Efaroxan (RX 821037) is a potent and selective alpha(2)-adrenoceptor antagonist. Additionally, Efaroxan is a selective antagonist at the imidazoline I1 receptor. Efaroxan promotes insulin secretion, in the absence of exogenous agonists, by a mechanism that involves inhibition of ATP-regulated K+ channels. Efaroxan was in clinical trials for the treatment of diabetes mellitus however its development has been discontinued.

Revatropate is a muscarinic antagonist with selectivity for M1 and M3 receptor subtypes. Significant improvement in airway function was shown in horses with heaves after inhalation of revatropate, and it was found to be a safe and effective bronchodilator. Early clinical studies in chronic obstructive airway disease (COAD) patients also showed that inhaled revatropate was an effective bronchodilator, and well tolerated.

Carbocloral is a carbamate ester derivative used as sedative and hypnotic drug. Carbocloral is as effective as chloral hydrate in producing sedation, hypnosis, and general anesthesia, and more effective in inducing relaxation of skeletal muscles. Carbocloral was also more effective as an anticonvulsant and less toxic than chloral hydrate.

FLORIFENINE is an anti-inflammatory agent. It inhibits the cyclooxygenase pathway and, in addition, it inhibits migration and decreases in vitro the release of neutrophil elastase.

Altanserin is a potent and selective 5-HT2A receptor antagonist. Serotonin (5-HT) system functioning have been proposed for a variety of psychiatric disorders, but a direct method quantitatively assessing 5-HT release capacity in the living human brain is still lacking. It was suggested that the combination of a dexfenfluramine-induced 5-HT release and subsequent assessment of 5-HT(2A) receptor availability with [(18)F]altanserin by positron emission tomography (PET) was suitable to measure cortical 5-HT release capacity in the human brain. Besides human neuroimaging studies altanserin has also been used in the study of rats.

Orbofiban was developed as an orally active glycoprotein IIb/IIIa antagonist. By 2001, this drug had progressed to phase III clinical trials. Unfortunately, was found that orbofiban induced thrombocytopenia and thrombosis. In addition, despite no significant excess risk of intracranial hemorrhage, orbofiban was not effective in preventing ischemic stroke or transient ischemic attack. Besides, the use of this drug had led to an increase in mortality. Based on all these results further development of this drug was discontinued.

Glisindamide is a hypoglycemic agent and part of the second-generation sulfonamide derivatives, used as medication to control blood sugar levels in patients with diabetes mellitus type 2. Glisindamide exerts greater binding affinity to sulfonylurea receptor type 1 (SUR1) than the first-generation compounds. It also exerts greater binding affinity for peroxisome proliferator-activated receptor gamma (PPARgamma) agonistic activity.

Gadopenamide is an MRI contrast agent that was introduced in 1991. It has been investigated as a potential clinical contrast medium by Schering AG (Germany), but has never been used as such.

Tisoquone is the hypolipaemic agent.