SB-334867 (free base)

SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively[1]. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo[2][3].

Product Specifications

CAS Number

[792173-99-0]

Product Name Alternative

SB334867A free base

UNSPSC

12352005

Hazard Statement

H315

Target

Orexin Receptor (OX Receptor)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/SB-334867-free-base.html

Purity

99.88

Solubility

0.1 M HCl : 6 mg/mL (ultrasonic; adjust pH to 3 with HCl) |DMSO : 50 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC(OC(C)=N2)=C2C=C1)NC3=CC=NC4=CC=CN=C43

Molecular Formula

C17H13N5O2

Molecular Weight

319.32

Precautions

H315

References & Citations

[1]Porter RA, et al. 1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor.Bioorg Med Chem Lett. 2001 Jul 23;11 (14) :1907-10.|[2]Łupina M, et al. SB-334867 (an Orexin-1 Receptor Antagonist) Effects on Morphine-Induced Sensitization in Mice-a View on Receptor Mechanisms.|[3]Anderson RI, et al. Orexin-1 and orexin-2 receptor antagonists reduce ethanol self-administration in high-drinking rodent models.Front Neurosci. 2014 Feb 25;8:33.|[4]Smart D, et al. SB-334867-A: the first selective orexin-1 receptor antagonist.Br J Pharmacol. 2001 Mar;132 (6) :1179-82.