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Item No. 11158

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Diphenhydramine (DPH) is a first generation antihistamine that is a potent antagonist of the histamine H1 receptor (Ki = 11.7 nM using human recombinant receptors).1,2 DPH readily crosses the blood-brain barrier and produces diverse cognitive and psychomotor effects.1,3 DPH also antagonizes muscarinic cholinergic receptors (Kis = 100 to 260 nM for M1-M5), increasing the range of central nervous system effects and applications.4 This product is also available as an analytical reference standard (Item No. 22489).
WARNING This product is not for human or veterinary use.
1. The role of histamine H1 and H4 receptors in allergic inflammation: The search for new antihistamines. Nat. Rev. Drug Discov. 7(1), 41-53 (2008).
2. A novel phenylaminotetralin radioligand reveals a subpopulation of histamine H1 receptors. J. Pharmacol. Exp. Ther. 302(1), 328-336 (2002).
3. Loratadine: A non-
4. Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells. J. Pharmacol. Exp. Ther. 260(2), 576-580 (1992).
Physicochemical evaluation of DEAE-