An article Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists WOS:000541741100028 published article about P2X(1) ION-CHANNEL; MOUSE MODEL; ATP; ACTIVATION; EXPRESSION; RESPONSES; NF449; INHIBITOR; PHARMACOLOGY; NUCLEOTIDES in [Tian, Maoqun; Abdelrahman, Aliaa; Azazna, Djamil; Spanier, Claudia; Densborn, Sabrina; Hinz, Sonja; Mueller, Christa E.] Univ Bonn, PharmaCtr Bonn, Pharmaceut Inst, Pharmaceut & Med Chem, D-53121 Bonn, Germany; [Baqi, Younis] Sultan Qaboos Univ, Dept Chem, Fac Sci, Muscat 123, Oman; [Fuentes, Eduardo] Univ Talca, Dept Clin Biochem & Immunohaematol, Thrombosis Res Ctr, Med Technol Sch,Fac Hlth Sci,Interdisciplinary Ct, Talca 3460000, Chile; [Schmid, Ralf] Univ Leicester, Dept Mol & Cell Biol, Leicester LE1 7RH, Leics, England; [Schmid, Ralf] Univ Leicester, Leicester Inst Struct & Chem Biol, Leicester LE1 7RH, Leics, England in 2020, Cited 78. The Name is Isobenzofuran-1(3H)-one. Through research, I have a further understanding and discovery of 87-41-2. Safety of Isobenzofuran-1(3H)-one
Antagonists for the ATP-gated ion channel receptor P2X1 have potential as antithrombotics and for treating hyperactive bladder and inflammation. In this study, salicylanilide derivatives were synthesized based on a screening hit. P2X1 antagonistic potency was assessed in 1321N1 astrocytoma cells stably transfected with the human P2X1 receptor by measuring inhibition of the ATP-induced calcium influx. Structure-activity relationships were analyzed, and selectivity versus other P2X receptor subtypes was assessed. The most potent compounds, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxybenzamide (1, IC50 0.0192 mu M) and N-[3,5-bis(trifluoromethyl)phenyl]-4-chloro-2-hydroxybenzamide (14, IC50 0.0231 mu M), displayed >500-fold selectivity versus P2X2 and P2X3, and 10-fold selectivity versus P2X4 and P2X7 receptors, and inhibited collagen-induced platelet aggregation. They behaved as negative allosteric modulators, and molecular modeling studies suggested an extracellular binding site. Besides selective P2X1 antagonists, compounds with ancillary P2X4 and/or P2X7 receptor inhibition were discovered. These compounds represent the first potent, non-acidic, allosteric P2X1 receptor antagonists reported to date.
Safety of Isobenzofuran-1(3H)-one. About Isobenzofuran-1(3H)-one, If you have any questions, you can contact Tian, MQ; Abdelrahman, A; Baqi, Y; Fuentes, E; Azazna, D; Spanier, C; Densborn, S; Hinz, S; Schmid, R; Muller, CE or concate me.
Reference:
Benzofuran – Wikipedia,
,Benzofuran | C8H6O – PubChem