Literature DB >> 11055342

N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.

Y Tsai1, M Dukat, A Slassi, N MacLean, L Demchyshyn, J E Savage, B L Roth, S Hufesein, M Lee, R A Glennon.   

Abstract

N-Benzenesulfonyl-5-methoxy-N,N-dimethyltryptamine (BS/5-OMe DMT; 5) was shown to bind at human 5-HT6 serotonin receptors with high affinity (Ki = 2.3 nM) relative to serotonin (Ki = 78 nM). Structural variation failed to result in significantly enhanced affinity. BS/5-OMe DMT acts as an antagonist of 5-HT-stimulated adenylate cyclase (pA2 = 8.88 nM) and may represent the first member of a novel class of 5-HT6 antagonists.

Entities:  

Mesh：

Substances：

Year:  2000        PMID： 11055342     DOI： 10.1016/s0960-894x(00)00453-4

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  7 in total

1.  Synthesis, pharmacological evaluations, and molecular docking studies on a new 1,3,4,11b-tetrahydro-1H-fluoreno[9,1-cd]azepine framework: Rigidification of D1 receptor selective 1-phenylbenzazepines and discovery of a new 5-HT6 receptor scaffold.

Authors:  Rajan Giri; Ian Alberts; Wayne W Harding
Journal:  Chem Biol Drug Des       Date:  2020-04-22       Impact factor: 2.817

2.  Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.

Authors:  Ramakrishna V S Nirogi; Prabhakar Kothmirkar; Ramasastri Kambhampati; Jagadish Babu Konda; Sobhanadri Arepalli; Narasimhareddy G Pamuleti; Amol D Deshpande; Trinathreddy Bandyala; Anil K Shinde; P K Dubey
Journal:  ACS Med Chem Lett       Date:  2010-06-24       Impact factor: 4.345

Review 3.  The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs.

Authors:  Richard A Glennon; Uma Siripurapu; Bryan L Roth; Renata Kolanos; Mikhail L Bondarev; Donald Sikazwe; Mase Lee; Małgorzata Dukat
Journal:  Curr Top Med Chem       Date:  2010       Impact factor: 3.295

4.  Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.

Authors:  Małgorzata Dukat; Philip D Mosier; Renata Kolanos; Bryan L Roth; Richard A Glennon
Journal:  J Med Chem       Date:  2008-01-18       Impact factor: 7.446

5.  Reversal of a cholinergic-induced deficit in a rodent model of recognition memory by the selective 5-HT6 receptor antagonist, Ro 04-6790.

Authors:  Marie L Woolley; Charles A Marsden; Andrew J Sleight; Kevin C F Fone
Journal:  Psychopharmacology (Berl)       Date:  2003-09-10       Impact factor: 4.530

6.  The effect of the intramolecular C-H⋯O interactions on the conformational preferences of bis-arylsulfones - 5-HT6 receptor antagonists and beyond.

Authors:  Justyna Kalinowska-Tłuścik; Jakub Staroń; Anna Krawczuk; Stefan Mordalski; Dawid Warszycki; Grzegorz Satała; Adam S Hogendorf; Andrzej J Bojarski
Journal:  RSC Adv       Date:  2018-05-22       Impact factor: 4.036

7.  Novel N-Arylsulfonylindoles Targeted as Ligands of the 5-HT6 Receptor. Insights on the Influence of C-5 Substitution on Ligand Affinity.

Authors:  Loreto Arrieta-Rodríguez; Daniela Espinoza-Rosales; Gonzalo Vera; Young Hwa Cho; David Cabezas; David Vásquez-Velásquez; Jaime Mella-Raipán; Carlos F Lagos; Gonzalo Recabarren-Gajardo
Journal:  Pharmaceuticals (Basel)       Date:  2021-06-01
  7 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.