For research use only. Not for therapeutic Use.
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].
The GABAB antagonist phaclofen (500 µM) partly prevents the effect of 1 µM of (R＋) baclofen[5].
Phaclofen (2 mg/kg; i.p) shows that fewer neuropeptide Y-like immunoreactive fibers are detected in the stimulated cuneate nucleus[4].
Phaclofen (2 mg/kg; s.c) antagonizes the effects of 6 mg/kg R(＋) baclofen in dorsal striatum[5].
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].
| Catalog Number | M027273 |
| CAS Number | 114012-12-3 |
| Synonyms | [3-amino-2-(4-chlorophenyl)propyl]phosphonic acid |
| Molecular Formula | C9H13ClNO3P |
| Purity | ≥95% |
| InChI | InChI=1S/C9H13ClNO3P/c10-9-3-1-7(2-4-9)8(5-11)6-15(12,13)14/h1-4,8H,5-6,11H2,(H2,12,13,14) |
| InChIKey | VSGNGLJPOGUDON-UHFFFAOYSA-N |
| SMILES | C1=CC(=CC=C1C(CN)CP(=O)(O)O)Cl |
| Reference | [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. |
