| 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 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 (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 |
|
