892273-40-4Relevant academic research and scientific papers
Synthesis and biological study of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3] triazolo[1,5-a]pyrimidines as potent and selective serotonin 5-HT6 receptor antagonists
Ivachtchenko, Alexandre V.,Golovina, Elena S.,Kadieva, Madina G.,Koryakova, Angela G.,Kovalenko, Sergiy M.,Mitkin, Oleg D.,Okun, Ilya M.,Ravnyeyko, Irina M.,Tkachenko, Sergey E.,Zaremba, Oleg V.
experimental part, p. 5282 - 5290 (2010/09/06)
A number of 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a] pyrimidines were prepared and their 5-HT6 receptor binding affinity and ability to inhibit the functional cellular responses to serotonin were evaluated. 3-[(3-Chlorophenyl)sulfonyl]-N-(tetrahydrofuran-2-ylmethyl)thieno[2, 3-e][1,2,3]triazolo[1,5-a]pyrimidin-5-amine 2{5,26} appeared to be the most active in a functional assay (IC50 = 29.0 nM) and 3-(phenylsulfonyl)-N-(2-thienylmethyl) thieno[2,3-e][1,2,3]triazolo[1,5-a] pyrimidin-5-amine 2{1,28} demonstrated the greatest affinity in a 5-HT 6 receptor radioligand binding assay (Ki = 1.7 nM). A screening of 5-HT2A and 5-HT2B receptor affinity revealed that 3-(phenylsulfonyl)thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines are highly selective 5-HT6 receptor ligands.
