A potent OX1R antagonist (Ki = 26.9 nM in a calcium mobilization assay); selective for OX1R over OX2R (Kds = 21.7 and 1

SB-408124 – 5 mg

Brand:
Cayman
CAS:
288150-92-5
Storage:
-20
UN-No:
Non-Hazardous - /

SB-408124 is a potent antagonist of orexin 1 receptors (OX1Rs) with a Ki value of 26.9 nM in a calcium mobilization assay using CHO cells that stably express human OX1R.{34091} It is selective for OX1R over OX2R, with Kd values of 21.7 and 1,704 nM, respectively, in a radioligand binding assay. In vivo co-perfusion of SB-408124 with human OX1R in the rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations and reduces cocaine-seeking behavior in rats.{36123}  

 

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Description

A potent OX1R antagonist (Ki = 26.9 nM in a calcium mobilization assay); selective for OX1R over OX2R (Kds = 21.7 and 1,704 nM, respectively, in a radioligand binding assay); co-perfusion with human OX1R in rat ventral tegmental area inhibits OX1R-induced glutamate and dopamine elevations; reduces cocaine-seeking behavior in rats

Formal name: N-(6,8-difluoro-2-methyl-4-quinolinyl)-N’-[4-(dimethylamino)phenyl]-urea

Synonyms: 

Molecular weight: 356.4

CAS: 288150-92-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Neuroendocrinology

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