H1 receptor Selective Inhibitors | Agonists | Antagonists

Catalog No.	Product Name	Information	Selective / Pan	IC50 / Ki
S5447	Triprolidine Hydrochloride	Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.	Selective
S0897	Cyclizine	Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.	Selective
S5864	Levocetirizine	Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.	Selective
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.	Selective
S4696	CarbinoxaMine Maleate	Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.	Selective
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.	Selective
S4849	Levocetirizine Dihydrochloride	Levocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.	Selective
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 fumarate	Clemastine fumarate 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 K_i 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 (Alavert,Claritin,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
S4240	Doxylamine Succinate	Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.	Selective
S4139	Cyclizine 2HCl	Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.	Selective
S2585	Brompheniramine hydrogen maleate	Brompheniramine hydrogen maleate(Brompheniramine maleate) is a histamine H1 receptors antagonist.	Selective
S1986	Meclizine 2HCl	Meclizine (NSC 28728,Meclozine dihydrochloride) 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.	Selective
S1866	Diphenhydramine HCl	Diphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis.	Selective
S4008	Pemirolast potassium	Pemirolast potassium (BMY26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.	Selective
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.	Selective
S2024	Ketotifen Fumarate	Ketotifen Fumarate(HC 20511 fumarate) is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer.	Selective
S4262	Ebastine	Ebastine(LAS-W 090,RP64305) is a potent H1-histamine receptor antagonist, used for allergic disorders.	Selective
S4117	Histamine Phosphate	Histamine(Histamine diphosphate) acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors.	Pan
S4118	Histamine 2HCl	Histamine(Ceplene) is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.	Pan