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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 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.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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