A potent inhibitor that blocks dopamine uptake (IC50 = 1-51 nM); effectively inhibits dopamine uptake in vivo

GBR 12909 (hydrochloride) – 25 mg

Brand:
Cayman
CAS:
67469-78-7
Storage:
-20
UN-No:
Non-Hazardous - /

GBR 12909 is a potent inhibitor that blocks dopamine uptake (IC50 = 1-51 nM).{25553,25555} It is more than 100-fold less effective at blocking serotonin or noradrenaline uptake.{25553,25555} GBR 12909 effectively inhibits dopamine uptake in vivo, leading to consequent stimulation of dopamine receptors.{25553,25554} GBR 12909 also inhibits pyrilamine binding to the histamine H1 receptor (IC50 = 18 nM) but poorly inhibits ligand binding to dopamine, adrenergic, acetylcholine, serotonin, and γ-aminobutyric acid receptors.{25555} It also blocks ligand binding to sigma receptors in rat brain (IC50 = 48 nM).{25552}  

 

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Description

A potent inhibitor that blocks dopamine uptake (IC50 = 1-51 nM); effectively inhibits dopamine uptake in vivo, leading to consequent stimulation of dopamine receptors.

Formal name: 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)-piperazine, dihydrochloride

Synonyms:  I 893

Molecular weight: 523.5

CAS: 67469-78-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology||Product Type|Biochemicals|Transporter & Exchanger Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research

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