N-Skatyltryptamines-Dual 5-HT6R/D2R Ligands with Antipsychotic and Procognitive Potential was written by Hogendorf, Agata;Hogendorf, Adam S.;Kurczab, Rafal;Satala, Grzegorz;Szewczyk, Bernadeta;Cieslik, Paulina;Latacz, Gniewomir;Handzlik, Jadwiga;Lenda, Tomasz;Kaczorowska, Katarzyna;Staron, Jakub;Bugno, Ryszard;Duszynska, Beata;Bojarski, Andrzej J.. And the article was included in Molecules in 2021.Product Details of 146939-27-7 This article mentions the following:
A series of N-skatyltryptamines was synthesized and their affinities for serotonin and dopamine receptors were determined Compounds exhibited activity toward 5-HT1A, 5-HT2A, 5-HT6, and D2 receptors. Substitution patterns resulting in affinity/activity switches were identified and studied using homol. modeling. Chosen hits were screened to determine their metabolism, permeability, hepatotoxicity, and CYP inhibition. Several D2 receptor antagonists with addnl. 5-HT6R antagonist and agonist properties were identified. The former combination resembled known antipsychotic agents, while the latter was particularly interesting due to the fact that it has not been studied before. Selective 5-HT6R antagonists have been shown previously to produce procognitive and promnesic effects in several rodent models. Administration of 5-HT6R agonists was more ambiguous-in naive animals, it did not alter memory or produce slight amnesic effects, while in rodent models of memory impairment, they ameliorated the condition just like antagonists. Using the identified hit compounds 15 and 18, we tried to sort out the difference between ligands exhibiting the D2R antagonist function combined with 5-HT6R agonism, and mixed D2/5-HT6R antagonists in murine models of psychosis. In the experiment, the researchers used many compounds, for example, 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7Product Details of 146939-27-7).
5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one (cas: 146939-27-7) belongs to isothiazole derivatives. Some representatives of isothiazoles have proven to be synergists of bioactive substances, which opens the way to lower the doses of drugs used and is especially important in cancer chemotherapy. It has been found that isothiazole-based compounds show synergistic effects when used with other biocidal compounds.Product Details of 146939-27-7
Referemce:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com