Histamine Receptor

Ritanserin (R 55667) is a highly effective, relatively selective, long-acting antagonist of 5-HT2 receptor (IC50: 0.9 nM), less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.

AVN-101 is a potent 5-HT7 receptor antagonist.

Pitolisant (Tiprolisant) is a selective and potent non-imidazole recombinant human histamine H3 receptor antagonist for the study of excessive daytime sleepiness and sudden collapse in patients with episodic narcolepsy.

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

Mianserin hydrochloride (Org GB 94) is a tetracyclic compound with antidepressant effects. it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. It may cause drowsiness and hematological problems.

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

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

Trazodone hydrochloride (Trazodone HCl) is a serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety.

Famotidine (MK-208) is a propanimidamide and histamine H2-receptor antagonist with antacid activity. As a competitive inhibitor of histamine H2-receptors located on the basolateral membrane of the parietal cell, famotidine reduces basal and nocturnal gastric acid secretion, resulting in a reduction in gastric volume, acidity, and amount of gastric acid released in response to various stimuli.

N-Acetylhistamine (N-Omega-acetylhistamine) is a metabolite of histamine.

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

Pimethixene (Calmixen) is a highly potent 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors antagonist(pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively).

S 38093 is a novel brain-penetrant antagonist/inverse agonist of H3 receptors.

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

Oxmetidine FA is an orally available specific histamine H2 receptor antagonist with antiulcerogenic properties.

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

LY-2624803 is a 5-HT2A receptor antagonist and histamine receptor inverse agonist that can be used to improve slow wave sleep.

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

(±)-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.

Vapitadine is a non-sedative antihistamine compound that relieves itching caused by atopic dermatitis.

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.

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

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

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

Linetastine (TMK-688) is a 5-lipoxygenase inhibitor (5-LOX) that inhibits leukotriene production and antagonizes the effects of histamine.Linetastine is used in studies of asthma, atherosclerosis, and peptic ulcers.

Dioxopromethazine is a target-based classification of drug and available in a number of countries worldwide.

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.

Noberastine (R 64947) is a novel histamine H1 antagonist with potent and specific peripheral antihistamine activity.

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.

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

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

GSK-239512 is an antagonist of H3 receptor and can be used in studies about the treatment of cognitive dysfunction in neurodegenerative disorders.

Carcinine ditrifluoroacetate Acetate (β-Alanylhistamine dihydrochloride) is an H3 receptor antagonist.

JNJ 10191584 maleate (VUF6002 maleate) is an orally active and selective antagonist of H4 receptor (Ki = 26 nM). JNJ 10191584 maleate inhibits chemotaxis of eosinophils and mast cells (IC50 = 530 nM and 138 nM).

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

Enerisant HCl is a novel potent and selective histamine H3 receptor antagonist, a substrate for P-gp, mediated by cytochrome P450 (CYP) and transporter proteins.

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.

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

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

Efletirizine (UCB-28754) is a histamine receptor antagonist with inhibitory effects on the enzyme 5-lipoxygenase (5-LO), and is useful in the topical treatment of allergic diseases.

Impromidine hydrochloride is a very potent and specific histamine H2 receptor agonist for conducting cardiovascular studies.

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.

KSK94 FA is a potent histamine H3 receptor antagonist that inhibits H3 receptors and is used in the study of neuropathic pain and obesity.

KSK68 is a potent dual sigma-1 and histamine H3 receptor antagonist with potential analgesic activity and high affinity for H3 receptors, sigma-1, sigma-2 receptors.KSK68 can be used in the study of pain related diseases.

MK-0249 FA is an orally active, selective and potent histamine H3 inverse agonist for the study of attention deficit, hyperactivity disorder neurodivergent and cognitive disorders in adults.

Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.

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

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

KSK94 is a specific H3 receptor antagonist that inhibits H3, sigma-1, and sigma-2 receptors , with Ki values of 7.9, 2958, and 75.2 nM, respectively, and can be used to study injurious pain and neuropathic pain.

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