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| | 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 | | EINECS: | | | 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 | | 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 |
| 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 |
| | PHACLOFEN Usage And Synthesis |
| Uses | Phaclofen is a selective GABABreceptor 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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| | PHACLOFEN Preparation Products And Raw materials |
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