Diphenylpyraline, a histamine H1 receptor antagonist, has psychostimulant properties.

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Lapa GB, Mathews TA, Harp J, Budygin EA, Jones SR

Diphenylpyraline, a histamine H1 receptor antagonist, has psychostimulant properties.

Eur J Pharmacol. 2005 Jan 4;506(3):237-40. Epub 2004 Dec 8.

PubMed ID

15627433 [ View in PubMed

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Abstract

Diphenylpyraline hydrochloride (DPP) is used clinically as an antihistamine drug, but its neurobiological effects are not completely understood. Voltammetry and microdialysis were used to investigate potential actions of DPP on the dopamine system. Voltammetric monitoring of dopamine signals in mouse nucleus accumbens slices showed that DPP (10 microM) markedly inhibited dopamine uptake. There was a 20-fold increase in apparent Km for dopamine uptake, while Vmax was unchanged. Microdialysis experiments demonstrated that DPP (5 mg/kg, i.p.) elevated extracellular dopamine levels (approximately 200%) in mouse nucleus accumbens. DPP (5 and 10 mg/kg) also induced locomotor activation. All of the effects of DPP were comparable with those of cocaine. Taken together, these results indicate that DPP acts as a competitive dopamine transporter inhibitor similar to cocaine.

DrugBank Data that Cites this Article

Drugs

Diphenylpyraline

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Diphenylpyraline	Histamine H1 receptor	Protein	Humans	Yes	Antagonist	Details
Diphenylpyraline	Sodium-dependent dopamine transporter	Protein	Humans	Unknown	Inhibitor	Details