Novel and Potent Dopamine D2 Receptor Go-Protein Biased Agonists was written by Bonifazi, Alessandro;Yano, Hideaki;Guerrero, Adrian M.;Kumar, Vivek;Hoffman, Alexander F.;Lupica, Carl R.;Shi, Lei;Newman, Amy Hauck. And the article was included in ACS Pharmacology & Translational Science in 2019.SDS of cas: 68867-17-4 This article mentions the following:
The discovery of functionally biased and physiol. beneficial ligands directed toward G-protein coupled receptors (GPCRs) has provided the impetus to design dopamine D2 receptor (D2R) targeted mols. that may be therapeutically advantageous for the treatment of certain neuropsychiatric or basal ganglia related disorders. Here we describe the synthesis of a novel series of D2R agonists linking the D2R unbiased agonist sumanirole with privileged secondary mol. fragments. The resulting ligands demonstrate improved D2R affinity and selectivity over sumanirole. Extensive in vitro functional studies and bias factor anal. led to the identification of a novel class of highly potent Go-protein biased full D2R agonists with more than 10-fold and 1000-fold bias selectivity toward activation of specific G-protein subtypes and β-arrestin, resp. Intracellular electrophysiol. recordings from midbrain dopamine neurons demonstrated that Go-protein selective agonists can elicit prolonged ligand-induced GIRK activity via D2Rs, which may be beneficial in the treatment of dyskinesias associated with dopamine system dysfunction. In the experiment, the researchers used many compounds, for example, Benzothiazole-5-carboxylic acid (cas: 68867-17-4SDS of cas: 68867-17-4).
Benzothiazole-5-carboxylic acid (cas: 68867-17-4) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.SDS of cas: 68867-17-4
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica