Phaclofen

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Phaclofen 是一种选择性 GABAB receptor 拮抗剂。Phaclofen 是一种外周和中央的 baclofen 拮抗剂。酞氯芬在确定中枢和外周 GABA 和 (-)-baclofen 相互作用的 bicuculline-insensitive 受体的生理意义方面可能是一种潜在的化合物。

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 中的溶解度 : 50 mg/mL (200.30 mM; 超声助溶)DMSO 中的溶解度 : < 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