Product Details of 61-82-5. I found the field of Pharmacology & Pharmacy very interesting. Saw the article Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5 published in 2019.0, Reprint Addresses IJzerman, AP (corresponding author), Leiden Univ, Div Drug Discovery & Safety, Leiden Acad Ctr Drug Res, POB 9502, NL-2300 RA Leiden, Netherlands.. The CAS is 61-82-5. Through research, I have a further understanding and discovery of 1H-1,2,4-Triazol-5-amine.
CC chemokine receptors 2 (CCR2) and 5 (CCR5) are involved in many inflammatory diseases; however, most CCR2 and CCR5 clinical candidates have been unsuccessful. (Pre)clinical evidence suggests that dual CCR2/CCR5 inhibition might be more effective in the treatment of such multifactorial diseases. In this regard, the highly conserved intracellular binding site in chemokine receptors provides a new avenue for the design of multitarget ligands. In this study, we synthesized and evaluated the biological activity of a series of triazolopyrimidinone derivatives in CCR2 and CCR5. Radioligand binding assays first showed that they bind to the intracellular site of CCR2, and in combination with functional assays on CCR5, we explored structure-affinity/activity relationships in both receptors. Although most compounds were CCR2-selective, 39 and 43 inhibited beta-arrestin recruitment in CCR5 with high potency. Moreover, these compounds displayed an insurmountable mechanism of inhibition in both receptors, which holds promise for improved efficacy in inflammatory diseases.
Product Details of 61-82-5. Welcome to talk about 61-82-5, If you have any questions, you can contact Zacarias, NVO; van Veldhoven, JPD; den Hollander, LS; Dogan, B; Openy, J; Hsiao, YY; Lenselink, EB; Heitman, LH; IJzerman, AP or send Email.
Reference:
Article; Safari, Niloufar; Shirini, Farhad; Tajik, Hassan; Journal of Molecular Structure; vol. 1201; (2020);,
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