H1 receptor Selective Inhibitors | Agonists | Antagonists

Catalog No. Product Name Information Selective / Pan IC50 / Ki
S1847 Clemastine Fumarate

Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.

Selective Histamine H1 receptor, IC50: 3 nM
S1816 Chlorpheniramine Maleate

Chlorpheniramine (Chlorpheniramine maleate, Chlorphenamine) 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
S2107 Mizolastine

Mizolastine 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 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 inhibits histamine H1 receptor with IC50 of 246 nM.

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

Bepotastine 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

Loratadine 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 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.

S4262 Ebastine

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

S1986 Meclizine 2HCl

Meclizine 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.

S4008 Pemirolast potassium

Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.

S1866 Diphenhydramine HCl

Diphenhydramine HCl (Benadryl), a histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations.

S2585 Brompheniramine hydrogen maleate

Brompheniramine hydrogen maleate is a histamine H1 receptors antagonist.

S4139 Cyclizine 2HCl

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

S2024 Ketotifen Fumarate

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

S4118 Histamine 2HCl

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

S4117 Histamine Phosphate

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