Histamine Receptor

Oxmetidine (SKF 92994) is a novel H2 receptor antagonist that is cytotoxic. Oxmetidine inhibits transmembrane calcium flux in cardiac and vascular tissues and is used in the treatment of active duodenal ulcers.

Bepotastine (Bepotastine free base) free base is a histamine 1 (H1) receptor antagonis.

Clemizole, an H1 histamine receptor antagonist, inhibits NS4B's RNA binding and hepatitis C virus (HCV) replication.

CHLORCYCLIZINE is a histamine H1 antagonist and a potent hepatitis C virus (HCV) entry inhibitor.

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.

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.

ABT-288 is a selective and potent H3 antagonist for the treatment of mild to moderate Alzheimer's dementia.

Lodoxamide (Lodoxamidum) is an antiallergic drug acting as a mast-cell stabilizer. It is effective in the treatment of asthma and allergic conjunctivitis.

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).

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

Nepetin (6-Methoxyluteolin) has antioxidant activity, it is a potent inhibitor of histamine release and calcium influx via down-regulation of the FcεRI α chain.

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.

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.

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

Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties. Amitriptyline is widely used to treat depression and neuropathic pain.

(±)-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.

ICI 162,846 is an orally active and potent H2 receptor antagonist that inhibits gastric secretion and may be used in the study of duodenal ulcers.

Acrivastine (Acrivastin) is a short-acting histamine 1 receptor antagonist.

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

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

JNJ-39220675 (JNJ 39220675) is a selective and brain permeable histamine H3 receptor antagonist.

Thonzylamine hydrochloride (Resistab) is an anticholinergic and antihistamine used as an antipruritic.

Meclizine, also known as Meclozine, is a piperazine class H1 antagonist with antihistamine properties that inhibits the interaction of histamine at H1 receptors reversibly. It serves as an effective anti-motion sickness agent, able to cross the blood-brain barrier. Additionally, Meclizine acts as an agonist ligand for the mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR, making it useful in research on polyQ toxicity disorders, including Huntington's disease.

Carebastine, the active metabolite of Ebastine, is an antagonist of the histamine H1 receptor.

Ranitidine (HSDB 3925) is a non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.

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

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.

Mifentidine (DA 4577) is an orally available H2 receptor antagonist for the study of gastric emptying and experimental gastric and duodenal ulcers.

Fexofenadine (Carboxyterfenadine), an antihistamine pharmaceutical drug, is used to treat allergy symptoms, such as nasal congestion, hay fever, and urticaria. Compared to first-generation antihistamines, Fexofenadine is less able to pass the blood-brain barrier and cause sedation.

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

BMY 25368 HCl is a competitive histamine H2 receptor antagonist that antagonizes gastric secretion stimulated by pentagastrin, ethacrynic choline, and food.

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.

Metoprine is a potent inhibitor of histamine N-methyltransferase (HMT), with potential antineoplastic activity.

Thioperamide maleate (MR-12842 maleate) is an effective and selective H3 receptor antagonist (Ki = 4.3 nM) that inhibits [3H]histamine synthesis (Ki = 31 nM).

Bilastine (Bilaxten) is a novel new-generation antihistamine that is highly selective for the H1 histamine receptor, has a rapid onset and prolonged duration of action.

Quinacrine dihydrochloride (Mepacrine dihydrochloride) is the dihydrochloride salt of the 9-aminoacridine derivative quinacrine with potential antineoplastic and antiparasitic activities.

Samelisant (SUVN-G3031) is a selective and inverse agonist of H3 receptor with Kis of 8.7 nM and 9.8 nM for human and rat. Samelisant has anticataplectic effects and can be used in studies about narcolepsy.

Mirtazapine (6-Azamianserin) is a tetracyclic antidepressant with a somewhat unique mechanism of action. Mirtazapine therapy can be associated with transient asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent acute liver injury.

Clemastine (Meclastin) is an antagonist of the H1 receptor and exhibits anti-inflammatory effects.

Psoralenoside is a natural product isolated from the fruits of Psoralea corylifolia, shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

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

Conessine (Conessinum), a steroidal alkaloid isolated from Holarrhena floribunda, interacts with the histamine H3 receptor and has anti-malarial activity.

Pitolisant hydrochloride (Ciproxidine) is a potent and selective inverse agonist of the histamine H3 receptor(Ki : 0.16 nM).

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

Protopine (Fumarine) is a benzylisoquinoline alkaloid. It has been found to inhibit histamine H1 receptors and platelet aggregation, and acts as an analgesic.

Ritanserin (R 55667) is a long-acting, highly potent, relatively selective, orally bioavailable 5-HT2 receptor antagonist with an IC50 of 0.9 nM.

Lodoxamide tromethamine is a mast cell stabilizer with anti-allergic properties and can be used in studies about the treatment of asthma and allergic conjunctivitis.

Cetirizine Impurity B dihydrochloride (De(carboxymethoxy) Cetirizine Acetic Acid Dihydrochloride) is an impurity of Cetirizine dihydrochloride. Cetirizine is a second-generation antihistamine. Cetirizine is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.