTPitalic gammaS binding, regardless of morphine pretreatment. It elicits withdrawal behaviour and conditioned place aversion in morphine pretreated rodents.