Saclofen

Saclofen is an orally active and a competitive GABAB receptor antagonist with an IC50 of 7.8 μM. Saclofen has weak antagonistic effects on GABAB1b and GABAB2 heterodimeric recombinant receptors. Saclofen inhibits the binding of Baclofen (HY-B0007) to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts, and exhibits anti-inflammatory and analgesic effects in rats[1][2][3][4][5].

Product Specifications

CAS Number

[125464-42-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/saclofen.html

Purity

99.70

Solubility

H2O : 10 mg/mL (ultrasonic)

Smiles

O=S(CC(CN)C1=CC=C(Cl)C=C1)(O)=O

Molecular Formula

C9H12ClNO3S

Molecular Weight

249.72

Precautions

H302, H315, H319, H335

References & Citations

[1]Sallam MY, et al. Central GABAA receptors are involved in inflammatory and cardiovascular consequences of endotoxemia in conscious rats. Naunyn Schmiedebergs Arch Pharmacol. 2016 Mar;389 (3) :279-88. |[2]K R Biggs, et al. GABAB receptor stimulation phase-shifts the mammalian circadian clock in vitro. Brain Res. 1998 Oct 5;807 (1-2) :250-4.|[3]M D Wood, et al. The human GABA (B1b) and GABA (B2) heterodimeric recombinant receptor shows low sensitivity to phaclofen and saclofen. Br J Pharmacol. 2000 Nov;131 (6) :1050-4.|[4]Seyyed Hamid Bathaei, et al. The Effect of Flavonoids Catechin, Baclofen and Saclofen on Acetic Acid - Induced Visceral Pain by in Rat. International Journal of Pharmaceutical Research & Allied Sciences. 2016, 5 (1) :81-85|[5]C A Drew, et al. Inhibition of baclofen binding to rat cerebellar membranes by phaclofen, saclofen, 3-aminopropylphosphonic acid and related GABAB receptor antagonists. Neurosci Lett. 1990 May 18;113 (1) :107-10.