MK 0777 is a selective GABAA α2/3 receptor partial agonist, for potential use in the treatment of Schizophrenia, Anxiety Disorder, and Generalized Anxiety Disorder. MK-0777 is functionally selective for the α2 and α3 subunits, with virtually no activity for the α1 and α5 subunits. Therefore, MK-0777 cause less sedation, interact less with alcohol, and exhibit less abuse potential and physical dependence than benzodiazepines. Unfortunately, in clinical trials, MK-0777 has little benefit for cognitive impairments in people with schizophrenia and anxiety disorder.

Ciclotropium is quaternary ammonium compound with anticholinergic and parasympatholytic activity. Oral Cyclotropium bromide inhibited fasting and meal-stimulated colonic motility significantly without causing adverse side effects. After cyclotropium bromide, there was a significant correlation between antral contraction amplitude and gastric emptying.

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.

Dimesna is a prodrug of mesna (dimer of mesna). Dimesna is reduced to mesna in the kidneys. Dimesna does not prevent cellular damage by metabolites of ifosfamide and cyclophosphamide in the renal tubular cell line LLC-PK1. Dimesna is a mucolytic agent used to alleviate toxic side effects of antitumor drugs. The organic acid transporter OAT4 on the luminal side of the proximal renal tubule facilitates the reabsorption of dimesna, and therefore its reduction to mesna, whereas the multidrug and toxin extrusion protein MATE1, the multidrug resistance protein MRP2, and P glycoprotein facilitate the efflux of mesna and/or dimesna back into the lumen; dimesna may also be excreted unchanged by MRP4. It has therefore been suggested that polymorphism of these renal transport proteins or transporter-mediated drug-drug interactions may reduce the efficacy of mesna and dimesna.

Furacrinic acid (also known as GP 48 674) was studied as a diuretic agent and participated in clinical trials. However, information about the further development of this drug is not available.

Eprotirome (KB2115) is a thyroid hormone mimetic developed at Karo Bio AB (Huddinge, Sweden). Eprotirome has a 22-fold higher affinity for thyroid hormone receptor (TR)β in comparison with TRα. It lowers plasma LDL cholesterol and stimulates bile acid synthesis. Eprotirome can lower LDL cholesterol concentrations in patients with familial hypercholesterolaemia when added to conventional statin treatment with or without ezetimibe, but that it has the potential to induce liver injury. These findings, along with findings of cartilage damage in dogs, raise serious doubts about selective thyroid hormone mimetics as a therapeutic approach to lower LDL cholesterol concentrations. Eprotirome development was discontinued.

Amfonelic acid (AFA) is a dopamine reuptake inhibitor. Experiments on rats have shown that AFA treatment completely prevented the effects of methamphetamine on the dopaminergic system, both morphologically and biochemically.

N,N-Dimethyl-5-Methoxytryptamine (aka 5-MeO-DMT) is a psychedelic of the tryptamine class. It is found in a wide variety of plant species, and a single psychoactive toad species, the Colorado River toad. Like its close relatives DMT and bufotenin (5-HO-DMT), it has been used as an entheogen in South America. It can also be found in the dart poison traditionally used by the Yanoama Indians of Upper Orinoco. It acts as a non-selective serotonin (5-HT) agonist. -MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metabolite, bufotenine. 5-MeO-DMT is classified as a controlled substance in China, Australia, Sweden, Turkey, and the USA.

Muscimol is one of the principal psychoactive constituents of Amanita muscaria and related species of mushroom. Muscimol is a potent, selective agonist for the GABAAreceptors and displays sedative-hypnotic, depressant and hallucinogenic psychoactivity. The effects of the Amanita mushrooms begin 30–120 minutes after consumption and the effects last for 5–10 hours. Some of the desired effects include euphoria, dream-like (lucid) state of mind, out-of-body experiences, and synesthesia. Neutral effects include dizziness, clumsiness, the feeling of increased physical strength, loss of equilibrium, and a glassy-eyed stare. Calming effects may be felt, but completely opposite effects such as extreme energy bursts have been described. Negative effects include mild to moderate nausea, stomach discomfort, increased salivation, and muscle twitching or tremors. In large doses, strong dissociation or delirium may be felt.

Iosefamic Acid is triiodoisophthalamic acid derivative patented by Mallinckrodt Chemical Works as x-ray contrast agent for imaging in the biliary and urinary systems and in vasography.