AzoCholine Enables Optical Control of Alpha 7 Nicotinic Acetylcholine Receptors in Neural Networks

作者：Damijonaitis Arunas; Broichhagen Johannes; Urushima Tatsuya; Huell Katharina; Nagpal Jatin; Laprell Laura; Schoenberger Matthias; Woodmansee David H; Rafiq Amir; Sumser Martin P; Kummer Wolfgang; Gottschalk Alexander; Trauner Dirk^*

来源：ACS Chemical Neuroscience, 2015, 6(5): 701-707.

DOI：10.1021/acschemneuro.5b00030

• Photopharmacology
• photochromic ligand
• AzoCholine
• BisQ
• nicotinic acetylcholine receptor
• cholinergic system

Nicotinic acetylcholine receptors (nAChRs) are essential for cellular communication in higher organisms. Even though a vast pharmacological toolset to study cholinergic systems has been developed, control of endogenous neuronal nAChRs with high spatiotemporal precision has been lacking. To address this issue, we have generated photoswitchable nAChR agonists and re-evaluated the known photochromic ligand, BisQ Using electrophysiology, we found that one of our new compounds, AzoCholine, is an excellent photoswitchable agonist for neuronal alpha 7 nAChRs, whereas BisQ was confirmed to be an agonist for the muscle-type nAChR AzoCholine could be used to modulate cholinergic activity in a brain slice and in dorsal root ganglion neurons. In addition, we demonstrate light-dependent perturbation of behavior in the nematode, Caenorhabditis elegans.

• 出版日期2015-5