h1 histamine receptor

(±)-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.

Paliperidone (9-hydroxyrisperidone)(Invega) is used as an atypical antipsychotic. It applies to the acute and maintenance treatment of schizophrenia. Chemically, paliperidone is the primary active metabolite of the older atypical antipsychotic risperidone.

Cetirizine dihydrochloride (UCB P071) is an effective second-generation histamine H1 antagonist that is potent in the therapy of allergic rhinitis, confirmed urticaria, and pollen-induced asthma. Unlike other conventional antihistamines, it does not cause side effects of drowsiness or anticholinergic.

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

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.

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

Maprotiline hydrochloride (Psymion) is a bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.