Molecular structure of 2-Hydroxysaclofen, CAS Number: 117354-64-0
2-Hydroxysaclofen (CAS 117354-64-0)
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Alternate Names:
(RS)-3-Amino-2-(4-chlorophenyl)-2-hydroxypropyl-sulfonic acid
Application:
2-Hydroxysaclofen is a selective GABAB antagonist
CAS Number:
117354-64-0
Molecular Weight:
265.71
Molecular Formula:
C9H12ClNO4S
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
2-Hydroxysaclofen is a sulphonic analogue of baclofen that acts as a selective GABAB antagonist. 2-Hydroxysaclofen functions as an antagonist by reducing the amplitude of the excitatory postsynaptic potentials (EPSPs) in hippocampal CA1 pyrimidal neurons. Studies suggest that 2-Hydroxysaclofen displaces baclofen from the binding site of GABAB, via reducing the apparent density and affinity of the binding sites. These studies indicate that 2-Hydroxysaclofen can possibly be a useful tool in determining the physiological significance of central baclofen receptors.
2-Hydroxysaclofen (CAS 117354-64-0) References
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- The GABA-B antagonist 2-hydroxysaclofen reverses the effects of baclofen on the discriminative stimulus effects of D-amphetamine in the conditioned taste aversion procedure. | Miranda, F., et al. 2009. Pharmacol Biochem Behav. 93: 25-30. PMID: 19361543
- Effect of 2-hydroxy-saclofen, an antagonist of GABAB action, upon the binding of baclofen and other receptor ligands in rat cerebrum. | al-Dahan, MI., et al. 1990. Brain Res. 526: 308-12. PMID: 2175242
- Effects of GABAB receptor agonists and antagonists on glycemia regulation in mice. | Bonaventura, MM., et al. 2012. Eur J Pharmacol. 677: 188-96. PMID: 22210053
- Baclofen and 2-hydroxysaclofen modify acute hypolocomotive and antinociceptive effects of nicotine. | Varani, AP., et al. 2014. Eur J Pharmacol. 738: 200-5. PMID: 24886886
- Nicotine-induced molecular alterations are modulated by GABAB receptor activity. | Varani, AP., et al. 2018. Addict Biol. 23: 230-246. PMID: 28419642
- 2-Hydroxy-saclofen: an improved antagonist at central and peripheral GABAB receptors. | Kerr, DI., et al. 1988. Neurosci Lett. 92: 92-6. PMID: 2847092
- Baclofen antagonism by 2-hydroxy-saclofen in the cat spinal cord. | Curtis, DR., et al. 1988. Neurosci Lett. 92: 97-101. PMID: 2847093
- Participation of GABAB Receptors of Parafacial Respiratory Group in the Regulation of Respiration in Rats. | Kovaleva, TE. and Vedyasova, OA. 2019. Bull Exp Biol Med. 168: 24-27. PMID: 31745683
- 2-Hydroxy-saclofen causes a phaclofen-reversible reduction in population spike amplitude in the rat hippocampal slice. | Caddick, SJ., et al. 1995. Eur J Pharmacol. 274: 41-6. PMID: 7768279
- Supraspinal delta 2 opioid agonist analgesia in Swiss-Webster mice involves spinal GABAA receptors. | Rady, JJ. and Fujimoto, JM. 1996. Pharmacol Biochem Behav. 54: 363-9. PMID: 8743596
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Inhibitor of:
GABA Receptor, and GABAB R2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
2-Hydroxysaclofen, 2.5 mg | sc-202011 | 2.5 mg | $203.00 | |||
2-Hydroxysaclofen, 5 mg | sc-202011A | 5 mg | $306.00 |