Midaglizole (also known as DG 5128) is a α2 adrenoceptor antagonist. Daiichi Pharmaceutical developed this drug as an oral antidiabetic agent and to treat asthma. However, further study of this drug was discontinued.

Emapunil acts as a selective agonist at the peripheral benzodiazepine receptor (TSPO). At the cellular level, the selective TSPO ligand XBD173 potentiated the amplitude and duration of GABA-mediated inhibitory postsynaptic currents in mouse medial prefrontal cortical neurons, which was prevented by finasteride. In animal and human trials, XBD173 produced rapid anxiolytic and anti-panic effects probably via newly synthesized neurosteroids, without producing sedation or withdrawal symptoms, and may represent a promising target for the development of fast-acting anxiolytics with a more favourable side-effect profile than benzodiazepines.

Ambasilide, a class III antiarrhythmic, has been shown to block multiple cardiac channels in a variety of animals including humans. Ambasilide is a potassium channel antagonist. Ambasilide has multichannel blocking properties including beta-adrenergic antagonism.

Amiterol, a phenethylamine derivative, is an oral anti-asthma drug (bronchodilator).

Telinavir (previously known as SC-52151) was developed as an anti-HIV aspartyl protease inhibitor for the treatment of HIV Infections. Telinavir participated in Phase I/II clinical study. In spite of the drug was well tolerated no antiviral activity was produced and further development of the drug was discontinued.

Milfasartan is an inhibitor of angiotensin II receptor type 1 was used in phase II clinical trial for the treatment of hypertension. However, these studies were discontinued.

Myrophine is an opiate analog and long-acting prodrug for morphine with a slow onset of effects. It is weaker than morphine as an analgesic but longer-lasting in effects and was thought to have a more local anesthetic effect than morphine, though with a somewhat greater tendency to cause histamine reactions like itching and rash. In addiction studies conducted in human subjects in the 1950s, myrophine did not substitute for morphine in withdrawal, did not produce notable morphine-like effects, and did not produce addiction or dependence regardless of dose or how it was administered.

Englitazone is a thiazolidinedione antidiabetic agent. It has insulinomimetic and insulin-enhancing actions in vitro and glucose-, insulin-, triglyceride-, and cholesterol-lowering properties in an animal model of non-insulin-dependent diabetes mellitus. It acts as a peroxisome-proliferator-activated receptor-gamma ligand. Englitazone inhibits ATP-sensitive potassium and calcium-activated non-selective cation channels in a voltage-independent manner.

Pyrroliphene is a dialkylaminodiphenylbutanol ester with antitussive and analgesic activities. In clinical trials the major side effect of Pyrroliphene was sedation, and the other side effect liabilities were similar to those of morphine.

Rivoglitazone hydrochloride (CS-011) is a thiazolidinedione-derivative peroxisome proliferator–activated receptor (PPAR)-γ agonist. It has been developed as potential treatment in type 2 diabetes mellitus and was shown to decrease plasma glucose and triglyceride levels in a dose-dependent manner in animals. Phase II and III clinical studies have assessed the efficacy and safety of rivoglitazone hydrochloride in patients with type 2 diabetes mellitus.