| Bioactivity | VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents[1]. | ||||||||||||
| In Vivo | VU0650786 (VU786) (i.p., 30 mg/kg) increases the proportion of c-Fos-positive cells by approximately 4-fold, enhances synaptic strength in cone cell subpopulations, weakens thalamocortical long-term depression (LTD), and reduces passive coping in acute models of antidepressant-like activity in inducible cFos-EGFP mice[2].The pharmacokinetic parameters of VU0650786 (compound 106) in rats[1]. Parameters | ||||||||||||
| Name | VU0650786 | ||||||||||||
| CAS | 1809085-30-0 | ||||||||||||
| Formula | C18H15ClFN5O2 | ||||||||||||
| Molar Mass | 387.80 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Engers JL, et al. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J Med Chem. 2015 Sep 24;58(18):7485-500. [2]. Max E Joffe, et al. mGlu2 and mGlu3 Negative Allosteric Modulators Divergently Enhance Thalamocortical Transmission and Exert Rapid Antidepressant-like Effects. Neuron. 2020 Jan 8;105(1):46-59.e3. |
VU0650786
CAS: 1809085-30-0 F: C18H15ClFN5O2 W: 387.80
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subty
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