Nolpitantium (SR-140333) is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extravasation in rats. Nolpitantium was found to be effective in the modulation of the inflammatory response and airway remodeling in mice. Nolpitantium is reported to cause antagonism of the SP-induced relaxations of human isolated intralobar pulmonary arterial rings. Nolpitantium also blocked the activation of rat thalamic neurons after nociceptive stimulation. Nolpitantium has been shown to reduce the severity of inflammation in trinitrobenzene sulfonic acid-induced colitis in the rat colon. Nolpitantium inhibited mustard oil-induced plasma protein extravasations in the dorsal skin of the rat hind paw. Nolpitantium had been in some phase II clinical trials but further studies were discontinued.

Toloconium methylsulphate is a quaternary ammonium antiseptic which has been used in infections of the mouth.

Ethomoxane is antagonist of alpha-adrenoreceptor exerting antihypertensive properties.

Clazosentan is an endothelin receptor antagonist, developed by the Swiss pharmaceutical company Actelion, and licensed to its spin-off, Idorsia. The drug was designed to inhibit endothelin-mediated cerebral vasospasm and associated delayed ischaemic neurological deficit. The drug has been investigated in a phase III clinical trials in patients with aneurysmal subarachnoid hemorrhage. Clazosentan at 5 mg/h had no significant effect on mortality and vasospasm-related morbidity or functional outcome. Clinical investigation of a higher dose of the drug is underway.

Dabuzalgron is an orally active and selective alpha1A/1L-adrenoreceptor partial agonist, developed by Roche. In anesthetized micropigs and rabbits, dabuzalgron produced non-selective, dose-dependent increases in intraurethral and arterial blood pressures. In conscious micropigs, both agents produced dose-dependent increases in urethral tension. Dabuzalgron was investigated in a clinical study in women with stress urinary incontinence (SUI). It was demonstrated that 1.5 mg of the drug administered twice daily lead to a significantly lower mean weekly number of SUI episodes with little or no cardiovascular effect. Despite positive results, no development of the drug was reported by Roche.

Esproquine is a tetrahydroisoquinoline derivative. It exerts positive inotropic effect and increases arterial pressure.

Elinogrel, previously known as PRT060128 or PRT128, is a direct-acting, reversible P2Y12 inhibitor for both intravenous and oral administration. Elinogrel has been tested in 2 phase II studies for the treatment of acute coronary syndrome, myocardial infarction and prevention of secondary thrombotic events. Elinogrel therapy was associated with an increased incidence of dyspnea and incidence of elevated liver transaminases. The development of the drug was terminated in January 2012 by Novartis.

1,​2-​Dioleoyl-​sn-​glycero-​3-​phospho-​L-​serine Sodium Salt is a lipid being studied in the assembly and long-term stability of solid supported lipid bilayers from artificial and natural lipid mixtures.

Fantridone is an antidepressant.

Tetronasin is a furanone derivative patented by Imperial Chemical Industries Ltd. as antibiotic and feed additive for ruminants. Tetronasin acts as divalent antiporter that binds preferentially with Ca2+ or Mg2+ and inhibits anaerobic fungi and Gram-negative bacteria in vitro.