antihistamine

Clemastine fumarate (Meclastine (fumarate)) is a synthetic ethanolamine with anticholinergic, sedative, and histamine H1 antagonistic properties.

Brompheniramine maleate (Dimotane) is an antagonist against histamine H1 receptors.

Triprolidine hydrochloride monohydrate is a histamine H1 antagonist used in allergic rhinitis, asthma.

Meclizine dihydrochloride (NSC28728) is a histamine H1 antagonist used in the treatment of motion sickness, vertigo, and nausea during pregnancy and radiation sickness.

Ebastine (Kestine) (trade names Evastin, Kestine, Ebastel, Aleva) is a non-sedating H1 antihistamine. It does not penetrate the blood-brain barrier and thus allows an effective block of the H1 receptor in peripheral tissue without a central side effect, i. e not causing sedation or drowsiness.

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.

Epinastine hydrochloride (WAL-801CL HCl) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.

Cyproheptadine hydrochloride is an effective orally active 5-HT2A receptor antagonist with antidepressant, anti-serotonin, and antiplatelet activities. It can be used for research on thromboembolic diseases and for the establishment of diabetes models.

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

Azelastine hydrochloride (Astelin) is a phthalazinone derivative with antihistaminergic activity.

Bromodiphenhydramine hydrochloride is a new antihistaminic in the control of cutaneous.

Dioxopromethazine (Dioxoprothazine) is a drug for the treatment of a cough and expectoration. It also can be used in local anesthesia.

Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic activity. It is a selective antagonist of mycotoxins M1 receptors, exhibiting high (Ki=84 nM, M1 receptors) and low (Ki=1.65 μM, M2 receptors) affinity, with a 20-fold difference. Oxomemazine is an antihistamine and anticholinergic agent used in cough studies[1][2].

Antihistamine-1 is an H1-antihistamine (Ki: 6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel (IC50s: 5.4 and 0.8 μM).

Mizolastine (SL 850324) (IC50= 47 nM) is a histamine H1-receptor antagonist.It is used in the treatment of allergic reactions such as hay fever (seasonal allergic rhinitis), hives.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

Benztropine mesylate (Benztropine methanesulfonate) is a centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.

Oxatomide (Oxatomida) is a potent and orally active dual H1 histamine receptor and P2X7 receptor antagonist with antihistamine and antiallergic activity.Oxatomide can be used to block ATP-induced currents in the human P2X7 receptor with an IC50 value of 0.95 μM.Oxatomide has an inhibitory effect on ATP-induced Ca2+ inward currents with an IC50 value of 0.43 μM.Oxatomide inhibits 5-hydroxytryptamine. Oxatomide inhibits 5-hydroxytryptamine with an IC50 of 0.43 μM.Oxatomide is used in the treatment of immune system diseases and in the study of hypersensitivity reactions.

Noberastine (R 64947) is a novel histamine H1 antagonist with potent and specific peripheral antihistamine activity.

Vapitadine is a non-sedative antihistamine compound that relieves itching caused by atopic dermatitis.

Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.

Talastine is an antihistamine compound that can induce an allergic rash.

Antazoline hydrochloride (Phenazoline hydrochloride), a first-generation antihistamine, can bind to the histamine H1 receptor and block the action of endogenous histamine.

Mebhydrolin napadisylate (Incidal) is an antihistamine used to relieve allergic symptoms caused by histamine release, including nasal allergies and allergic dermatosis.