PHCCC 是 I 组 mGluR 拮抗剂，IC50 为 3 μM。 PHCCC 是 mGlu4 受体的选择性正调节剂。抗帕金森效应。
| Cas No. | 179068-02-1 |
| 别名 | N-苯基-7-(羟基亚胺基)环丙烯并[B]苯并吡喃-1A-甲酰胺 |
| 化学名 | (1aS,7aS,Z)-7-(hydroxyimino)-N-phenyl-1,1a,7,7a-tetrahydrocyclopropa[b]chromene-1a-carboxamide |
| Canonical SMILES | O=C([C@]1([C@H]/2C1)OC3=CC=CC=C3C2=N/O)NC4=CC=CC=C4 |
| 分子式 | C17H14N2O3 |
| 分子量 | 294.31 |
| 溶解度 | Soluble in DMSO |
| 储存条件 | Store at RT |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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. |
