Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators

Cannabinoid 1 receptor (CB1R) allosteric ligands hold a far-reaching therapeutic promise. We report the application of fluoro- and nitrogen-walk approaches to enhance the drug-like properties of GAT211, a prototype CB1R allosteric agonist-positive allosteric modulator (ago-PAM). Several analogs exhi...

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Veröffentlicht in:	Journal of medicinal chemistry Jg. 63; H. 2; S. 542 - 568
Hauptverfasser:	Garai, Sumanta, Kulkarni, Pushkar M., Schaffer, Peter C., Leo, Luciana M., Brandt, Asher L., Zagzoog, Ayat, Black, Tallan, Lin, Xiaoyan, Hurst, Dow P., Janero, David R., Abood, Mary E., Zimmowitch, Anaelle, Straiker, Alex, Pertwee, Roger G., Kelly, Melanie, Szczesniak, Anna-Maria, Denovan-Wright, Eileen M., Mackie, Ken, Hohmann, Andrea G., Reggio, Patricia H., Laprairie, Robert B., Thakur, Ganesh A.
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	WASHINGTON Amer Chemical Soc 23.01.2020
Schlagworte:	Chemistry, Medicinal Life Sciences & Biomedicine Pharmacology & Pharmacy Science & Technology NEUROPATHIC PAIN DESIGN CB1 PROTEIN AGONISM SIGNALING SYSTEM ENDOCANNABINOID SYSTEM INTRAOCULAR-PRESSURE SELECTIVITY STRATEGIES
ISSN:	0022-2623, 1520-4804, 1520-4804
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