Kaempferol (3,5,7-trihydroxy-2-(4-hydroxyphenyl)-4H-1-benzopyran-4-one) is a flavonoid found in many edible plants (e.g. tea, broccoli, cabbage, kale, beans, endive, leek, tomato, strawberries and grapes) and in plants or botanical products commonly used in traditional medicine (e.g. Ginkgo biloba, Tilia spp, Equisetum spp, Moringa oleifera, Sophora japonica and propolis). Numerous preclinical studies have shown that kaempferol and some glycosides of kaempferol have a wide range of pharmacological activities, including antioxidant, anti-inflammatory, antimicrobial, anticancer, cardioprotective, neuroprotective, antidiabetic, anti-osteoporotic, estrogenic/antiestrogenic, anxiolytic, analgesic and antiallergic activities.

Dihydroisocodeine is an opioid derivative. Dihydroisocodeine is much less toxic for rabbits than codeine, and in these and other animals its convulsant action is less marked. The minimum analgesic dose for cats is considerably less than for codeine. In the 1930s it was clinically investigated for cough relief, where it has no demonstrable clinical superiority over standard codeine in the usual therapeutic dosage.

PJ34 is PARP inhibitor. It protects primary neuronal cells from oxygen-glucose deprivation in vitro and reduces infarct size following cerebral and cardiac ischemia in vivo. PJ34 exhibit suppresses cell growth and enhances the suppressive effects of cisplatin in liver cancer cells.

SDB-005 is a synthetic cannabinoid. It is considered to be a constituent of illicit smoking mixtures "spice".

5F-SDB-006 is a synthetic cannabinoid. It is considered to be a constituent of illicit smoking mixtures "spice".

NS1738 (1-(5-chloro-2-hydroxy-phenyl)-3-(2-chloro- 5-trifluoromethyl-phenyl)-urea) is a positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor (nAChR). NS1738 is capable of producing cognitive enhancement in vivo. NS1738 significantly reduced thermal hyperalgesia in mice.

NS11394 is the novel subtype-selective GABAA receptor-positive modulator which possesses a functional efficacy selectivity profile of alpha5 > alpha3 > alpha2 > alpha1 at GABAA alpha subunit-containing receptors. Compared with other subtype-selective ligands, NS11394 is unique in having superior efficacy at GABAA-alpha3 receptors while maintaining low efficacy at GABAA- alpha1 receptors. NS11394 has an excellent pharmacokinetic profile, which correlates with pharmacodynamics endpoints (CNS receptor occupancy), yielding a high level of confidence in deriving in vivo conclusions anchored to an in vitro selectivity profile and allowing for translation to higher species. Specifically, we show that NS11394 is potent and highly effective in rodent anxiety models. The anxiolytic efficacy of NS11394 is most probably mediated through its high efficacy at GABAA-alpha3 receptors, although a contributory role of GABAA-alpha2 receptors cannot be excluded.

BAY-59-3074 is a novel, selective cannabinoid CB(1)/CB(2) receptor ligand (K(i) = 55.4, 48.3, and 45.5 nM at rat and human cannabinoid CB(1) and human CB(2) receptors, respectively), with partial agonist properties at these receptors in guanosine 5-[gamma(35)S]-thiophosphate triethyl-ammonium salt ([(35)S]GTPgammaS) binding assays. It displays anti-hyperalgesic and antiallodynic properties in rat models of chronic neuropathic and inflammatory pain. BAY-59-3074 may offer a valuable therapeutic approach to treat diverse chronic pain conditions.

BAY-36-7620 is a potent and selective antagonist at mGlu1receptors and inhibits >60% of mGlu1a receptor constitutive activity (IC50 = 0.38 uM). BAY-36-7620 is thus the first described mGlu1 receptor inverse agonist. It impairs classical conditioning and associated synaptic plasticity in hippocampal neurons. BAY-36-7620 exhibits neuroprotective and anticonvulsive effects in vivo following systemic administration.

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.