Product Description: Saclofen (Standard) is the analytical standard of Saclofen. This product is intended for research and analytical applications. Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats[1][2][3][4][5].
Formula: C9H12ClNO3S
References: [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.
CAS Number: 125464-42-8
Molecular Weight: 249.719
Research Area: Inflammation/Immunology; Neurological Disease
Target: GABA Receptor;Reference Standards
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