MedChemExpress -Model Diphenhydramine hydrochloride -147-24-0

FromMedChemExpress LLC (MCE)

Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB)[1][2].

Diphenhydramine hydrochloride

MCE China：Diphenhydramine hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-B0303A

CAS：147-24-0

Purity：99.98%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB).

In Vitro：Diphenhydramine hydrochloride inhibits Cisplatin (HY-17394)-induced cell death in kidney proximal tubular cells (HK-2 and LLC-PK1 cells)[3]. Diphenhydramine (0.2-1 mM, 24 h) hydrochloride inhibits cell viability in CCRF-CEM and Jurkat cells[4]. Diphenhydramine (0.5 and 1 mM, 24 h) hydrochloride induces apoptosis in CCRF-CEM and Jurkat cells[4]. Diphenhydramine (0-10 μg/mL, 24 or 48 h) hydrochloride increases the expression of Bad and Bax, and decreases BCL-2 level in PANC-1 cells[5].

In Vivo：Diphenhydramine (20 mg/kg) hydrochloride inhibits Cisplatin (HY-17394)-induced kidney toxicity in mice[3]. Diphenhydramine (3-30 mg/kg, i.m., 5 minutes prior to a s.c. of 25 mg/kg Dichlorvos) hydrochloride reduces mortality in rats with acute, severe dichlorvos exposure[6].

IC50 & Target：H1 Receptor

References：

[1]. Simons FE. H1-receptor antagonists. Comparative tolerability and safety. Drug Saf. 1994;10(5):350-380. [Content Brief]

[2]. Sadiq MW, et al. Diphenhydramine active uptake at the blood-brain barrier and its interaction with oxycodone in vitro and in vivo. J Pharm Sci. 2011;100(9):3912-3923. [Content Brief]

[3]. Hamano H, et al. Diphenhydramine may be a preventive medicine against cisplatin-induced kidney toxicity. Kidney Int. 2021 Apr;99(4):885-899. [Content Brief]

[4]. Jangi SM, et al. Apoptosis of human T-cell acute lymphoblastic leukemia cells by diphenhydramine, an H1 histamine receptor antagonist. Oncol Res. 2004;14(7-8):363-72. [Content Brief]

[5]. Zhang R, Chen M, Yu L, et al. Anticancer activity of diphenhydramine against pancreatic cancer by stimulating cell cycle arrest, apoptosis, and modulation of PI3K/Akt/mTOR pathway[J]. Cell proliferation, 2021, 69: 5.

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