Midafotel, also known as SDZ-EAA 494 and D-CPP-ene, is a potent, competitive antagonist at the NMDA receptor. It was originally designed as a potential therapy for excitotoxicity, epilepsy or neuropathic pain. It looked very promising in in vitro trials proving to be a potent competitive antagonist at the NMDA without affecting other receptors.

Mofegiline, also known as MDL-72974, or MDL-72974A (HCl salt), is a selective, irreversible inhibitor of monoamine oxidase B (MAO-B) and semicarbazide-sensitive amine oxidase (SSAO) which was under investigation for the treatment of Parkinson's disease and Alzheimer's disease, but was never marketed.

Ranirestat, also known as AS-3201; SX-3201, is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy by Dainippon Sumitomo Pharma and PharmaKyorin. It has been granted orphan drug status. The drug is to be used orally. Aldose reductase is an enzyme that catalyzes one of the steps in sorbitol (polyol) pathway which is responsible for formation of fructose from glucose. Aldose reductase activity is increased, parallel to glucose blood levels, in tissues that are not insulin sensitive, including lenses, peripheral nerves and renal glomeruli. Sorbitol does not diffuse through cell membranes easily and therefore accumulates in these tissues, causing osmotic damage, leading to retinopathy and neuropathy.

Pyridoxamine, also known as K-163, is one form of vitamin B6. Chemically it is based on a pyridine ring structure, with hydroxyl, methyl, aminomethyl, and hydroxymethyl substituents. It differs from pyridoxine by the substituent at the 4-position. The phenol at position 3 and aminomethyl group at position 4 of its ring endow pyridoxamine with a variety of chemical properties, including the scavenging of free radical species and carbonyl species formed in sugar and lipid degradation and chelation of metal ions that catalyze Amadori reactions.

Foropafant, also known as SR-27417; SR-27417A, is a potent platelet activating factor (PAF) inhibitor potentially for the treatment of asthma and allergic rhinitis (AR). SR 27417 inhibits in a dose-dependent manner the hypotensive effect of PAF in rats. It protected rats with an ED50 value of 6 +/- 2 micrograms/kg (n = 6), when given i.v., 1 min before PAF administration. PAF plays a major role in anaphylactic shock. SR 27417 may be an effective prophylactic as well as a potent curative drug in this pathology.

Remacemide, also known as PR-934423 and FPL 12924AA, is a low-affinity NMDA antagonist with sodium channel blocking properties. It has been studied for the treatment of acute ischemic stroke, epilepsy, Huntington's disease, and Parkinson's disease. Remacemide binds weakly and noncompetitively to the ionic channel site of the NMDA receptor complex. Remacemide binds both allosterically and in the channel. However, because remacemide binds so weakly to NMDAR, much of remacemide's in vivo effect against excitotoxicity is thought to be caused by its metabolic transformation to the more potent desglycine derivative FPL 12495.

Selfotel, also known as CGS-19755 and CPDD 0027, is a competitive NMDA antagonist. Selfotel directly competes with glutamate for binding to the receptor. Initial studies showed it to have anticonvulsant, anxiolytic, analgesic and neuroprotective effects, and it was originally researched for the treatment of stroke, but subsequent animal and human studies showed phencyclidine-like effects, as well as limited efficacy and evidence for possible neurotoxicity under some conditions, and so clinical development was ultimately discontinued.

Darodipine, also known as PY-108068, is a potent a calcium antagonist. Darodipine dose-depentently blocks I(Ca,L) in rat isolated cardiomyocytes. Darodipine exerts protective effects against free-radical-induced electrophysiological alterations independently of its calcium antagonistic properties; this effect is possibly due to trapping of specific radical species. .

Sunepitron, also known as CP-93,393 or CP-93,393-1 (HCl), is a combined 5-HT1A receptor agonist and α2-adrenergic receptor antagonist. It was previously under development by Pfizer for the treatment of depression and anxiety. It made it to phase III clinical trials before being discontinued.

Taribavirin, also known as Viramidine, is an antiviral drug candidate. It is a prodrug of ribavirin, active against a number of DNA and RNA viruses. Taribavirin has better liver-targeting than ribavirin, and has a shorter life in the body due to less penetration and storage in red blood cells. It is expected eventually to be the drug of choice for viral hepatitis syndromes in which ribavirin is active. These include hepatitis C and perhaps also hepatitis B and yellow fever.

