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Submit ReviewA 77636 hydrochloride is a potent and selective dopamine D1-like receptor agonist (pEC50 values are 8.97 and < 5 for D1-like and D2-like receptors respectively). Displays anti-Parkinsonian activity following oral administration in vivo. Exhibits 11-fold cell type bias over dopamine in a functional assay in U2 cells.
分子量 | 365.9 |
公式 | C20H27NO3.HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 145307-34-2 |
PubChem ID | 9811493 |
InChI Key | RSJAXPUYVJKAAA-JPGJPTAESA-N |
Smiles | NC[C@@H]2O[C@H]([C@]35CC(CC(C5)C4)CC4C3)CC1=C(O)C(O)=CC=C12.Cl |
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 | |||
water | 36.59 | 100 |
以下数据基于产品分子量 365.9。 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 |
---|---|---|---|
1 mM | 2.73 mL | 13.66 mL | 27.33 mL |
5 mM | 0.55 mL | 2.73 mL | 5.47 mL |
10 mM | 0.27 mL | 1.37 mL | 2.73 mL |
50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
参考文献是支持产品生物活性的出版物。
Acquas et al (1994) The potent and selective DA D1 receptor agonist A-77636 increases cortical and hippocampal acetylcholine release in the rat. Eur.J.Pharmacol. 260 85 PMID: 7957630
Kebabian et al (1992) A-77636: a potent and selective DA D1 receptor agonist with antiparkinsonian activity in marmosets. Eur.J.Pharmacol. 229 203 PMID: 1362704
Lewis et al (1998) Homologous desensitization of the D1A DA receptor: efficacy in causing desensitization dissociates from both receptor occupancy and functional potency. J.Pharmacol.Exp.Ther. 286 345 PMID: 9655879
If you know of a relevant reference for A 77636 hydrochloride, please let us know.
关键词: A 77636 hydrochloride, A 77636 hydrochloride supplier, Potent, selective, D1-like, agonists, Orally, active, Dopamine, D1, Receptors, D5, dopaminergic, A77636, hydrochloride, biased, agonism, and, 1701, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 A 77636 hydrochloride 的部分引用包括:
Chan et al (2012) Target identification by chromatographic co-elution: monitoring of drug-protein interactions without immobilization or chemical derivatization. Mol Cell Proteomics 11 M111.016642 PMID: 22357554
Guha et al (2012) Stimulation of the D5 DA receptor acidifies the lysosomal pH of retinal pigmented epithelial cells and decreases accumulation of autofluorescent photoreceptor debris. J Neurochem 122 823 PMID: 22639870
Zalocusky et al (2016) Nucleus accumbens D2R cells signal prior outcomes and control risky decision-making. Nature 531 642 PMID: 27007845
Lee et al (2018) The small molecule CA140 inhibits the neuroinflammatory response in wild-type mice and a mouse model of AD. J Neuroinflammation 15 286 PMID: 30309372
Chai et al (2017) Neural Circuit-Specialized Astrocytes: Transcriptomic, Proteomic, Morphological, and Functional Evidence. Neuron 95 531 PMID: 28712653
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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。
Written by Phillip Strange and revised by Kim Neve in 2013, this review summarizes the history of the dopamine receptors and provides an overview of individual receptor subtype properties, their distribution and identifies ligands which act at each receptor subtype. Compounds available from Tocris are listed.
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.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.