antiemetic

Pheniramine maleate (Trimetose), an alkylamine derivative with antihistaminic and vasodilatory properties, binds to histamine H1 receptors, thereby inhibiting phospholipase A2 and production of the endothelium-derived relaxing factor, nitric oxide.

Netupitant (CID 6451149) is a specific neurokinin 1 (NK1) receptor antagonist (Ki: 0.95 nM).

Domperidone (R33812)(Motilium) is a dopamine blocker and an antidopaminergic reagent. It blocks the action of. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which - among others - regulates nausea and vomiting (area postrema on the floor of the fourth ventricle and rhomboid fossa).

Rolapitant (SCH619734) Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy. Compared to other NK1-receptor antagonists, rolapitant has both a more rapid onset of action and a much longer half-life.

Cipropride S enantiomer is the S enantiomer of cipropride which is an antiemetic drug.

Duoperone is a neuroleptic agent. Duoperone shows antiemetic activity in animal models.

Benzquinamide (P2647), an antiemetic agent with anticancer activity, inhibits p-glycoprotein-mediated drug efflux and potentiates the cytotoxicity of anticancer drugs in multidrug-resistant cells.The Ki values of Benzquinamide for α2A, α2B, and α2C adrenergic receptor (α2-AR) were 1,365, 691, and 545 nM, respectively. 545 nM, respectively.

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

ADR-851 free base (ADR 851 free base) is a 5-HT3 receptor antagonist and a novel antiemetic with analgesic activity.

Itasetron (U 98079A) is a 5-hydroxytryptamine 3-receptor antagonist used to prevent age-related memory deficits in rats.Itasetron's antiemetic activity in animal models of cancer chemotherapy and radiation therapy may be useful in the study of amnesia.

Nonabine is a compound with strong antiemetic properties that can be used to prevent nausea and vomiting associated with cancer chemotherapy.

Litoxetine is a selective 5-HT uptake inhibitor and is a 5-HT3 receptor antagonist. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. Litoxetine (1 and 10 mg/kg i.v.) dose-dependently reduced the number of regurgitations and vomiting and delayed the onset of vomiting. Litoxetine has an affinity for brain 5HT3 receptors (Ki = 85 nM).

Benzoquinamide hydrochloride (3-carbamoyl-N,N-diethyl-1,3,4,6,7,11b-hexahydro-9,11-dimethoxy-2H-benzo[a]quinolizin-2-yl acetate hydrochloride) is an antiemetic agent and increases intra-arterial pressure due to the increased peripheral vascular resistance.

Hydroxyzine Pamoate (Bobsule) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Diphenhydramine hydrochloride (DPH) is a histamine H1 antagonist used as an antitussive and antiemetic. It is also used for pruritus and dermatoses, for hypersensitivity reactions, as an antiparkinson, a hypnotic, and as an ingredient in common cold preparations.

Promazine hydrochloride (Romtiazin hydrochloride) is a phenothiazine with actions similar to CHLORPROMAZINE but with less antipsychotic activity. It is primarily used in short-term treatment of disturbed behavior and as an antiemetic.

Phenothiazine (ENT 38) is a class of agents exhibiting antiemetic, antipsychotic, antihistaminic, and anticholinergic activities. Phenothiazines antagonize the dopamine D2-receptor in the chemoreceptor trigger zone (CTZ) of the brain, potentially preventing chemotherapy-induced emesis.

Diphenidol hydrochloride (Difenidol hydrochloride), a muscarinic antagonist, is employed as an anti-vertigo and as an antiemetic drug.

Cinnarizine (Stugeron) is a piperazine derivative having histamine H1-receptor and calcium-channel blocking activity with vasodilating and antiemetic properties but it induces PARKINSONIAN DISORDERS.

Granisetron hydrochloride (Granisetron HCl) is a serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.

Metoclopramide hydrochloride (Metoclopramide HCl) is a selective dopamine D2 receptor antagonist, used as an antiemetic.

Tropisetron hydrochloride (Tropisetron HCl) is the hydrochloride salt form of tropisetron, a selective, competitive serotonin 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist, with antinauseant and antiemetic activities.

Bromopride (Valopride) is a dopamine antagonist with prokinetic properties closely related to metoclopramide, and is widely used as an antiemetic. It is not available in the United States or the United Kingdom.

Trifluoperazine dihydrochloride (SKF5019) is a potent dopamine D2 receptor inhibitor used as an antipsychotic and an antiemetic.