anti-histamine

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.

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

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

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.

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.

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

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

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.

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

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.

D18024 belongs to phthalazinone derivatives and is a histamine H1 receptor antagonist with anti-allergic activity. This compound exhibits good selectivity and cell permeability, and can be used in research on allergic diseases such as chronic spontaneous urticaria.

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

KP136 (AL136) is an orally active anti-allergic compound that inhibits histamine release and is used in studies of asthma and allergic edema.

Tecastemizole (R 43512) is a selective antagonist of H1 receptor and a major metabolite of astemizole with anti-inflammatory effects.

DF-1111301 is a novel anti-allergic compound with anti-histamine H1 and anti-PAF activity.

ReN-1869 is a novel selective histamine H(1) receptor antagonist with anti-neurogenic pain and anti-inflammatory activity for the study of neurological diseases.

ST-1006, a potent histamine H4 receptor agonist (pKi: 7.94), exhibits significant anti-inflammatory and anti-pruritic effects. It is also a potent inducer of basophil migration.