| Identification | Back Directory | [Name]
PHACLOFEN | [CAS]
114012-12-3 | [Synonyms]
PHACLOFEN
PHACLOFEN GABA(B) RECEPTOR ANTA
3-AMINO-2-(4-CHLOROPHENYL)PROPYLPHOSPHONIC ACID
3-amino-2-(4-chlorophenyl)*propanephosphonic acid
(RS)-3-AMINO-2-(4-CHLOROPHENYL)PROPYLPHOSPHONIC ACID
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 | [Molecular Formula]
C9H13ClNO3P | [MDL Number]
MFCD00069328 | [MOL File]
114012-12-3.mol | [Molecular Weight]
249.63 |
| Chemical Properties | Back Directory | [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 | [InChI]
1S/C9H13ClNO3P/c10-9-3-1-7(2-4-9)8(5-11)6-15(12,13)14/h1-4,8H,5-6,11H2,(H2,12,13,14) | [InChIKey]
VSGNGLJPOGUDON-UHFFFAOYSA-N | [SMILES]
NCC(CP(O)(O)=O)c1ccc(Cl)cc1 |
| Safety Data | Back Directory | [Hazard Codes ]
Xi | [Risk Statements ]
36/37/38 | [Safety Statements ]
26-36 | [WGK Germany ]
3 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Eye Irrit. 2
Skin Irrit. 2
STOT SE 3 |
| Hazard Information | Back Directory | [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.
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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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