ChemicalBook CAS DataBase List 114012-12-3

114012-12-3

Name	PHACLOFEN
CAS	114012-12-3
Molecular Formula	C9H13ClNO3P
MDL Number	MFCD00069328
Molecular Weight	249.63
MOL File	114012-12-3.mol

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

Safety Data

Hazard Codes	Xi
Risk Statements	36/37/38 less more
Safety Statements	26-36 less more
WGK Germany	3
Storage Class	11 - Combustible Solids
Hazard Classifications	Eye Irrit. 2 Skin Irrit. 2 STOT SE 3

Hazard Information

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.

Spectrum Detail

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