h1 receptor antagonist

(±)-Tazifylline is a selective and long-acting antagonist of histamine H1 receptor. Tazifylline shows much lower affinity for H2 receptors, α- and β-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes.

QF0301B is a potent α1-adrenergic receptor antagonist with inhibitory effects on α2-adrenergic receptors, 5-HT2A and histamine H1 receptors.

Wy 49051 is an orally active antagonist of H1 receptor(IC50 of 44 nM).

Rocastine (AHR-11325) is a selective and potent non-sedating H1 receptor antagonist.

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.

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

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

Fenclozine Maleate (S 1429) is a potential histamine H1 receptor antagonist , which can be used to study fever, inflammation and pain.

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.

Promethazine hydrochloride (Promethazine HCl) , the first-generation antihistamine, is a strong antagonist of the H1 receptor and a moderate antagonist of the mACh receptor, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

Loratadine (SCH 29851) is a second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.

Doxylamine Succinate is a pyridine derivate histamine H1 antagonist with pronounced sedative properties. Doxylamine succinate (Decapryn) competitively blocks the histamine H1 receptor and limits the typical allergic and anaphylactic responses, including bronchoconstriction, vasodilation, increased capillary permeability, and spasmodic contraction of the gastrointestinal smooth muscle, caused by actions of histamine on bronchial and gastrointestinal smooth muscles, and on capillaries. This drug also prevents histamine-induced pain and itching of the skin and mucous membranes.

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.

Levocetirizine Dihydrochloride (Xyzal Dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Acting as an antihistaminic agent, it specifically targets the histamine H1-receptor. Levocetirizine Dihydrochloride is the R-enantiomer of Cetirizine, which gives it a higher affinity for the H1-receptor than the S-enantiomer. Due to this enhanced affinity, Levocetirizine Dihydrochloride is effective in treating allergic rhinitis and chronic idiopathic urticaria.

Alcaftadine (Lastacaft) is an H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis.

Bepotastine Besilate (TAU 284) is a non-sedating and selective H1 receptor antagonist (pIC50: 5.7).

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.

Mebhydrolin (Mebhydroline) is a specific histamine H1 receptor antagonist.

Emedastine (LY188695) is a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. Emedastine reversibly and competitively blocks histamine by binding to H1 receptors, thus blocking its downstream activity. As a result this agent interferes with mediator release from mast cells either by inhibiting calcium ion influx across mast cell basophil plasma membrane or by inhibiting intracellular calcium ion release within the cells. In addition, emedastine may also inhibit the late-phase allergic reaction mediated through leukotrienes or prostaglandins, or by producing an anti-platelet activating factor effect. Upon ocular administration, emedastine causes a dose-dependent inhibition of histamine-stimulated vascular permeability in the conjunctiva. Emedastine does not affect adrenergic, dopamine, or serotonin receptors.

Epinastine (WAL801), a potent, selective, and orally-active antihistamine and mast cell stabilizer, functions as a histamine H1 receptor antagonist. It also inhibits IL-8 release from human eosinophils, showcasing antiallergic action [1] [2] [3] [4].

Niaprazine is a histamine H1-receptor antagonist exhibiting significant sedative properties.

Quetiapine (ICI204636) is used for the therapy of schizophrenia, and for the treatment of acute manic episodes associated with bipolar I disorder. The mechanism of quetiapine' action is thought by mediated through antagonist activity at serotonin and dopamine receptors. Specifically, the D1 and D2 dopamine, the α1 adrenoreceptor and α2 adrenoreceptor, and 5-HT1A and 5-HT2 serotonin receptor subtypes are antagonized. Quetiapine also can inhibit the histamine H1 receptor.

Chloropyramine hydrochloride (Alergosan) is a histamine receptor H1 antagonist.

Alimemazine (Trimeprazine) is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist. Alimemazine also acts as a partial agonist against the histamine H1 receptor (H1R) and other GPCRs.