Saclofen

Names

[ Name ]:
Saclofen

[Synonym ]:
Saclofen
3-Amino-2-(4-chlorophenyl)propane-1-sulfonic acid
UNII:LRZ36BCQ1Y
Benzeneethanesulfonic acid, β-(aminomethyl)-4-chloro-
MFCD00216817
3-Amino-2-(4-chlorophenyl)-1-propanesulfonic acid
beta-(Aminomethyl)-4-chlorobenzeneethanesulfonic acid

Biological Activity

[Description]:

Saclofen is a competitive antagonist of the GABAB receptor with an IC50 of 7.8 μM. Saclofen can be used to determine the functional roles for the GABAB receptor as a mediator of slow inhibitory postsynaptic potentials in the brain[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[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.

Chemical & Physical Properties

[ Density]:
1.437±0.06 g/cm3

[ Melting Point ]:
310-315 ºC

[ Molecular Formula ]:
C₉H₁₂ClNO₃S

[ Molecular Weight ]:
249.714

[ Exact Mass ]:
249.022644

[ PSA ]:
88.77000

[ LogP ]:
0.03

[ Index of Refraction ]:
1.600

[ Storage condition ]:
Store at RT

[ Water Solubility ]:
Slightly soluble (7.5 g/L) (25 ºC)

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ HS Code ]:
2921499090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2921499090

[ Summary ]:
2921499090 other aromatic monoamines and their derivatives; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

Articles

Opioid receptor-dependent sex differences in synaptic plasticity in the hippocampal mossy fiber pathway of the adult rat.

J. Neurosci. 35(4) , 1723-38, (2015)

The mossy fiber (MF) pathway is critical to hippocampal function and influenced by gonadal hormones. Physiological data are limited, so we asked whether basal transmission and long-term potentiation (...

Spinal segmental and supraspinal mechanisms underlying the pain-relieving effects of spinal cord stimulation: an experimental study in a rat model of neuropathy.

Neuroscience 215 , 196-208, (2012)

Spinal cord stimulation (SCS) may alleviate certain forms of neuropathic pain; its mechanisms of action are, however, not fully understood. Previous studies have mainly been focused onto segmental spi...

GABA-induced uncoupling of GABA/benzodiazepine site interactions is associated with increased phosphorylation of the GABAA receptor.

J. Neurosci. Res. 92(8) , 1054-61, (2014)

The use-dependent regulation of the GABAA receptor occurs under physiological, pathological, and pharmacological conditions. Tolerance induced by prolonged administration of benzodiazepines is associa...