Phaclofen

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].

Product Specifications

CAS Number

[114012-12-3]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

GABA Receptor

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/phaclofen.html

Purity

99.98

Solubility

1M NaOH : 50 mg/mL (ultrasonic) |DMSO : < 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

ClC1=CC=C(C(CN)CP(O)(O)=O)C=C1

Molecular Formula

C9H13ClNO3P

Molecular Weight

249.63

Precautions

H315, H319, H335

References & Citations

[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.|[4]Chen SH, et al. Changes in GABA and GABA (B) receptor expressions are involved in neuropathy in the rat cuneate nucleus following median nerve transection. Synapse.2012; 66 (6) :561-572.|[5]Abellán MT, et al. Dual control of dorsal raphe serotonergic neurons by GABA (B) receptors. Electrophysiological and microdialysis studies. Synapse. 2000;36 (1) :21-34.