Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia

The adenosine A 1 receptor (A 1 R) is a promising therapeutic target for non-opioid analgesic agents to treat neuropathic pain 1 , 2 . However, development of analgesic orthosteric A 1 R agonists has failed because of a lack of sufficient on-target selectivity as well as off-tissue adverse effects 3...

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Veröffentlicht in:	Nature (London) 2021-09, Vol.597 (7877), p.571-576
Hauptverfasser:	Draper-Joyce, Christopher J., Bhola, Rebecca, Wang, Jinan, Bhattarai, Apurba, Nguyen, Anh T. N., Cowie-Kent, India, O’Sullivan, Kelly, Chia, Ling Yeong, Venugopal, Hariprasad, Valant, Celine, Thal, David M., Wootten, Denise, Panel, Nicolas, Carlsson, Jens, Christie, Macdonald J., White, Paul J., Scammells, Peter, May, Lauren T., Sexton, Patrick M., Danev, Radostin, Miao, Yinglong, Glukhova, Alisa, Imlach, Wendy L., Christopoulos, Arthur
Format:	Artikel
Sprache:	eng
Schlagworte:	101/28 631/154/436/2387 631/45/535/1258/1259 96 Adenosine Allosteric properties Analgesia Analgesics Binding Binding sites Drug development Drug dosages Experiments Humanities and Social Sciences Ligands Lipids Molecular dynamics multidisciplinary Narcotics Neuralgia Opioid receptors Pain Pain perception Pharmaceutical sciences Proteins Receptors Science Science (multidisciplinary) Selectivity Spinal cord
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