h1 receptor

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.

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

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.

Diphenhydramine hydrochloride (DPH) is a histamine H1 antagonist used as an antitussive and antiemetic. It is also used for pruritus and dermatoses, for hypersensitivity reactions, as an antiparkinson, a hypnotic, and as an ingredient in common cold preparations.

Trimipramine maleate (Surmontil maleate) appears to inhibit serotonin transport and norepinephrine uptake by nerve terminals. This increases available norepinephrine or serotonin and prolongs its action. Trimipramine Maleate is the maleate salt form of trimipramine, a tricyclic secondary amine of the dibenzazepine class, with an antidepressant property.

Levocarnitine propionate hydrochloride (ST-261) is used for the treatment of the deterioration of renal function, congestive heart failure, intermittent claudication, and other diseases.

Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

Sodium butanoate (Sodium Butyrate) is the sodium salt of butyrate with potential antineoplastic activity. Butyrate, a short chain fatty acid, competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).

Diphenhydramine (Syntedril), a first-generation antihistamine possessing antiemetic, antitussive, anticholinergic, and sedative properties, is mainly used in the treatment of allergies. Diphenhydramine is also used in the management of drug-induced parkinsonism and other extrapyramidal symptoms.

Desloratadine (Sch34117) is a long-acting piperidine derivate with selective H1 antihistaminergic and non-sedating properties. Desloratadine diminishes the typical histaminergic effects on H1-receptors in bronchial smooth muscle, capillaries and gastrointestinal smooth muscle, including vasodilation, bronchoconstriction, increased vascular permeability, pain, itching and spasmodic contractions of gastrointestinal smooth muscle. Desloratadine is used to provide symptomatic relieve of allergic symptoms.

Osthole (Osthol), a potential inhibitor of histamine H1 receptor, has been shown to stimulate osteoblast proliferation and differentiation.

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

Escitalopram (Seroplex) is a furancarbonitrile that is one of the SEROTONIN UPTAKE INHIBITORS used as an antidepressant. The drug is also effective in reducing ethanol uptake in alcoholics and is used in depressed patients who also suffer from tardive dyskinesia in preference to tricyclic antidepressants, which aggravate this condition.

Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.

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.

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.

Hydroxyzine (Hydroxyzine free base) is an antagonist of histamine H1-receptor.

(S)-(+)-Dimethindene maleate is an orally available, selective muscarinic M2 receptor and histamine H1 receptor antagonist that also inhibits muscarinic M1, M3, and M4 receptors.

AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values ​​of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.

Betahistine (Vasomotal) is a histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers. Betahistine dihydrochloride is an anti-vertigo drug. It is commonly prescribed for balance disorders or to alleviate vertigo symptoms associated with Ménière's disease.