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TargetMol | Tags GPCR/G Protein
TargetMol | Tags Immunology/Inflammation
TargetMol | Tags Neuroscience

Histamine Receptor

The histamine receptors are a class of G protein–coupled receptors which bind histamine as their primary endogenous ligand.

  • Ritanserin
    T1675987051-43-2
    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.
    • $34
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  • AVN-101
    T266901061354-48-0
    AVN-101 is a potent 5-HT7 receptor antagonist.
    • $32
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  • Pitolisant
    T60636362665-56-3
    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.
    • $40
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  • Ziprasidone hydrochloride monohydrate
    T0031138982-67-9
    Ziprasidone hydrochloride monohydrate (CP 88059) is a united 5-HT (serotonin) and dopamine receptor antagonist which shows potent effects of the antipsychotic activity.
    • $50
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  • Mianserin hydrochloride
    T078321535-47-7
    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.
    • $32
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  • Perphenazine
    T109058-39-9
    Perphenazine (Trilafon) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
    • $29
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    TargetMol | Citations Cited
  • Trazodone hydrochloride
    T161925332-39-2
    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.
    • $39
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  • Protopine
    T3429130-86-9
    Protopine (Fumarine) is a benzylisoquinoline alkaloid. It has been found to inhibit histamine H1 receptors and platelet aggregation, and acts as an analgesic.
    • $50
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  • Famotidine
    T162776824-35-6
    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.
    • $50
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  • N-Acetylhistamine
    T19443673-49-4
    N-Acetylhistamine (N-Omega-acetylhistamine) is a metabolite of histamine.
    • $29
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  • Oxmetidine FA
    T68122L In house
    Oxmetidine FA is an orally available specific histamine H2 receptor antagonist with antiulcerogenic properties.
    • $195
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  • Vapitadine dihydrochloride
    T29096279253-83-7In house
    Vapitadine dihydrochloride(R-129160 2HCl) is a novel, potent, selective and non-sedating compound with inhibitory effects on histamine H1.
    • $258
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  • LY-2624803
    T24421879409-35-5In house
    LY-2624803 is a 5-HT2A receptor antagonist and histamine receptor inverse agonist that can be used to improve slow wave sleep.
    • $143
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  • Pimethixene
    T12489314-03-4
    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).
    • $35
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  • KP136
    T1566676239-32-2In house
    KP136 (AL136) is an orally active anti-allergic compound that inhibits histamine release and is used in studies of asthma and allergic edema.
    • $293 TargetMol
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  • S 38093 HCl
    T40871222097-72-4
    S 38093 is a novel brain-penetrant antagonist/inverse agonist of H3 receptors.
    • $79
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  • Dimethindene
    T314885636-83-9In house
    Dimethindene (Dimetindeno) is a selective antagonist of H1 receptor and blocks K+ current. Dimethindene exhibits antihistamine and anticholinergic effects.
    • $117
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  • Meclizine
    T40652569-65-3
    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.
    • $195
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  • Clemastine
    T1996615686-51-8
    Clemastine (Meclastin) is an antagonist of the H1 receptor and exhibits anti-inflammatory effects.
    • $61
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  • Fenclozine Maleate
    T8397576823-82-0In house
    Fenclozine Maleate (S 1429) is a potential histamine H1 receptor antagonist , which can be used to study fever, inflammation and pain.
    • $195 TargetMol
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  • BMY 25368 HCl
    T23811L86134-36-3In house
    BMY 25368 HCl is a competitive histamine H2 receptor antagonist that antagonizes gastric secretion stimulated by pentagastrin, ethacrynic choline, and food.
    • $89 TargetMol
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  • (±)-Tazifylline
    T1000079712-55-3In house
    (±)-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.
    • $151
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  • Vapitadine
    T29096L793655-64-8In house
    Vapitadine is a non-sedative antihistamine compound that relieves itching caused by atopic dermatitis.
    • $195
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  • Wy 49051
    T13352113418-56-7In house
    Wy 49051 is an orally active antagonist of H1 receptor(IC50 of 44 nM).
    • $253
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  • Linetastine
    T25737159776-68-8In house
    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.
    • $130
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  • Dioxopromethazine hydrochloride
    T372315374-15-9
    Dioxopromethazine is a target-based classification of drug and available in a number of countries worldwide.
    • $30
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  • Cetirizine Impurity B dihydrochloride
    T90841000690-91-4
    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.
    • $47
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  • Noberastine
    T25875110588-56-2In house
    Noberastine (R 64947) is a novel histamine H1 antagonist with potent and specific peripheral antihistamine activity.
    • $146
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  • Fexofenadine
    T2139083799-24-0
    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.
    • $46
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    TargetMol | Citations Cited
  • Chlorcyclizine
    T971782-93-9
    CHLORCYCLIZINE is a histamine H1 antagonist and a potent hepatitis C virus (HCV) entry inhibitor.
    • $30
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  • Azelastine
    T021158581-89-8
    Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.
    • $50
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  • Abt-288
    T26526948845-91-8In house
    ABT-288 is a selective and potent H3 antagonist for the treatment of mild to moderate Alzheimer's dementia.
    • $195
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  • Rocastine
    T1677891833-49-7
    Rocastine (AHR-11325) is a selective and potent non-sedating H1 receptor antagonist.
    • $700
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  • Samelisant
    T97701394808-82-2
    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.
    • $113
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  • DF-1111301
    T27159160665-99-6In house
    DF-1111301 is a novel anti-allergic compound with anti-histamine H1 and anti-PAF activity.
    • $293 TargetMol
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  • GSK-239512
    T27462720691-69-0In house
    GSK-239512 is an antagonist of H3 receptor and can be used in studies about the treatment of cognitive dysfunction in neurodegenerative disorders.
    • $39
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  • JNJ 10191584 maleate
    T22879869497-75-6
    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).
    • $49
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  • Enerisant HCl
    T704891152749-07-9In house
    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.
    • $93
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  • Efletirizine
    T27244150756-35-7In house
    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.
    • $195
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  • Impromidine hydrochloride
    T6892165573-02-6In house
    Impromidine hydrochloride is a very potent and specific histamine H2 receptor agonist for conducting cardiovascular studies.
    • $258
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  • Carcinine ditrifluoroacetate Acetate
    T22624L
    Carcinine ditrifluoroacetate Acetate (β-Alanylhistamine dihydrochloride) is an H3 receptor antagonist.
    • $97
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  • Thonzylamine hydrochloride
    T2101463-56-9
    Thonzylamine hydrochloride (Resistab) is an anticholinergic and antihistamine used as an antipruritic.
    • $50
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  • Mianserin
    T2142824219-97-4
    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.
    • $397
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    TargetMol | Citations Cited
  • Bamirastine
    T13566215529-47-8
    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.
    • $700
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  • NP10679
    T734472914889-88-4In house
    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.
    • $293 TargetMol
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  • JNJ-39220675
    T27678959740-39-7In house
    JNJ-39220675 (JNJ 39220675) is a selective and brain permeable histamine H3 receptor antagonist.
    • $293 TargetMol
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  • KSK94 FA
    T79500L In house
    KSK94 FA is a potent histamine H3 receptor antagonist that inhibits H3 receptors and is used in the study of neuropathic pain and obesity.
    • $195 TargetMol
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  • KSK68
    T794992566715-91-9In house
    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.
    • $68
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  • KSK94
    T795002566716-07-0In house
    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.
    • $54
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  • MK-0249 FA
    T12054L In house
    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.
    • $195
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