R-1485 is a lead candidate identified from Roche Pharmaceuticals research programme for the treatment of Alzheimer's disease. Selective and high affinity 5-HT6 antagonist; displays low hERG inhibition. Exhibits >100 fold selectivity against a panel of 50 targets including other 5-HT receptor subtypes. R-1485 is currently in Phase I trials at Roche for the treatment of Alzheimer’s type dementia. This compound showed a pKi value of 9.3 when it was tested for inhibition of [3H]-LSD binding to human 5-HT6 receptors expressed in HEK293 cells. In addition, it was also found that in rats this agent has good BBB permeability.

Citrinin is a mycotoxin produced by several species of the genera Aspergillus, Penicillium and Monascus. It is often found in food. Citrinin is nephrotoxic agent. Inhibition of RNA (predominantly rRNA) and DNA synthesis by citrinin has been reported in different mammalian cell lines including kidney cells. The induction of oxidative stress has also been proposed to account for citrinin toxicity. Citrinin inhibits immune response – it inhibits lipopolysaccharide/interferon-gamma-induced nitric oxide production in glomerular mesangial cells. Citrinin induced apoptosis in human colon cancer and promyelocytic leukemia cell lines.

Isoorientin is a common C-glycosyl flavone in the human diet. It has been isolated from several plant species, including Phyllostachys pubescens, Crataegus monogyna and Crataegus pentagyna, Patrinia villosa Juss, Drosophyllum lusitanicum, buckwheat, Arum palaestinum, and Rumex and Swertia. Isoorientin possesses significant anti-nociceptive and anti-inflammatory activities. Significantly protected PC12 nerve cells from 6-OHDA-induced apoptotic neurotoxicity and reduced the proliferation of HepG2 cells. Isoorientin showed anti-RSV (respiratory syncytial virus) activity.