📜对甲基苯甲酸甲酯 在 N-溴代丁二酰亚胺(Nbs),偶氮二异丁腈,溴,Potassium Carbonate,Sodium Hydroxide,Lithium Diisopropyl Amide体系中,用 四氢呋喃,甲醇,四氯化碳,二氯甲烷作为反应溶剂,反应 28.5H,获得 4-[Bromo-(4-Carboxyphenyl)Methylene]-Piperidine-1-Carboxylic Acid Tert-Butyl Ester
参考文献:Tuned-Affinity Bivalent Ligands For The Characterization Of Opioid Receptor Heteromers
标题:Tuned-Affinity Bivalent Ligands For The Characterization Of Opioid Receptor Heteromers
摘要:Opioid Receptors,Including The Mu-And Delta-Opioid Receptors (Mor And Dor),Are Important Targets For The Treatment Of Pain. Although There Is Mounting Evidence That These Receptors Form Heteromers,The Functional Role Of The Mor/Dor Heteromer Remains Unresolved. We Have Designed And Synthesized Bivalent Ligands As Tools To Elucidate The Functional Role Of The Mor/Dor Heteromer. Our Ligands (L2 And L4) Are Comprised Of A Compound With Low Affinity At The Dor Tethered To A Compound With High Affinity At The Mor,With The Goal Of Producing Ligands With "Tuned Affinity" At Mor/Dor Heteromers As Compared To Dor Homomers. Here,We Show That Both L2 And L4 Demonstrate Enhanced Affinity At Mor/Dor Heteromers As Compared To Dor Homomers,Thereby Providing Unique Pharmacological Tools To Dissect The Role Of The Mor/Dor Heteromer In Pain.
Doi:10.1021/Ml300083P