PHCCC

PHCCC is a Group I metabotropic glutamate receptor antagonist with EC50 of 6 uM and a positive allosteric modulator of mGluR4. Also as a potent to antagonism for mGluR2 and mGluR8.target: a Group I metabotropic glutamate receptor antagonistEC 50: 6 uMIn vitro: PHCCC potentiates L-AP4-mediated inhibition of striatopallidal synaptic transmission in vitro. 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.

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.