Sulrnazole (the former AR-L 115 BS) is a benzimidazole derivative with positive inotropic, positive chronotropic and vasodilator effects. Sulrnazole also has been shown to improve cardiac index and reduce pulmonary capillary wedge pressure without significant change in heart rate or arterial pressure. Intravenous administration caused a 217 per cent increase in cardiac output with a 25 per cent decrease in pulmonary wedge pressure. Short-term oral administration resulted in a 317 per cent increase in cardiac index and a 317 per cent increase in ejection fraction. Side effects have included visual blurring and transient colour blindness. Sulmazol has been demonstrated to improve regional wall motion in patients with ischemic heart disease and to abolish pacing-induced ischemia. Sulrnazole is an A1 adenosine receptor antagonist. It is also a phosphodiesterase inhibitor.

Spiramide (AMI-193) is a spiperone derivative, a selective 5-HT2A, (Ki = 2 nM) 5-HT1A (Ki = 50 nM), and D2 receptor (Ki = 3 nM) antagonist, with negligible affinity for the 5-HT2C receptor (Ki = 4300 nM). The ability of Spiramide to serve as a functional 5-HT2A antagonist in behavioral studies was demonstrated through studies in which Spiramide blocked the discriminative - stimulus effects of the 5HT2A agonist 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM).

Drinabant is a selective CB1 receptor antagonist under investigation varyingly as a treatment for obesity, schizophrenia, Alzheimer's disease, Parkinson's disease, and nicotine dependence. Drinabant may be useful to treat the cognitive deficits in schizophrenia and as a co-treatment with currently available antipsychotics. Coadministration of olanzapine and drinabant attenuated body weight gain, diminishing the enhanced food intake while maintaining increased energy expenditure and decreased motility. Sanofi has outlicensed global development and commercialization rights to drinabant to Opiant Pharmaceuticals, which said it plans to start developing the acute cannabinoid overdose (ACO) candidate in the 2019 year. Opiant said drinabant will be developed as an injectable for administration in an emergency department setting.

Adaprolol is a beta-adrenergic antagonist that is being developed as a topical agent to treat glaucoma. Adaprolol demonstrated a safer cardiovascular profile, especially in the population over 70 years old. It was in Phase II clinical trials for the treatment of glaucoma. This research has been discontinued.

Daltroban (also known as BM 13505, SKF 96148), a specific thromboxane A2 receptor antagonist, was studied as an antithrombotic agent. The drug was licensed to Smith Kline Beecham, underwent phase III clinical trials in the UK and Germany as an antithrombotic agent but did not enter clinical trials in the USA. Besides, вaltroban was investigated in patients with an ischemic heart disorder. However, the development of daltroban has been discontinued.

Atropine-N-oxide hydrochloride is an alkaloid of the belladonna plants. It is the major metabolite of atropine. It is a competitive nonselective antagonist at central and peripheral muscarinic acetylcholine receptors.

Olcegepant is a potent and selective CGRP (Calcitonin gene-related peptide) antagonist. The drug was tested in phase II clinical trial, in patients with a migraine, however, the development was terminated.

Ritolukast (WY 48252) is an aerosol leukotriene D4 (LTD4) receptor antagonist. This orally administered drug was developed for use in treatment of asthma. Ritolukast was shown to prevent and reverse bronchoconstriction produced by aerosol LTD4 in guinea pigs. This drug also inhibited the synthesis of eicosanoids in rats and was therefore concluded to have modulatory effects on the arachidonic acid metabolism.

Relcovaptan is a potent, orally active nonpeptide vasopressin V1a antagonist that was undergoing clinical development with Sanofi-Synthélabo (formerly Sanofi) in France. SR49059 is specifically and selectively antagonizes the effect of vasopressin on the V1a receptor in animals’ and in humans. The drug has been shown to have an excellent safety profile in single and repeated dose toxicological studies in animals. In the human uterus in vitro, SR49059 caused a dose-dependent inhibition of vasopressin V1a receptor-mediated activity of myometrial strips and isolated uterine arteries. In vivo in nonpregnant women, an inhibition of vasopressin-induced uterine activity has been observed.

Priralfinamide, also known as Ralfinamide, FCE-26742A; NW-1029; PNU-0154339E, is a Na-channel blocker for the treatment of neuropathic pain and other pain conditions such as post-operative dental pain. It has a relatively complex pharmacology, acting as a mixed voltage-gated sodium channel blocker (including Nav1.7), N-type calcium channel blocker, noncompetitive NMDA receptor antagonist, and monoamine oxidase B inhibitor. Priralfinamide is in phase Ⅲ clinical trials by Newron for the treatment of chronic neuropathic pain.