Nefiracetam is a cyclic derivative of gamma-aminobutyric acid (GABA). It is thought to act by normalising dysfunctional acetylcholine, GABA and possibly monoamine neurotransmitter systems, but it may also facilitate N/L-type calcium channel opening. Nefiracetam has received attention as a treatment for seizures, depression, and dementia. Nefiracetam was found to be extremely testicular toxic in both rats and dogs; it was found to significantly decrease the levels of testicular testosterone leading to atrophy and malformation of sperm.

Mafoprazine is a phenylpiperazine derivative exerting postsynaptic dopamine D2 receptor blocking activity and alpha-adrenergic activity (alpha 1 receptor blocking activity and alpha 2 receptor stimulating activity). In animal models, mafoprazine demonstrated antipsychotic, aggression-inhibiting and cataleptogenic actions.

Netoglitazone (also called MCC-555) is a hypoglycemic agent belonging to the thiazolidinedione group that exerts both peroxisome proliferator-activated receptor (PPAR) alpha and gamma agonist activity. It was developed by Mitsubishi-Tokyo (formerly Mitsubishi Chemical) as a potential treatment for type 2 diabetes due to the enhancement of insulin sensitivity. This drug was in clinical trial phase II but then was discontinued. In addition, was also investigated the behaviour of MCC-555 on colorectal cancer (CRC) cells and was revealed, that the drug had an effect on the early events of colon carcinogenesis and could be a potential preventive compound for CRC.

(S)-baclofen (or L-baclofen) is an enantiomer of baclofen, a direct GABA-B receptor mimetic. L-baclofen represents a significant improvement over racemic baclofen in the treatment of trigeminal neuralgia.

Ecabapide (DQ 2511) is a compound with antiulcer and gastroprokinetic activity. Evidence from basic studies in animal models suggests that the drug acts on peripheral mechanisms of neural control. In the stomach, ecabapide acts to suppress firing in vagal afferent nerves and thereby reduce the flow of sensory information into the dorsal vagal complex. The mechanism of action of ecabapide in suppressing discharge in vagal afferent terminals appears to mimic that of nitric oxide by stimulating formation of cGMP and activation of an inhibitory transduction cascade in the sensory fibres. In this respect the mechanism of its pro-kinetic action differs from other promoter agents. Ecabapide development has been discontinued.

Pinokalant is the isoquinoline derivative. It is a broad-spectrum cation channel blocker which inhibits store-operated cation channels in human endothelial cells, mast cells, HL60 cells and in primary cultures of cortical and hippocampal neurons. Pinokalant inhibits voltage-operated calcium channels of the L- and N-subtypes in primary cultures of cortical neurons and shows some antagonism on the NMDA- and AMPA glutamate receptor subtypes. Pinokalant also acts as an antagonist at the delayed rectifier K+ channel in PC12 cells and cortical neurons. Pinokalant reduced in vivo lesion size as well as post mortem infarct size derived from 2,3,5-triphenyltetrazolium chloride-stained brain slices 24 hr after middle cerebral artery occlusion. Pinokalant has been evaluated as a potential neuroprotectant in rodent models of stroke.

Tyramine is a naturally occurring monoamine compound and trace amine derived from the amino acid tyrosine. Tyramine occurs widely in plants and animals, and is metabolized by the enzyme monoamine oxidase. Tyramine is an alpha-adrenergic agonist. Hypertension can occur, from ingestion of tyramine-rich foods in conjunction with monoamine oxidase inhibitors. The possibility that tyramine acts directly as a neurotransmitter was revealed by the discovery of a G protein-coupled receptor with high affinity for tyramine, called TAAR. It exhibits sympathomimetic effects by causing the release of endogenic norepinephrine. It has been used in mydriatic eyedrops. This has been said to reduce the intraocular pressure in rabbits and in some patients with open-angle glaucoma.

Deterenol is a beta-adrenoceptor agonist. It is an effective nonmydriatic and nonmiotic hypotensive agent, which can be used in antiglaucoma treatment.

Etiprednol dicloacetate (BNP-166; ethyl-17alpha-dichloroacetoxy-11beta-hydroxyandrosta-1,4-diene-3-one-17beta-carboxylate) is a new soft steroid. The compound proved to be a dissociated glucocorticoid, showing a reduction in transactivating activity while preserving transrepressive abilities. The compound effectively decreased cytokine production in lipopolysaccharide-stimulated lymphocytes and attenuated lectin-induced proliferation of blood mononuclear cells in tissue culture. The significant local effect of the compound will very likely be accompanied by a drastically reduced systemic activity indicating an encouraging selectivity of the pharmacological action of etiprednol dicloacetate. Etiprednol dicloacetate had been in a clinical trial for the treatment of allergic rhinitis, asthma and Crohn's disease. However, development has been discontinued.

MK-0354 is a GPR109a (Niacin receptor 1) agonist, originated by Arena Pharmaceuticals. In phase II of clinical trials against dyslipidemia treatment with MK-0354 failed to produce changes in high-density lipoprotein cholesterol, low-density lipoprotein cholesterol, or triglycerides.