货号 | 16295-1mg |
描述 | Metabotropic glutamate receptors (mGluRs) modulate brain excitability through diverse mechanisms.1 VU0361737 is a selective positive allosteric modulator (PAM) of mGluR4, displaying EC50 values of 110 and 240 nM for rat and human receptors, respectively.2 It has weak or no activity at other mGluRs.2 VU0361737 passes the blood-brain barrier to act centrally in rats.2,3 VU0361737, alone or in combination with an mGluR2 selective PAM, does not potentiate glutamate responses through mGlu2/4 heterodimers.4 |
供应商 | Cayman |
应用文献 | |
1.Schoepp, D.D. Unveiling the functions of presynaptic metabotropic glutamate receptors in the central nervous system. Journal of Pharmacology and Experimental Therapeutics 299(1), 12-20 (2001). 2.Engers, D.W.,Niswender, C.M.,Weaver, C.D., et al. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). Journal of Medicinal Chemistry 52(14), 4115-4118 (2009). 3.Engers, D.W.,Field, J.R.,Le, U., et al. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. Journal of Medicinal Chemistry 54(4), 1106-1110 (2011). 4.Kammermeier, P.J. Functional and pharmacological characteristics of metabotropic glutamate receptors 2/4 heterodimers. Molecular Pharmacology 82(3), 438-447 (2012). | |
运输条件 | Wet ice in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 262.7 |
分子式 | C13H11ClN2O2 |
CAS号 | 1161205-04-4 |
稳定性 | ≥ 2 years |
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