| Identification | Back Directory | [Name]
CHPG | [CAS]
170846-74-9 | [Synonyms]
CHPG
(RS)-2-CHLORO-5-HYDROXYPHENYLGLYCINE
α-amino-2-chloro-5-hydroxybenzeneacetic acid
Benzeneacetic acid, α-amino-2-chloro-5-hydroxy-
(RS)-2-chloro-5-hydroxyphenylglycine α-amino-2-chloro-5-hydroxybenzeneacetic acid
α-Amino-2-chloro-5-hydroxybenzeneacetic acid, (RS)-2-Chloro-5-hydroxyphenylglycine | [Molecular Formula]
C8H8ClNO3 | [MDL Number]
MFCD01321059 | [MOL File]
170846-74-9.mol | [Molecular Weight]
201.61 |
| Hazard Information | Back Directory | [Description]
(R,S)-CHPG is a potent and selective agonist at metabotropic glutamate receptor 5 (mGluR5). In CHO cells, it had an EC50 of 750 μM for calcium mobilization in mGluR5a-expressing cells but was inactive in mGluR1a-expressing cells. In transfected HEK293 cells, (R,S)-CHPG bound mGluR1a and mGluR5a (Kis = 0.9 and 3.9 μM, respectively) but not ionotropic glutamate receptors. It reduced oxidative stress and inflammatory markers in cultured BV-2 microglial cells. In mouse models of traumatic brain injury, it reduced lesion volume, improved sensorimotor deficits in the beam walk test, and improved spatial memory in the Morris water maze. | [Uses]
CHPG is a selective mGluR-5 agonist. | [Biological Activity]
A selective mGlu 5 metabotropic glutamate receptor agonist, completely inactive at mGlu 1a receptors expressed in CHO cells. Active in vivo . | [in vitro]
(r,s)-2-chloro-5-hydroxyphenylglycine [chpg] selectively activated mglu5a receptors with no activation of mglu1a receptors. this selective mglu5 receptor agonist also enhances nmda-induced depolarizations in rat hippocampalslices. chpg may be used to study the role of mglu5 receptors in the cns [1]. | [in vivo]
to compare the effects of treatment with the newly developed selective mglur5 antagonist mpep and the selective mglur5 agonist chpg in a rat intraluminal filament model of temporary middle cerebral artery occlusion (mcao), rats, after induction of ischemia for 2 h, were administered mpep or chpg (i.c.v.) beginning 15 or 135 min. measured after either 22 or 70 h of reperfusion measured infarct size, and quantified neurological function at 2, 24, 48 and 72 h. 24 h infarct volumes after treatment with mpep or chpg at 15 min were reduced by 61 and 44%, respectively. the neuroprotective effects were dose-dependent. the neuroprotective effects were eliminated by delaying mpep treatment until 135 min. in other studies, with early mpep treatment (15 min) at optimal doses, infarct volume was reduced by 44% at 72 h, being correlated with significant neurological recovery [2]. | [storage]
+4°C (desiccate) | [References]
[1] doherty aj, palmer mj, henley jm, collingridge gl, jane de. (rs)-2-chloro-5-hydroxyphenylglycine (chpg) activates mglu5, but no mglu1, receptors expressed in cho cells and potentiates nmda responses in the hippocampus. neuropharmacology. 1997 feb;36(2):265-7.
[2]. bao wl, williams aj, faden ai, tortella fc. selective mglur5 receptor antagonist or agonist provides neuroprotection in a rat model of focal cerebral ischemia. brain res. 2001 dec 20;922(2):173-9. |
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