Diphenhydramine


CAS No. : 58-73-1

58-73-1
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Cat. No. : HY-B0303
M.Wt: 255.36
Formula: C17H21NO
Purity: >98 %
Solubility: DMSO : 100 mg/mL (ultrasonic)
Introduction of 58-73-1 :

Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) [1][2][3]. In Vitro:Diphenhydramine (1-300 μM, 30 s) can block NMDA-activated membrane currents. This property can be responsible for or add to its sedative, analgesic and memory related effects[2].
In Vivo:Diphenhydramine (0-10 mg/kg, i.v. and p.o.) has better oral bioavailability when used in combination with Dimenhydrinate (HY-B1215)sup>[3].
Diphenhydramine (20 mg/kg, i.p.) can improve the kidney injury induced by Cisplatin (CDDP) (HY-17394) in mice, and does not affect the anti-tumor efficacy of Cisplatin[4].

Pharmacokinetic parameters for diphenhydramine after single oral or intravenous administration of diphenhydramine HCl (5 mg/kg) to six healthy dogs by using a noncompartmental model with first-order elimination[3]
Route Dose (mg/kg) AUClast (ng·h/mL) C0 (ng/Ml) CL (Ml/h/kg) T1/2 (h) Kel (1/h) MRT (h) Vss_obs (mL/kg) Cmax (ng/mL) Tmax (h) Vz (mL/kg) F (%)
i.v. 5 391.20 266.10 2833.04 1.89 0.45 2.47 6582.36 / / / /
p.o. 5 153.80 / / 4.98 0.59 6.97 / 35.80 1.30 180157.36 7.75

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