Dexamisole is the dextro-isomer of tetramisole, a broad spectrum anthelmintic. Dexamisole significantly improves mood and psychotonicity. In adrenergically innervated blood vessels dexamisole inhibits neuronal uptake of norepinephrine more than levamisole. Dexamisole antagonized the reserpine-induced hypothermia but was ineffective in the apomorphine-induced hypothermia in mice. It reduced ptosis produced by reserpine in mice but this effect was very weak. The effect of dexamisole on the amphetamine-induced hyperactivity depended upon the animal species. Dexamisole reduced the duration of immobility in the despair test in rats. It did not modify the 5-HTP-induced head twitch reaction in mice but produced stimulation of the hind limb flexor reflex in spinal rats. The latter effect was blocked by phenoxybenzamine but not by cyproheptadine and metergoline. Dexamisole also exerted a sedative and hypothermic effect. The above findings indicate that the pharmacological profile of dexamisole resembles in some respects that of tricyclic antidepressants; they also point out that this drug has a central noradrenergic activity.

Etazolate (EHT-0202) is a selective, positive GABAA receptor modulator has completed phase II clinical trials in patients with Alzheimer's disease. It is also a selective phosphodiesterase-4 inhibitor that is specific for cAMP. Etazolate showed anxiolytic and antidepressant activity and could be useful in managing post-traumatic stress disorder.

Pirnabine is the synthetic dibenzopyran drug. It was developed as anti-glaucoma drug.

Dicarbine is an orally active drug approved in Russia under the trade name Карбидин, is used for the treatment patients with schizophrenia and alcoholic psychosis. This drug blocks dopamine receptors in various brain parts, which leads to a reduction in the productive symptoms of psychosis: delusions and hallucinations.

Flutroline, an antipsychotic drug that was studied to treat patients with schizophrenia. Clinical trials have shown that the drug was a safe, effective, and 20 mg and above offered the best potential for optimal clinical effectiveness. However, information about the further development of this drug is not available.

Ralimetinib (LY2228820), a trisubstituted imidazole derivative, is a potent and selective, ATP-competitive inhibitor of the α- and β-isoforms of p38 mitogen-activated protein kinase. LY2228820 produced significant tumor growth delay in multiple in vivo cancer models (melanoma, non-small cell lung cancer, ovarian, glioma, myeloma, breast). Eli Lilly is developing ralimetinib for the treatment of cancer.

Stannsoporfin is a mesoporphyrin derivative patented by Rockefeller University as competitive heme oxygenase (HO) inhibitor for the prevention of hyperbilirubinemia in infants at risk of developing jaundice. Parenteral administration of Stannsoporfin has been shown to suppress or moderate jaundice in a wide variety of experimental and naturally occurring forms of hyperbilirubinemia in animals and man. Stannsoporfin is rapidly cleared from the plasma in animals, in adult humans, and in newborn infants and may inhibit competitive heme oxygenase for prolonged periods. The Stannsoporfin decreases the production of carbon monoxide from heme and increases the biliary excretion of unmetabolized heme but has no effect on the metabolic disposition of preformed bilirubin.

Etazepine (5,6-dihydro-5-methyl-11H-11-ethoxy-dibenzo[b,e]azepin-6-one) demonstrates anticonvulsant activity in rodents. Etazepine seems to exert its anticonvulsant effects by activating the GABAergic system.

Fosquidone (also known as GR63178A), a pentacyclic pyrroloquinone that was developed as an anticancer agent. Fosquidone participated in phase II clinical trial for the treatment of patients with colorectal, renal and non-small cell lung cancer. However, the drug didn’t show significant antitumor activity. The further development of this drug was discontinued.

Gomisin A (BESIGOMSIN/GA) one of the major dibenzocyclooctadiene lignans isolated from Schisandra chinensis Baill, has proved to possess a variety of pharmacological effects. It has been found to promote hepatocyte growth factor, limit lipid peroxidation, and inhibit apoptosis in acute hepatic injury animal models. Besigomsine also acts as an anti-inflammatory by preventing the release of arachidonic acid in macrophages in vitro. Laboratory evidence suggests that Besigomsine may have anticarcinogenic effects. Chronic administration of Gomisin A had an antihypertensive effect in AngII-induced hypertensive mice. Gomisin A may exert neuroprotective effects by attenuating the microglia-mediated neuroinflammatory response via inhibiting the TLR4-mediated NF-κB and MAPKs signaling pathways. Also it induces marked protective effects against hepatic and renal injury induced by CCl(4) exposure through differential regulation of the MAPK signal transduction pathway.