H1 receptor Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S4696 CarbinoxaMine Maleate

Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.

S5447 Triprolidine Hydrochloride

Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.

S4849 Levocetirizine Dihydrochloride

Levocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.

S5647 Emedastine Difumarate

Emedastine Difumarate (Rapimine, Emedastine fumarate) is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.

S3913 Pimethixene maleate

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.

Selective Histamine H1 Receptor, pKi: 10.14
S5659 Emedastine

Emedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM).

Selective H1 receptor, Ki: 1.3 nM
S1847 Clemastine (HS-592) fumarate

Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.

Selective Histamine H1 receptor, IC50: 3 nM
S4625 Alcaftadine

Alcaftadine (Lastacaft, R89674) is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor.

Selective H1 receptor, pKi: 8.5
S0398 Astemizole

Astemizole (R 43512) is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.

Selective H1 receptor, IC50: 4.7 nM
S1816 Chlorpheniramine Maleate

Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an histamine H1 receptor antagonist with IC50 of 12 nM.

Selective Histamine H1 receptor, IC50: 12 nM
S4026 Hydroxyzine 2HCl

Hydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM.

Selective Histamine H1 receptor, IC50: 10 nM-19 nM
S3721 Bilastine

Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.

Selective H1 receptor, Ki: 44.15 nM
S2107 Mizolastine

Mizolastine (SL 850324) is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.

Selective Histamine H1 receptor, IC50: 47 nM
S4012 Desloratadine

Desloratadine (SCH-34117, NSC 675447) is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.

Selective Histamine H1 receptor, IC50: 51 nM
S3052 Rupatadine Fumarate

Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.

Selective Histamine H1 receptor, Ki: 102 nM
S3208 Fexofenadine HCl

Fexofenadine (MDL 16455A) inhibits histamine H1 receptor with IC50 of 246 nM.

Selective Histamine H1 receptor, IC50: 246 nM
S3037 Bepotastine Besilate

Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.

Selective Histamine H1 receptor, pIC50: 5.7
S1358 Loratadine (SCH29851)

Loratadine (SCH29851) is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.

Selective H1 receptor, : ; B(0)AT2, IC50: 4 μM
S3146 Tripelennamine HCl

Tripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.

Selective H1 receptor, IC50: 30 μM
S4353 Terfenadine

Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.

S2024 Ketotifen Fumarate

Ketotifen Fumarate is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer.

S4008 Pemirolast potassium

Pemirolast potassium (BMY26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.

S1986 Meclizine 2HCl

Meclizine (NSC 28728) is a histamine H1 receptor antagonist used to treat nausea and motion sickness, has anti-histamine, anti-muscarinic and anti-oxidative phosphorylation properties, also an agonist ligand for mCAR (constitutive androstane receptor) and an inverse agonist for hCAR.

S5864 Levocetirizine

Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.

S1866 Diphenhydramine HCl

Diphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis.

S4262 Ebastine

Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.

S4139 Cyclizine 2HCl

Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.

S2585 Brompheniramine hydrogen maleate

Brompheniramine hydrogen maleate is a histamine H1 receptors antagonist.

S5196 Promethazine

Promethazine is a potent histamine H1 receptor antagonist. Promethazine is a medication used in the management and treatment of allergic conditions, nausea and vomiting, motion sickness, and sedation. Promethazine exhibits antiparasitic properties.

S4240 Doxylamine Succinate

Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.

S4117 Histamine Phosphate

Histamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors.

S4118 Histamine 2HCl

Histamine is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.