PHACLOFEN
PHACLOFEN Basic information
- Product Name:
- PHACLOFEN
- Synonyms:
-
- 3-AMINO-2-(4-CHLOROPHENYL)PROPYLPHOSPHONIC ACID
- PHACLOFEN
- (RS)-3-AMINO-2-(4-CHLOROPHENYL)PROPYLPHOSPHONIC ACID
- 3-amino-2-(4-chlorophenyl)*propanephosphonic acid
- PHACLOFEN GABA(B) RECEPTOR ANTA
- Phosphonic acid, (3-amino-2-(4-chlorophenyl)propyl)-
- Phosphonic acid, P-[3-amino-2-(4-chlorophenyl)propyl]-
- Phaclofen,(RS)-3-Amino-2-(4-chlorophenyl)propylphosphonicaci
- CAS:
- 114012-12-3
- MF:
- C9H13ClNO3P
- MW:
- 249.63
- Product Categories:
-
- GABA/Glycine receptor
- Mol File:
- 114012-12-3.mol
PHACLOFEN Chemical Properties
- Melting point:
- 249-252 °C
- Boiling point:
- 467.1±55.0 °C(Predicted)
- Density
- 1.432±0.06 g/cm3(Predicted)
- storage temp.
- Store at RT
- solubility
- 0.1 M HCl: 13.3 mg/mL
- form
- solid
- pka
- 1.87±0.10(Predicted)
- color
- white
MSDS
- Language:English Provider:SigmaAldrich
PHACLOFEN Usage And Synthesis
Uses
Phaclofen is a selective GABAB?receptor antagonist.
General Description
Phaclofen is a phosphonic acid derivative of baclofen.
Biological Activity
Selective GABA B antagonist. Phosphono analog of GABA B agonist baclofen ((RS)-4-Amino-3-(4-chlorophenyl)butanoic acid ).
Biochem/physiol Actions
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.
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: | 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. |
| 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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