Chrysophanic acid (Chrysophanol) is a member of the anthraquinone family abundant in rhubarb, a widely used herb for obesity treatment in Traditional Korean Medicine. Chrysophanol has been shown to induce cell death in different types of cancer cells. Chrysophanol inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K. Chrysophanol also effectively suppresses breast cancer cell proliferation and facilitates chemosentivity through modulation of the NF-κB signaling pathway. A treatment of chrysophanol could reduce significantly the clinical signs and the levels of inflammatory mediators in a colitis model caused by DSS treatment. The anti-inflammatory activities of chrysophanol could be attributed, at least in part, to the inhibition of proinflammatory cytokine production (TNF-α and IL-6), COX-2, and iNOS protein expression. These effects of chrysophanol are caused by the inhibition of LPS-induced NF-κB activation, IκB-α degradation, and caspase-1 activation. These results provide experimental evidence showing that chrysophanol might prove useful in the treatment of inflammatory diseases.

U-92016A is a psychoactive drug and research chemical used in scientific studies. U-92016A acts as a potent, high efficacy, and selective 5-HT1A receptor full agonist with a long duration of action.

ORG 37684 is a selective full agonist of 5-hydroxytryptamine receptor 5-HT2 family with a high selectivity for 5-HT2C in comparison with 5-HT2B and 5-HT2A receptors. It was studied for treatment of depression, but that investigations were discontinued. On animal studies ORG 37684 possessed hypophagic effect, which was exclusively mediated by activation of 5-HT2C receptors. Thus, this compound can be further investigated in using for weight loss.

is a potent, selective, brain penetrant, orally active serotonin 5-HT(6) receptor antagonist with cognitive enhancing, anxiolytic and antidepressant properties. It is able to regulate sleep and wakefulness in rodents. In addition it demostrates antinociceptive and antiepileptic potentials.

ST1936 is a potent serotonin 6 (5-HT6) receptor agonist with activity in animal pharmacological models for central nervous system disorders: effect of ST 1936 was investigated on depression-like experimental models. In addition, ST 1936 displays moderate affinity for human α2 adrenergic receptors, shown to increase Ca2+ concentration and phosphorylation of Fyn kinase, and regulate the activation of ERK1/2 in cloned cells.

MRK-016 is a selective inverse agonist of GABA receptor alpha-5 subunit. It was shown; that in animal models this compound has effect effects on depression.

ANA-12 is a low-molecular weight antagonist of tropomyosin-related kinase B (TrkB), which is the main receptor of neurotrophin brain-derived neurotrophic factor (BDNF). TrkB and BDNF are both the key mediators in the pathophysiology of several mood disorders, including anxiety and depression. ANA-12 showed direct and selective binding to TrkB and inhibited processes downstream of TrkB without altering TrkA and TrkC functions. It was shown, that mice administered ANA-12 demonstrated reduced anxiety- and depression-related behaviors on a variety of tests predictive of anxiolytic and antidepressant properties in humans.

Org-12962 was developed by Organon as a potent and selective Serotonin 5-HT(2C) receptor agonist. It was in clinical trial phase II for depression treatment, but the investigation was discontinued. In addition, was shown, Org-12962 displayed antiaversive effects in a rat model of panic-like anxiety.

NE-100 is potent and selective σ1 receptor antagonist that displays > 55-fold selectivity over σ2receptors and > 6000-fold selectivity over D1, D2, 5-HT1A, 5-HT2 and PCP receptors. NE-100 exhibits reversible binding and displays antipsychotic activity in vivo.

2-ethyl-5-methoxy-N, N-dimethyltryptamine (EMDT) represents the first and most selective 5-HT(6) receptor agonist. Based on its activity in tail suspension test was suggested, that EMDT could be an effective antidepressant