The First Structure–Activity Relationship Studies for Designer Receptors Exclusively Activated by Designer Drugs

• Published in: ACS chemical neuroscience Vol. 6; no. 3; pp. 476 - 484
• Main Authors: Chen, Xin, Choo, Hyunah, Huang, Xi-Ping, Yang, Xiaobao, Stone, Orrin, Roth, Bryan L, Jin, Jian
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 18.03.2015
• Subjects: Acetylcholine - pharmacology; Animals; Cholinergic Agonists - pharmacology; Clozapine - analogs & derivatives; Clozapine - pharmacology; Designer Drugs; Dibenzazepines - pharmacology; Humans; Ligands; Receptor, Muscarinic M3 - chemistry; Receptor, Muscarinic M3 - drug effects; Serotonin Antagonists - pharmacology; Signal Transduction - drug effects; Structure-Activity Relationship; neuronal activation; CNO; SAR; hM3Dq; perlapine; DREADD

Over the past decade, two independent technologies have emerged and been widely adopted by the neuroscience community for remotely controlling neuronal activity: optogenetics which utilize engineered channelrhodopsin and other opsins, and chemogenetics which utilize engineered G protein-coupled rece...