Itopride is a dopamine D2 receptor antagonist and inhibitor of acetylcholinesterase. It is indicated in the for the treatment of gastrointestinal symptoms caused by reduced gastrointestinal motility, such as functional non-ulcer dyspepsia (chronic gastritis), gastric fullness, rapid satiation, pain or discomfort in the upper abdomen, anorexia, heartburn, nausea, and vomiting. The drug is not approved in the USA or UK but is available in Japan and Western European countries.

Tiemonium (often used in a form of iodide or methylsulphate salt) is a muscarinic acetylcholine receptor antagonist, which is available in Asia (mainly Bangladesh) for the alleviation of muscle spasms of the intestine, biliary system, uterus and urinary bladder in gastrointestinal, biliary, urinary and gynecological diseases.

Proroxan is a non-selective а-adrenoblocker. Proroxan was found to prevent the development of hypertensive crises and improve cerebral bioelectrical parameters in most of hypertensive patients. Proroxan has been used as an antihypertensive and in the treatment of Ménière’s disease, motion sickness, and allergic dermatitis.

Minaprine, a psychotropic drug, which was effective in the treatment of various depressive states. This drug was withdrawn because of the serious side effect. It was found, that minaprine inhibited the following enzymes, acetylcholinesterase and monoamine oxidase (MOA) A. It also binds to dopamine D1 and D2 receptors. Experiments on rodents also have revealed that minaprine suppressed the inhibitory effect of hydroxytryptamine (5-HT) on dopamine (DA) release via the inhibition of 5-HT binding at the 5-HT2 receptor on the nerve terminal.

The anticholinergic agent Flutropium is a classic competitive antagonist of acetylcholine. In in vitro experiments it is more effective than atropine. A poor enteral absorption is to be expected; this can be concluded from the low relative effectiveness after oral administration. After local administration as an aerosol it is superior to atropine with regard to both effectiveness and duration of action. It is used in Japan to treat asthma and chronic obstructive pulmonary disease. Flutropium can be described as a preparation which is free of side effects.

Atosiban (brand name Tractocile) is a competitive antagonist of human oxytocin at receptor level. In rats and guinea pigs, atosiban was shown to bind to oxytocin receptors, to decrease the frequency of contractions and the tone of the uterine musculature, resulting in a suppression of uterine contractions. Atosiban was also shown to bind to the vasopressin receptor, thus inhibiting the effect of vasopressin. Tractocile is indicated to delay imminent pre-term birth in pregnant adult women with: − regular uterine contractions of at least 30 seconds duration at a rate of ≥ 4 per 30 minutes − a cervical dilation of 1 to 3 cm (0-3 for nulliparas) and effacement of ≥ 50% − a gestational age from 24 until 33 completed weeks − a normal foetal heart rate. Atosiban does not have U.S. Food and Drug Administration (FDA) approval for use in the United States.

Vapiprost is a potent dicyclopentadiene thromboxane receptor antagonist that was being developed by Glaxo Wellcome in Japan. Vapiprost has been shown to be a potent and specific thromboxane (Tx)A2 receptor blocking drug in vitro using platelets and both vascular and airways smooth muscle preparations from different species. The drug is active in various experimental models of thrombosis. The potential clinical applications for a thromboxane receptor blocking drug include the treatment of thrombotic events and occlusive vascular disease. Phase III trials were underway in Japan for the treatment of deep vein thrombosis, which later were discontinued.

Aptiganel (CNS 1102, Cerestat), a selective ligand with antagonized properties for the ion-channel site of the N-methyl-D-aspartate receptor-channel complex, was developed as a neuroprotective agent for focal brain ischemia. However, in the clinical trials in patients with acute ischemic stroke aptiganel was not efficacious at either of the tested doses and may be harmful. That is why its further study was discontinued.

Beraprost is a stable, orally active prostacyclin analogue. Beraprost acts by binding to prostacyclin membrane receptors ultimately inhibiting the release of Ca2+ from intracellular storage sites. This reduction in the influx of Ca2+ has been postulated to cause relaxation of the smooth muscle cells and vasodilation. Beraprost is indicated for the treatment of pulmonary hypertension and improvement of ulcers, pain & feeling of coldness associated with chronic arterial occlusion. In addition beraprost displays thyroid hormone receptor antagonistic properties.

Bevonium is a parasympatolytic antimuscarinic compound. It possesses spasmolytic properties. The use of the drug is discontinued.