125464-42-8
125464-42-8
Chemical Structure
Saclofen
- CAS No.: 125464-42-8
- Formula:C9H12ClNO3S
- Molecular Weight:249.72
IUPAC Name: 3-amino-2-(4-chlorophenyl)propane-1-sulfonic acid
InChIKey: JYLNVJYYQQXNEK-UHFFFAOYSA-N
SMILES: O=S(CC(CN)C1=CC=C(Cl)C=C1)(O)=O
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Saclofen | 99.97% | 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. | ||||||||||||||||||||
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Saclofen (Standard) | ≥98% | Saclofen (Standard) is the analytical standard of Saclofen. | ||||||||||||||||||||
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References
- [1]. 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. [Content Brief]
- [2]. 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. [Content Brief]
- [3]. 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. [Content Brief]
- [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. [Content Brief]
