histamine h1-receptor

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.

Thiethylperazine dimaleate (Thiethylperazine maleate) is an antagonist of the D2 receptor and H1 receptor. Thiethylperazine dimaleate is an activator of ABCC1 and possesses antimicrobial, anti-emetic, and antipsychotic effects.

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].

ReN 1869 hydrochloride is a novel and selective histamine H1 receptor antagonist.

Pirolate is a receptor of histamine H1.

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.

(±)-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.

Pradigastat (LCQ-908) is an orally active, potent and selective diacylglycerol acyltransferase 1 (DGAT1) inhibitor for the treatment of constipation, which may be used in the study of obesity and diabetes.

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

Bamirastine inhibits ligand binding to recombinant human histamine H1 receptor (rhH1R) with an IC50 of 17.3 nM and possesses an inhibitory effect on allergic skin inflammation.

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.

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.

Vapitadine dihydrochloride(R-129160 2HCl) is a novel, potent, selective and non-sedating compound with inhibitory effects on histamine H1.

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

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

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

Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.

Ziprasidone hydrochloride (CP-88059 hydrochloride) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of antipsychotic activity.

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.

Chlorprothixene (Truxal) is a typical antipsychotic drug of the thioxanthene class, which was the first of the series to be synthesized.