Tonapofylline is a selective oral adenosine A, receptor antagonist, for the potential treatment of congestive heart failure. Oral tonapofylline over the dose range of 3 to 225 mg/day produced significant increases in sodium excretion in patients with stable heart failure without causing kaliuresis or reducing renal function. Tonapofylline may be useful in the clinical setting for the prevention of kidney failure induced by nephrotoxic agents such as cisplatin. Tonapofylline may be renoprotective in the setting of concomitant treatment with a loop-diuretic. Adverse effects were generally mild. Tonapofylline had been in phase III clinical trial for the treatment of acute heart failure. However, this development was discontinued.

Spirogermanium [NSC 192965, Spiro-32] is a germanium derivative which was under development by Unimed Pharmaceuticals. Spirogermanium is not a phase or cell cycle specific drug and inhibits DNA, RNA and protein synthesis, the protein synthesis being the most susceptible to this agent. Activity in malignant lymphoma, ovarian cancer, breast cancer, large bowel cancer, and prostatic cancer was reported in the clinical studies. The drug was under clinical investigation against the wide spectrum of solid tumors and malignant lymphomas. Spirogermanium also exhibits antiarthritic and immunoregulatory activities after p.o. administration to rats. Spirogermanium decreased hindleg inflammatory lesions of adjuvant arthritic rats when administered p.o. before or after the development of the arthritic lesions. However, the therapeutic use of spirogermanium has been discontinued because of its high toxicity and the low response rate.

Indatraline (Lu 19-005) is a non-selective monoamine transporter inhibitor that has been shown to block the reuptake of dopamine, norepinephrine, and serotonin with effects similar to those of cocaine. In vivo, indatraline produced behavioral effects suggestive of enhanced dopaminergic, noradrenergic, and serotonergic activity in mice. Indatraline also substituted for a high dose of cocaine in rats trained to discriminate between a low and a high dose of cocaine, which demonstrates that indatraline produces cocaine-like discriminative stimulus effects. Indatraline has been studied to block the action of methamphetamine and MDMA.

Levemopamil is a novel compound of the phenylalkylamine class of calcium channel blockers, possesses exceptionally high blood-brain barrier penetrability characteristics. It has a potent antagonistic action on serotonin 5-HT2-receptors. Activation of these receptors stimulates inositol phospholipid hydrolysis that can lead to the release of Ca2+ from intracellular stores as well as protein kinase C activation. Levemopamil thus has the potential for blocking deleterious increases of intracellular calcium arising from both intracellular stores and from the extracellular space. Levemopamil reduce both infarct size and extent of neuronal injury following permanent focal or transient global ischemia. The acute effect of bilateral clamping of carotid arteries on local cerebral blood flow was measured in the presence and absence of levemopamil in a separate group of rats. The data suggest that pretreatment with levemopamil reduces impairment in spatial behaviour and that this effect seems not related to the compound's cerebral vasodilatory action, but to direct neuronal mechanisms.

Nocloprost is a stable prostaglandin E2 analog with gastroprotective and ulcer-healing properties. It shows very high gastroprotective potency, relatively weak gastric inhibitory activity, and low systemic bioavailability after oral administration. Schering AG have discontinued development of the drug, which was in phase II clinical trials for the treatment of peptic ulcer.

Cyclophenazine is an antagonist of dopamine receptors, discovered by Eli Lilly. The drug is claimed to possess tranquilizing, anti-emetic action, and is able to potentiate the action of anticholinergic compounds in inhibiting the gastric secretion.

Alazanine triclofenate is a mixture of one molecule of 3-ethyl-2-(3-(3-ethyl-2-benzothiazolinylidene)propenyl)benzothiazolium 2,4,5-trichlorophenate and two molecules of 2,4,5-trichlorophenol. It is an antiparasitic agent. It is antimalarial drug, highly active against multiple Plasmodium falciparum isolates with IC50 value of 2.36E-07 M.

Nitramisole, an imidazothiazole derivative, is an anthelmintic. Nitramisole was effective against migrating Strongylus vulgaris larvae in ponies. Treatment of infected ponies with Nitramisole resulted both a clinical and radical cure.

Bendacalol (also known as CGS 10078B) is an alpha- and beta-adrenergic receptor inhibitor with calcium entry blocking effect was studied for the treatment of hypertension. Animal experiments have sown some positive results. However, information about further studies is not available.

Clofeverine is a compound synthesized by the Japanese company Fujisawa Pharmaceutical. Clofeverine is a highly selective relaxant for gastrointestinal smooth muscles with a beta-receptor stimulative nature. On isolated ileum, the inhibitory effect of clofeverine for spontaneous motility was comparable to that of isoproterenol and 100 times higher than that of papaverine.