Phaclofen

Research use only, not for human use.

Phaclofen (3-Amino-2-(4-chlorophenyl)propanephosphonic acid) is a selective GABAB receptor antagonist, which can partially antagonize the sedative effect of (-)-baclofen, and reversibly antagonize the inhibition of cholinergic convulsive response of guinea pig ileum and distal colon by baclofen or GABA.

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.

The GABAB antagonist phaclofen (500 μM) partly prevents the effect of 1 μM of (R＋) baclofen.

Phaclofen (2 mg/kg; i.p) shows that fewer neuropeptide Y-like immunoreactive fibers are detected in the stimulated cuneate nucleus. Phaclofen (2 mg/kg; s.c) antagonizes the effects of 6 mg/kg R(＋) baclofen in dorsal striatum.Phaclofen (100 nmol; intrathecal injection) antagonizes the depressant effect of baclofen. Phaclofen (100 nmol) is devoid of stimulatory or depressant effects on spinal reflexes.Animal Model:Sprague–Dawley rats (180–250 g)Dosage:2 mg/kg Administration:I.p．Result:Fewer neuropeptide Y-like immunoreactive fibers were detected in the stimulated cuneate nucleus.Animal Model:Male Wistar rats (280–320 g)Dosage:2 mg/kg Administration:S.c.Result:Antagonized the effects of 6 mg/kg R(＋) baclofen in dorsal striatum.

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Others

Other Targets

GABA Receptor

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114012-12-3

249.63

C9H13ClNO3P

>98% (HPLC)

In Vitro:?1M NaOH : 50 mg/mL (200.30 mM; Ultrasonic)DMSO : < 1 mg/mL (insoluble or slightly soluble)

O=P(O)(O)CC(C1=CC=C(Cl)C=C1)CN

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(-20℃)

With Ice Pack

≥ 2 years