Veralipride is a benzamide neuroleptic medicine indicated in the treatment of vasomotor symptoms associated with the menopause. It was first authorised for use in 1979. Veralipride was withdraw from the market in 2007.

Suxibuzone is a analgesic used for joint and muscular pain. It is a prodrug of the non-steroidal anti-inflammatory drug phenylbutazone, and is commonly used in horses.

Butibufen, also known as FF-106, is a cyclooxygenase inhibitor used to treat inflammatory and rheumatic disorders. utibufen was within the potency range of ibuprofen as an antipyretic and analgesic agent and greater than that of acetylsalicylic acid. The compound possesses the advantage of a low order to toxicity. Its ulcerogenicity was much lower than that of phenylbutazone. Therefore, butibufen appears to offer potential safety and efficacy in the treatment of rheumatic diseases. Butibufen was now withdraw from the market.

Alpidem is an anxiolytic drug from the imidazopyridine family, related to the more well known sleeping medication zolpidem. Unlike zolpidem however, alpidem does not produce sedative effects at normal doses, and is instead used specifically for the treatment of anxiety. It was approved for marketing in France in 1991 and was withdrawn fin 1994 and is not approved for marketing anywhere in the world. Alpidem has nanomolar binding affinity for both the central benzodiazepine receptor (CBR) and the peripheral benzodiazepine receptor (PBR) (translocator protein 18 kDa) (PBR (Ki ) 0.5-7 nM) and CBR (Ki ) 1-28 nM, respectively).

Medroxyprogesterone Acetate, also known as MPA, is a steroidal progestin, a synthetic variant of the steroid hormone progesterone. It is used as a contraceptive, in hormone replacement therapy and for the treatment of endometriosis as well as several other indications. MPA is a more potent derivative of its parent compound medroxyprogesterone (MP). While medroxyprogesterone is sometimes used as a synonym for medroxyprogesterone acetate, what is almost always being referred to is MPA and not MP It is on the World Health Organization's List of Essential Medicines, the most important medication needed in a basic health system.

Oxyphenbutazone, also known as G-29701, a non-steroidal anti-inflammatory drug (NSAID). It is a metabolite of phenylbutazone.

Rapacuronium Bromide, also known as Org 9487, is a rapidly acting, non-depolarizing neuromuscular blocker formerly used in modern anaesthesia, to aid and enable endotracheal intubation, which is often necessary to assist in the controlled ventilation of unconscious patients during surgery and sometimes in intensive care. As a non-depolarizing agent it did not cause initial stimulation of muscles before weakening them. Due to risk of fatal bronchospasm it was withdrawn from the United States market by Organon on March 27, 2001, less than 2 years after its FDA approval in 1999.

Aildenafil, also known as Methisosildenafil, is a phosphodiesterase type 5 inhibitor and a structural analog of sildenafil (Viagra). It was first reported in 2003, and it is not approved by any health regulation agency. Like sildenafil, aildenafil is a phosphodiesterase type 5 inhibitor. Aildenafil has been found as an adulterant in a variety of supplements which are sold as "natural" or "herbal" sexual enhancement products. The United States Food and Drug Administration has warned consumers that any sexual enhancement product that claims to work as well as prescription products is likely to contain such a contaminant.

Aceneuramic acid, also known as NPC-09; Ace-ER; UX-001; Neu-5Ac; SA-ER; AceER. is an immunomodulator potentially for treatment of hereditary inclusion body myopathy (HIBM). Aceneuramic acid is an N-acyl derivative of neuraminic acid. N-acetylneuraminic acid occurs in many polysaccharides, glycoproteins, and glycolipids in animals and bacteria.

Morinidazole was approved by China Food and Drug Administration (CFDA) on February 24, 2014. Morinidazole is a nitroimidazoles antibiotic used to treat bacterial infections including appendicitis and pelvic inflammatory disease. Morinidazole is a nitroimidazoles antibiotic indicated for the treatment of bacterial infections including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.

Ozenoxacin, also known as GF-001001-00; M-5120; T-3912; GF-00100100, is an experimental quinolone antibiotic being developed for the treatment of impetigo and other dermatological bacterial infections. Ozenoxacin is active against some bacteria that have developed resistance to currently used quinolone and fluoroquinolone antibiotics.

