HomeNew Histamine Receptor Antagonists

New Histamine Receptor Antagonists

Catalog No. Product Name Information
E6055 Epinastine Epinastine (WAL801) is potent nonsedative antiallergic agent and an antagonist of histamine H1 receptor. It inhibits the actions of leukotrienes, platelet-activating factor (PAF), and bradykinin. It also stabilizes mast cells and reduces IL-8 release from eosinophils, helping to control allergic inflammation.
E4955 Pitolisant Pitolisant(BF2.649, Tiprolisant) is a potent, selective antagonist of the non-imidazole histamine H3 receptor, with a Ki value of 0.16 nM and an EC50 of 1.5 nM as an inverse agonist. It enhances the activity of histaminergic neurons, promoting vigilance and cognitive function. It is useful in research on wakefulness, memory deficits, and cognitive disorders.
E4873 Mebhydroline Mebhydroline acts as a selective antagonist of farnesoid X receptor (FXR). Mebhydrolin improves blood glucose balance in in vivo mice models by inhibiting hepatic gluconeogenesis through the FXR/miR-22-3p/PI3K/AKT/FoxO1 pathway and enhancing glycogen synthesis. It also acts as a specific antagonist of histamine H1 receptor. It has potential for its use in the treatment of Type 2 diabetes mellitus (T2DM).
E4938 Diphenylpyraline Diphenylpyraline(Allergen, Difenilpiralina; 4-Diphenylmethoxy-1-methylpiperidine), also known as 4-Diphenylmethoxy-1-methylpiperidine, is a first-generation antihistamine that acts as an antagonist of the histamine H1 receptor. It provides therapeutic antiallergic effects and has the potential to treat cocaine addiction.
E4862 Pimethixene Pimethixene(Calmixen, Pimetixene) is a highly potent and non-selective antagonist of the 5-HT2B receptor, with a pKi of 10.44. It also functions as an antihistamine and anticholinergic agent, and is a highly potent multi-target antagonist with antagonistic effects on multiple receptors.
≡ All Histamine Receptor Antagonists