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Submit ReviewCDPPB is a brain penetrant, selective positive allosteric modulator at the mGlu5 receptor (EC50 values are 10 and 20 nM for human and rat receptors respectively). Antipsychotic; reverses amphetamine-induced locomotor activity and amphetamine-induced deficits in prepulse inhibition in rats.
Manufactured and sold under license from Merck & Co., Inc. for use solely for preclinical research purposes (ie: not for administration to or other use in humans)
CDPPB is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 364.4 |
公式 | C23H16N4O |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 781652-57-1 |
PubChem ID | 11245456 |
InChI Key | BKUIZWILNWHFHD-UHFFFAOYSA-N |
Smiles | O=C(C4=CC(C#N)=CC=C4)NC1=CC(C3=CC=CC=C3)=NN1C2=CC=CC=C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 27.33 | 75 |
以下数据基于产品分子量 364.4。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.75 mM | 3.66 mL | 18.29 mL | 36.59 mL |
3.75 mM | 0.73 mL | 3.66 mL | 7.32 mL |
7.5 mM | 0.37 mL | 1.83 mL | 3.66 mL |
37.5 mM | 0.07 mL | 0.37 mL | 0.73 mL |
参考文献是支持产品生物活性的出版物。
Lindsley et al (2004) Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides that potentiate receptor function in vivo. J.Med.Chem. 47 5825 PMID: 15537338
Kinney et al (2005) A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rats behavioral models. J.Pharmacol.Exp.Ther. 313 199 PMID: 15608073
Chen et al (2007) Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol.Pharmacol. 71 1389 PMID: 17303702
If you know of a relevant reference for CDPPB, please let us know.
关键词: CDPPB, CDPPB supplier, Positive, allosteric, modulators, mGlu5, mGluR5, mGlur, Group, I, Receptors, Glutamate, Metabotropic, merck, PAM, (Metabotropic), 3235, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 CDPPB 的部分引用包括:
Pacey et al (2011) Subchronic administration and combination metabotropic glutamate and GABAB receptor drug therapy in fragile X syndrome. Front Pharmacol 338 897 PMID: 21636656
Arsenault et al (2015) Loss of Metabotropic Glutamate Receptor 5 Function on Peripheral Benzodiazepine Receptor in Mice Prenatally Exposed to LPS. PLoS One 10 e0142093 PMID: 26536027
Vicidomini et al (2017) Pharmacological enhancement of mGlu5 receptors rescues behavioral deficits in SHANK3 knock-out mice. Mol Psychiatry 22 689 PMID: 27021819
Bellozi et al (2019) A positive allosteric modulator of mGluR5 promotes neuroprotective effects in mice models of Alzheimer's disease. Neuropharmacology. 160 107785 PMID: 31541651
Martinez et al (2016) OE Facilitation of Cocaine Self-Administration in Female Rats Requires Activation of mGluR5. Eneuro 3 PMID: 27822496
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
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