Phaclofen

CAS: 114012-12-3 F: C9H13ClNO3P W: 249.63

Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen

Contact QiTai

This product is for research use only, not for human use. We do not sell to patients.

Bioactivity	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].
Target	GABAB receptor
Invitro	The GABAB antagonist phaclofen (500 µM) partly prevents the effect of 1 µM of (R＋) baclofen[5].
In Vivo	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]. Animal Model:
Name	Phaclofen
CAS	114012-12-3
Formula	C9H13ClNO3P
Molar Mass	249.63
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
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.

Echimidine N-oxide

[DPen2, Pen5] Enkephalin