Phaclofen is a selective GABABreceptor antagonist.
Phaclofen is a phosphonic acid derivative of baclofen.
Selective GABA B antagonist. Phosphono analog of GABA B agonist baclofen ((RS)-4-Amino-3-(4-chlorophenyl)butanoic acid ).
Phaclofen plays a vital role in identifying the physiological importance of central and peripheral bicuculline-insensitive receptors with which GABA and () baclofen interact. Phaclofen acts as a GABAB receptor antagonist. Phaclofen has an ability to reversibly block the late, bicuculline resistant, K+ dependent inhibitory postsynaptic potential (IPSP) logged in projection cells of the cat and rat dorsal lateral geniculate nucleus and in rat hippocampal CA1 pyramidal neurons.
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: | Sprague–Dawley rats (180–250 g)[4] |
| Dosage: | 2 mg/kg |
| Administration: | I.p． |
| Result: | Fewer neuropeptide Y-like immunoreactive fibers were detected in the stimulated cuneate nucleus.
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| Animal Model: | Male Wistar rats (280–320 g)[5] |
| Dosage: | 2 mg/kg |
| Administration: | S.c. |
| Result: | Antagonized the effects of 6 mg/kg R(＋) baclofen in dorsal striatum.
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