PHACLOFEN

Names

[ Name ]:
PHACLOFEN

[Synonym ]:
3-Amino-2-(4-chlorophenyl)propanephosphonic acid
MFCD00069328

Biological Activity

[Description]:

Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact[1][2].

[Related Catalog]:

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

Research Areas >> Neurological Disease

Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

GABAB receptor[1]

[In Vivo]

Phaclofen (100 nmol; intrathecal injection) antagonizes the depressant effect of baclofen. Phaclofen (100 nmol) is devoid of stimulatory or depressant effects on spinal reflexes[3].

[References]

[1]. Johnson CM, et al. The antitussive cloperastine improves breathing abnormalities in a Rett Syndrome mouse model by blocking presynaptic GIRK channels and enhancing GABA release. Neuropharmacology. 2020;176:108214.

[2]. Kerr DI, et al. Phaclofen: a peripheral and central baclofen antagonist. Brain Res. 1987;405(1):150-154.

[3]. Wüllner U, et al. Phaclofen antagonizes the depressant effect of baclofen on spinal reflex transmission in rats. Brain Res. 1989;496(1-2):341-344.

Chemical & Physical Properties

[ Density]:
1.432 g/cm3

[ Boiling Point ]:
467.1ºC at 760 mmHg

[ Molecular Formula ]:
C₉H₁₃ClNO₃P

[ Molecular Weight ]:
249.63100

[ Flash Point ]:
236.3ºC

[ Exact Mass ]:
249.03200

[ PSA ]:
93.36000

[ LogP ]:
2.26030

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

PKC-mediated GABAergic enhancement of dopaminergic responses: implication for short-term potentiation at a dual-transmitter synapse.

J. Neurophysiol. 112(1) , 22-9, (2014)

Transmitter-mediated homosynaptic potentiation is generally implemented by the same transmitter that mediates the excitatory postsynaptic potentials (EPSPs), e.g., glutamate. When a presynaptic neuron...

Transcriptome analysis of the key role of GAT2 gene in the hyper-accumulation of copper in the oyster Crassostrea angulata.

Sci. Rep. 5 , 17751, (2015)

One paradigm of oysters as the hyper-accumulators of many toxic metals is the inter-individual variation of metals, but the molecular mechanisms remain very elusive. A comprehensive analysis of the tr...

The antinociceptive effect of stimulating the retrosplenial cortex in the rat tail-flick test but not in the formalin test involves the rostral anterior cingulate cortex.

Pharmacol. Biochem. Behav. 131 , 112-8, (2015)

The stimulation of the retrosplenial cortex (RSC) is antinociceptive in the rat tail-flick and formalin tests. The rat RSC is caudal to and send projections to the ipsilateral anterior cingulate corte...