antiemetic

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

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

Ricasetron (Brl 46470) is a 5-HT3 receptor antagonist with pro-axonal lysis and antiemetic properties, and is used in the study of anxiety and anxiety disorders.

Ramosetron is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting. It is believed to have higher potency and longer antiemetic action than other 1st generation 5-HT3 antagonists such as ondansetron. Ramosetron is also indicated for a treatment of diarrhea-predominant irritable bowel syndrome in males . It is only licensed for use in Japan and selected Southeast Asian countries.

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.

Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.

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

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

N-desmethylmirtazapine (J1.061.658A) is a metabolite of mirtazapine. N-desmethylmirtazapine is also commonly used as an anxiolytic, hypnotic, antiemetic, and appetite stimulant.

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.

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

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

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

Triflupromazine is a phenothiazine drug used as an antipsychotic and antiemetic.

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

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.

Diphenidol, a muscarinic antagonist, is employed as an antivertigo and antiemetic agent.

2-Methoxybenzoic acid (o-Anisic acid) is a novel antiemetic which prevents nausea and vomiting in humans.

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, the water-soluble, N-phosphorylated prodrug of aprepitant, with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent binds selectively to the human substance P/neurokinin 1 (NK1) receptors in the central nervous system (CNS). This inhibits receptor binding of the endogenous substance P and prevents substance P-induced emesis.

Lerisetron is an antagonist of serotonin type 3 (5-HT3) receptor, with antiemetic activity.

Vestipitant, also known as GW597599, 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 is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.

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).

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.

Alimemazine hemitartrate (Trimeprazine hemitartrate) is aphenothiazine derivative that is used as an antipruritic. It also acts as a sedative, hypnotic, and antiemetic for prevention of motion sickness.

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.

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.

Hydroxyzine dihydrochloride-d4 is a deuterated compound of Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride has a CAS number of 2192-20-3. Hydroxyzine hydrochloride 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.

Mianserin-d3 is a deuterated compound of Mianserin. Mianserin has a CAS number of 24219-97-4. Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.

ProMazine-d6 hydrochloride is a deuterated compound of ProMazine hydrochloride. ProMazine hydrochloride has a CAS number of 53-60-1. Promazine 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.

Ondansetron-13C-d3 the 13C and deuterated compound of Ondansetron. Ondansetron has a CAS number of 99614-02-5. Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.

Trimethobenzamide (Ro 2-9578 free base) is a D2 receptor antagonist and an antiemetic agent. Primarily utilized to mitigate the occurrence of nausea and vomiting, trimethobenzamide effectively blocks the D2 receptor.

Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) 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.

Trimethobenzamide hydrochloride (Ro 2-9578) is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.

Granisetron, a serotonin receptor (5HT-3 selective) antagonist, is used as an antinauseant and antiemetic for cancer chemotherapy.

Arazasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27.

Methiomeprazine is an antiemetic agent.

Naboctate is a synthetic cannabinoid receptor agonist. It has antiemetic, sedative, anxiolytic and anti-glaucoma properties.

Alizapride is an antagonist of dopamine receptor. Alizapride can be used in human digestive disorders which is a potent antiemetic [1] [3].

Perphenazine-d4 is a deuterated compound of Perphenazine. Perphenazine has a CAS number of 58-39-9. Perphenazine is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

DAT 582 is a novel serotonin3 receptor antagonist. It is also an effective and long-lasting antiemetic agent

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.

Dazopride is an antiemetic agent.

Rolapitant Hydrochloride is the hydrochloride salt form of rolapitant, an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity.

Nabitan hydrochloride is a synthetic cannabinoid analog with antiemetic and analgesic effects. It may bind to and activate the CB1 and CB2 cannabinoid receptors. It also reduces intraocular pressure and may be useful in treating glaucoma.

Levonantradol is a synthetic cannabinoid analog of dronabinol (Marinol). It shows antiemetic and analgesic effects via activation of CB1 and CB2 cannabinoid receptors.

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.

Buclizine dihydrochloride (Buclina) is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine dihydrochloride binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine dihydrochloride exerts its anti-emetic effect by binding to and blocking the muscarinic and histamine receptors in the vomiting center of the central nervous system (CNS). This may prevent activation of the chemoreceptor trigger zone (CTZ) and may reduce nausea and vomiting.

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

Metoclopramide (5-Chloro-2-methoxyprocainamide) is a dopamine D2 antagonist which has been used for treatment of a variety of gastrointestinal symptoms over the last thirty years. In various countries, metoclopramide is the antiemetic drug of choice in pregnant women. Findings provide reassurance regarding the safety of metoclopramide for the fetus when the drug is given to women to relieve nausea and vomiting during pregnancy. Evidence also supports its use for gastroparesis (poor stomach emptying) and gastroesophageal reflux disease. It appears to bind to dopamine D2 receptors where it is a receptor antagonist, and is also a mixed 5-HT3 receptor antagonist/ 5-HT4 receptor agonist.