Imiclopazine is a phenothiazines derivative patented by Asta-Werke A.-G. as strong sedative and antiemetic agent. Imiclopazine was studied for treatment of schizophrenia but was never marketed.

Duoperone is a neuroleptic agent. Duoperone blocked d-amphetamine lethality in mice under aggregated conditions when the pretreatment interval was between one hour and seven days. Conditioned avoidance responding in mice and cats was suppressed by duoperone in doses that did not impair escape behavior. Duoperone produced catalepsy in rats. The onset of this effect was delayed and the duration was prolonged when compared with that of chlorpromazine. It was a potent antiemetic agent in dogs, with a delayed onset and prolonged duration of action.

Nonabine is a chromenol structurally related to the cannabinoids which has shown antiemetic efficacy in clinical trials. Nonabine also produced sedative clinical effects, but with an EEG profile which resembled that reportedly caused by cannabinoids. In contrast to cannabinoids, nonabine did not cause changes of mood or perception, suggesting that nonabine lacks the potential for social abuse at antiemetic doses. Nonabine was studied in the 1980s for the prevention of nausea and vomiting associated with cancer chemotherapy.

IPROZILAMINE, a member of 4-piperazinopyrimidines, has powerful antiemetic activity. It also exhibits a relaxant effect on smooth muscle fiber.

(4-AMINO-5-CHLORO-2-METHOXYPHENYL)[4-(1,3-BENZODIOXOL-5-YLMETHYL)-1-PIPERAZINYL]METHANONE (peralopride) is a tranquilliser, antidepressant.

Burapitant (SSR-240,600) is a drug developed by Sanofi-Aventis which was one of the first compounds developed that acts as a potent and selective antagonist for the NK1 receptor. Burapitant inhibited the binding of radioactive substance P to tachykinin NK1 receptors in human lymphoblastic IM9 cells, human astrocytoma U373MG cells, and human brain cortex. It also showed a subnanomolar affinity for guinea pig NK1 receptors but was less potent on rat and gerbil NK1 receptors. Burapitant inhibited [Sar(9),Met(O2)(11)]substance P-induced inositol monophosphate formation in human astrocytoma U373MG cells. Burapitant (0.1-10 mg/kg i.p. or p.o.) antagonized the excitatory effect of i.c.v. infusion of [Sar(9),Met(O2)(11)]substance P (SP) on the release of acetylcholine in the striatum of anesthetized and awake guinea pigs. This antagonistic action was still observed after repeated administration of Burapitant (5 days, 10 mg/kg p.o., once a day). Burapitant (10 mg/kg i.p.) inhibited the phosphorylation of the cAMP response element-binding protein in various brain regions induced by i.c.v. administration of [Sar9,Met(O2)(11)]SP. While burapitant itself did not proceed beyond early clinical trials and was never developed for clinical use in humans, promising animal results from this and related compounds have led to a number of novel drugs from this class that has now been introduced into medical use.

Lerisetron is a 5-hydroxytryptamine3 receptor antagonist. It was under development by FAES Farma for the potential treatment of emesis resulting from chemotherapy. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting. Lerisetron had been in phase III clinical trials for the treatment of emesis. However, this study was discontinued.

Etaminile is an antitussive agent.

Telmapitant, a neurokinin NK1 antagonist, was developed as an anti-emetic agent that has never been marketed. Information about the current use of the telmapitant is not available.