Sulfamerazine is a long-acting sulfanilamide antibacterial agent. Sulfamerazine inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for the binding site on dihydropteroate synthase.

Raclopride, also known as FLA 870, a selective antagonist on D2 dopamine receptor. Its selectivity to the cerebral D2 receptors is characterized by its respective Ki-values, which are as follows: 1.8, 3.5, 2400 and 18000 nM for D2, D3, D4 and D1 receptors respectively. It can be radiolabelled with radioisotopes, e.g. 3H or 11C and used as a tracer for in vitro imaging (autoradiography) as well as in vivo imaging positron emission tomography (PET). Images obtained by cerebral PET scanning (e.g. PET/CT or PET/MRI) allow the non-invasive assessment of the binding capacity of the cerebral D2 dopamine receptor, which can be useful for the diagnosis of movement disorders.

Eticlopride, also known as FLB 131, is a substituted benzamide analog with high affinity and selectivity for dopamine (DA) D2-like receptors that was initially developed as a potential antipsychotic agent. It is primarily used in pharmacological research. Eticlopride accelerates extinction and delays reacquisition of food self-administration in rats. Eticlopride induce microcatalepsy during operant performance in rats.

Phthalocyanine Chloroaluminum, also known as Aluminum phthalocyanine chloride, is an intensely blue-green-coloured aromatic macrocyclic compound that is widely used in dyeing. Phthalocyanine Chloroaluminum is a powerful photosensitizer and is useful in PDT. Photodynamic therapy (PDT) combines light, molecular oxygen and a photosensitizer to induce oxidative stress in target cells.

Pafuramidine, also known as DB289, is an orally bioavailable prodrug of furamidine (DB75) which was developed for the treatment of human African trypanosomiasis. Pafuramidine is less toxic than previous diamidines such as pentamidine. To date, human trials suggest that pafuramidine is well tolerated overall and has clinical activity against Pneumocystis pneumonia. DB289 is a promising new antimalarial compound that could become an important component of new antimalarial combinations.

Ebrotidine, also known as FI-3542, is an H2 receptor antagonist with gastroprotective activity against ethanol-, aspirin- or stress-induced gastric mucosal damage. The antisecretory properties of ebrotidine are similar to those of ranitidine, and approximately 10-fold greater than those of cimetidine. Ebrotidine has anti-Helicobacter pylori activity via inhibition of the urease enzyme and the proteolytic and mucolytic activities of the bacterium. However, its activity is synergistic with a number of antibacterial agents. Ebrotidine counteracts the inhibitory effects of H. pylori lipopolysaccharides. Ebrotidine has been shown to be as effective as ranitidine for the treatment of gastric or duodenal ulcers or erosive reflux oesophagitis, with significantly better ulcer healing rates (albeit inexplicably) in those who smoke.

Daminozide is a plant growth regulator, a chemical sprayed on fruit to regulate their growth, make their harvest easier, and keep apples from falling off the trees before they are ripe. This makes sure they are red and firm for storage. Alar was first approved for use in the U.S. in 1963, it was primarily used on apples until 1989 when it was voluntarily withdrawn by the manufacturer after the U.S. Environmental Protection Agency proposed banning it based on concerns about cancer risks to consumers.

Cromakalim, also known as BRL 34915, is a potassium channel-opening vasodilator. The active isomer is levcromakalim. It acts on ATP-sensitive potassium channels and so causes membrane hyperpolarization. It can be used to treat hypertension as it will relax vascular smooth muscle to lower blood pressure. Hyperpolarisation of smooth muscle cell membranes pulls their membrane potential away from the threshold, so making it more difficult to excite them and thereby cause contraction.

Naldemedine, also known as S 297995, is a peripherally-selective μ-opioid receptor antagonist under development by Shionogi for the treatment of opioid-induced adverse effects including constipation, nausea, and vomiting. Clinical studies have thus far found it to possess statistically significant effectiveness for these indications and to be generally well-tolerated with predominantly mild to moderate gastrointestinal side effects. No effects indicative of central opioid withdrawal or impact on the analgesic or mydriatic effects of co-administered opioids have been observed.