Halonamine was studied as an antiparkinsonian agent.

Tropapride is dopamine D2 receptor antagonist, which potential high antipsychotic activity has been clearly shown in biochemical and pharmacological tests.

Masilukast (ZD 3523) is an antagonist of leukotriene D4 (LTD4). It opposes LTD4-induced bronchoconstriction. It was being developed for the treatment of asthma.

Hexacyprone has been used as a choleretic agent. Information about the current use of this compound is not available.

Japan Tobacco developed JTV-519 (known also as K201) as an antiarrhythmic agent. This drug was in Phase II trials for the potential treatment of Atrial Fibrillation, but study was terminated. In experimental myofibrillar overcontraction models, JTV-519 demonstrated greater cardioprotectant effects than propranolol, also, this drug investigated against heart failure, but then these researches have been discontinued. In addition, K201 was in phase II clinical trial for investigation its topical implementation for Atopic Dermatitis. The mechanism of its action is both complex and controversial, known that it is a non-specific blocker of sodium, potassium and calcium channels (multiple-channel blocker). It is believed to stabilize the closed state of the RyR2 (cardiac ryanodine receptor) by increasing its affinity for the FKBP12.6 (12.6 kDa FK506 binding protein), in addition was suggested, that suppression of spontaneous Ca2 release and the activity of RyR2 contributes, at least in part, to the anti-arrhythmic properties of K201.

Dioxethedrin is the ephedrine derivative. It is the beta-adrenergic agonist. As a bronchodilator and sympathomimetic agent is was used in antitussive syrup Bexol.

Tradipitant is a neurokinin 1 receptor antagonist. The dose of 50 mg of tradipitant given orally for 4 weeks was not superior to placebo in reducing itch intensity in patients with atopic dermatitis. However, in a subsequent study, in which a higher dose (85 mg) was administered for 8 weeks, significant antipruritic effect compared with placebo was recorded. Tradipitant is in phase III clinical trial for the treatment of atopic dermatitis and gastroparesis. Vanda Pharmaceuticals plans a phase III trial in Motion Sickness in 2019.

GSK-923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E), and the third novel drug candidate to arise from Cytokinetics' broad strategic alliance with GlaxoSmithKline (GSK). GSK-923295 demonstrated a broad spectrum of activity against a range of human tumor xenografts grown in nude mice, including models of colon, breast, ovarian, lung and other tumors. GSK-923295 is the first drug candidate to enter human clinical trials that specifically targets CENP-E and is currently in Phase I human clinical trials being conducted by GSK. GSK-923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of CENP-E to microtubules is insufficient to satisfy the mitotic checkpoint. Consistent with genetic studies in mice suggesting that decreased CENP-E function can have a tumor-suppressive effect, inhibition of CENP-E induced tumor cell apoptosis and tumor regression.

Lipoprotein lipase (LPL) is a rate-limiting enzyme that hydrolyzes circulating triglyceride-rich lipoproteins such as very low-density lipoproteins and chylomicrons. Otsuka Pharmaceutical Factory, Inc. synthesized the LPL activator NO-1886 (ibrolipim, [4-(4-bromo-2-cyano-phenylcarbamoyl)-benzyl]-phosphonic acid diethyl ester, CAS 133208-93-2). NO-1886 increased LPL mRNA and LPL activity in adipose tissue, myocardium and skeletal muscle, resulting in an elevation of postheparin plasma LPL activity and LPL mass. It was discovered, that this agent has a potentially beneficial for the treatment of hypertriglyceridemia, hypo-HDL cholesterolemia, and protection from atherosclerosis. In addition, this agent may be used in the treatment of obesity and obesity-linked health problems in postmenopausal women.

Picumeterol (GR114297A) is a potent and highly selective beta2-adrenoceptor agonist with a longer duration of action than salbutamol, but shorter than salmeterol. Picumeterol is the (R)-isomer of the racemic entity GR63411B, and picumeterol has been shown to be about 40 times more potent than the (S)-isomer (GR114744A) in various in vitro pharmacological models of beta2-agonist activity. Picumeterol is of potential value in the treatment of asthma and related diseases in man following inhalation administration. In the clinical studies, the bronchodilator potencies of picumeterol and GR 63411B were similar. However, both drugs were short-acting, which is at odds with their activity in vitro. These compounds display dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction.