Cipropride is an anti-emetic drug of the substituted benzamide class. It was discovered by Synthelabo in the early 1980s. The drug acts by blocking the dopamine receptor and thus affecting the chemo-receptor trigger zone for vomiting. Clinical trials showed that cipropride was effective for the prevention of nausea and vomiting induced by cytotoxic chemotherapy agents dacarbazine and Cis-platinum. The subsequent development of the drug was not reported.

Batanopride, previously known as BMY-25801, a 5-hydroxytryptamine 3 receptor antagonist, was studied against emesis for cancer patients that were treated by chemotherapy procedure. Batanopride had the dose-limiting side effects including hypotension and long QT syndrome that is why any further experiments for its medical application were discontinued.

FIGOPITANT is a tachykinin NK1 receptor antagonist. It can inhibit scratching behavior in an atopic dermatitis model. It is under investigation in clinical trials to obtain preliminary pharmacokinetics data and information about FIGOPITANT safety and tolerability in healthy volunteers.

FLUMERIDONE is an antiemetic agent.

Vestipitant, also known as GW597599, is a neurokinin1 receptor antagonist that was being developed by GlaxoSmithKline for the treatment of postoperative nausea and vomiting. Vestipitant is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It was under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitus and insomnia. Vestipitant was shown to improve sleep maintenance in patients with primary insomnia, with no associated next-day cognitive impairment. The effects on wake after sleep onset and total sleep time were maintained following repeated dosing. Vestipitant has anxiolytic properties and a good safety profile. Vestipitant was investigated for potential effect against chronic tinnitus as a stand-alone treatment and in conjunction with a selective serotonin reuptake inhibitor, paroxetine. Although well-tolerated vestipitant, alone or in combination with paroxetine, was not effective in ameliorating tinnitus in this patient group.

Mociprazine is a piperazinyl(propargyloxy)propanol derivative with antiemetic activity.

Tinisulpride is a sulfamoylbenzoic acid patented by Fabre, Pierre, S. A. as an antiemetic agent.

LANEPITANT is a selective nonpeptide antagonist for the neurokinin-1 receptor. It inhibits neurogenic dural inflammation. LANEPITANT was under development as a potential analgesic drug for the treatment of migraine, arthritis and diabetic neuropathy. However, it failed to show sufficient efficacy to support further development.

Levonantradol is a synthetic cannabinoid analogue of delta (9)-tetrahydrocannabinol (delta(9)-THC) administered intramuscularly. It has antiemetic and anti-analgesic properties. Although its precise mechanism of action is unknown, levonantradol appears to bind and activate the cannabinoid receptors CB1 and/or CB2. Antiemetic effect of levonantradol significantly superior to chlorpromazine. However, its adverse central effects limit its utility. The main adverse events are drowsiness and dizziness. Levonantradol, administered intramuscularly to the patients suffering from postoperative pain, manifested significant analgesic efficacy. Analgesia persisted for more than 6 h with the 2.5 and 3 mg doses of levonantradol. Drowsiness was frequent but few other psychoactive effects were reported.

Lintopride is a benzamide, eliciting prokinetic properties on the upper gut in several animal models. Lintopride increases gastric emptying, stimulates antral and duodenal motility and accelerates intestinal transit in animals. In canines it also increases lower oesophageal sphincter (LOS) pressure and reinforces peristaltic waves after wet swallowing, indicating a stimulatory action which could potentially be greater than that of metoclopramide. The 5HT-4 agonist lintopride increases LOS basal pressure and the amplitude of peristaltic waves of the oesophagus following a single intravenous dose in healthy subjects. The action of lintopride on LOS basal pressure and oesophageal peristaltic waves could be beneficial in patients with gastro-oesophageal reflux disease.