Cas No.: | 179068-02-1 |
Chemical Name: | N-Phenyl-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide |
SMILES: | C1C\2C1(OC3=CC=CC=C3/C2=N\O)C(=O)NC4=CC=CC=C4 |
Formula: | C17H14N2O3 |
M.Wt: | 294.31 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | PHCCC is a Group I metabotropic glutamate receptor antagonist (IC50 ~ 3 μM).Also a positive allosteric modulator for mGlu4a; potentiates L-AP4-mediated inhibition of striatopallidal synaptic transmission in vitro. Displays antiParkinsonian effects in rats in vivo. |
Target: | target: a Group I metabotropic glutamate receptor antagonist EC 50: 6 uM |
In Vivo: | 1, PHCCC produced antiparkinsonian efficacy in the reserpinized rat model means a significant level of glutamate is available for the activation of the therapeutically relevant mGluR4. 2, The reference for animal administration is 10 mg/kg.(i.p) 3,PHCCC augmentes in vivo genetic and pharmacological models of absence seizures in rats. |
In Vitro: | PHCCC potentiates L-AP4-mediated inhibition of striatopallidal synaptic transmission in vitro. |
References: | [1]. Marino MJ et al. Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment. Proc Natl Acad Sci U S A. 2003 Nov 11;100(23):13668-73. [2]. Maj M et al. (-)-PHCCC, a positive allosteric modulator of mGluR4: characterization, mechanism of action, and neuroprotection. Neuropharmacology. 2003 Dec;45(7):895-906. [3]. Szczurowska E et al. Positive allosteric modulator of mGluR4 PHCCC exhibits proconvulsant action in three models of epileptic seizures in immature rats. Physiol Res. 2012;61(6):619-28. [4]. Domin H et al. Neuroprotective potential of the group III mGlu receptor agonist ACPT-I in animal models of ischemic stroke: In vitro and in vivo studies. Neuropharmacology. 2016 Mar;102:276-94. |