An article Application of Fluorine- and Nitrogen-Walk Approaches: Defining the Structural and Functional Diversity of 2-Phenylindole Class of Cannabinoid 1 Receptor Positive Allosteric Modulators WOS:000509438800006 published article about ENDOCANNABINOID SYSTEM; INTRAOCULAR-PRESSURE; NEUROPATHIC PAIN; SIGNALING SYSTEM; CB1; PROTEIN; STRATEGIES; DESIGN; SELECTIVITY; AGONISM in [Garai, Sumanta; Kulkarni, Pushkar M.; Schaffer, Peter C.; Thakur, Ganesh A.] Northeastern Univ, Bouve Coll Hlth Sci, Sch Pharm, Dept Pharmaceut Sci, Boston, MA 02115 USA; [Brandt, Asher L.; Zagzoog, Ayat; Black, Tallan; Laprairie, Robert B.] Univ Saskatchewan, Coll Pharm & Nutr, 104 Clin Pl, Saskatoon, SK S7N 2Z4, Canada; [Leo, Luciana M.; Abood, Mary E.] Temple Univ, Lewis Katz Sch Med, Ctr Subst Abuse Res, Philadelphia, PA 19140 USA; [Hurst, Dow P.; Reggio, Patricia H.] Univ North Carolina Greensboro, Ctr Drug Discovery, Greensboro, NC 27402 USA; [Janero, David R.] Northeastern Univ, Bouve Coll Hlth Sci, Coll Sci & Hlth Sci Entrepreneurs, Dept Chem & Chem Biol,Dept Pharmaceut Sci, Boston, MA 02115 USA; [Lin, Xiaoyan; Zimmowitch, Anaelle; Straiker, Alex; Mackie, Ken; Hohmann, Andrea G.] Indiana Univ, Program Neurosci Psychol & Brain Sci, Bloomington, IN 47405 USA; [Lin, Xiaoyan; Zimmowitch, Anaelle; Straiker, Alex; Mackie, Ken; Hohmann, Andrea G.] Indiana Univ, Gill Ctr Biomol Sci, Bloomington, IN 47405 USA; [Kelly, Melanie; Szczesniak, Anna-Maria; Denovan-Wright, Eileen M.; Laprairie, Robert B.] Dalhousie Univ, Fac Med, Dept Pharmacol, 5850 Coll St, Halifax, NS B3H 4R2, Canada; [Pertwee, Roger G.] Univ Aberdeen, Inst Med Sci, Sch Med Med Sci & Nutr, Aberdeen AB25 2ZD, Scotland in 2020.0, Cited 69.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Quality Control of 3-Pyridinecarboxaldehyde
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 exhibited improved functional potency (cAMP, beta-arrestin 2), metabolic stability, and aqueous solubility. Two key analogs, GAT591 (6r) and GAT593 (6s), exhibited augmented allosteric-agonist and PAM activities in neuronal cultures, improved metabolic stability, and enhanced orthosteric agonist binding (CP55,940). Both analogs also exhibited good analgesic potency in the CFA inflammatory-pain model with longer duration of action over GAT211 while being devoid of adverse cannabimimetic effects. Another analog, GAT592 (9j), exhibited moderate ago-PAM potency and improved aqueous solubility with therapeutic reduction of intraocular pressure in murine glaucoma models. The SAR findings and the enhanced allosteric activity in this class of allosteric modulators were accounted for in our recently developed computational model for CB1R allosteric activation and positive allosteric modulation. [GRAPHICS] .
Quality Control of 3-Pyridinecarboxaldehyde. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Garai, S; Kulkarni, PM; Schaffer, PC; Leo, LM; Brandt, AL; Zagzoog, A; Black, T; Lin, XY; Hurst, DP; Janero, DR; Abood, ME; Zimmowitch, A; Straiker, A; Pertwee, RG; Kelly, M; Szczesniak, AM; Denovan-Wright, EM; Mackie, K; Hohmann, AG; Reggio, PH; Laprairie, RB; Thakur, GA or concate me.
Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem