The Cis regioisomer of VU0155041 demonstrates similar potency, with 798±58 nM at human mGluR4 and 693±140 nM at rat mGluR4. In contrast, the concentration-response curve for the Trans regioisomer (VU0155040) does not plateau at the maximum concentration tested. At 30 μM, the Cis regioisomer of VU0155041 is more effective in inducing shifts in baseline in fold-shift experiments using the thallium flux assay, reaching about 45% of the maximal response seen with glutamate. VU0155041 acts as a partial agonist of mGluR4 by interacting with a site distinct from the glutamate binding site and shows selectivity for mGluR4 over 67 different targets, without affecting striatal NMDA receptor function[1].
体内研究
VU0155041 is water-soluble and its intracerebroventricular administration in doses ranging from 31 to 316 nmol dose-dependently alleviates haloperidol-induced catalepsy and reserpine-induced akinesia in rats. Specifically, doses of 31 and 92 nmol of VU0155041 significantly reduce the cataleptic effects of haloperidol, with effects persisting for 30 minutes post-infusion. A dose of 316 nmol of VU0155041 significantly reverses akinesia following administration[1].
体外研究
The Cis regioisomer of VU0155041 demonstrates similar potency, with 798±58 nM at human mGluR4 and 693±140 nM at rat mGluR4. In contrast, the concentration-response curve for the Trans regioisomer (VU0155040) does not plateau at the maximum concentration tested. At 30 μM, the Cis regioisomer of VU0155041 is more effective in inducing shifts in baseline in fold-shift experiments using the thallium flux assay, reaching about 45% of the maximal response seen with glutamate. VU0155041 acts as a partial agonist of mGluR4 by interacting with a site distinct from the glutamate binding site and shows selectivity for mGluR4 over 67 different targets, without affecting striatal NMDA receptor function[1].
搜索
