Literature DB >> 15808453

Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.

Renata Kolanos1, Uma Siripurapu, Manik Pullagurla, Mohamed Riaz, Vince Setola, Bryan L Roth, Małgorzata Dukat, Richard A Glennon.   

Abstract

To determine if the indolic nitrogen atom is required for the binding of N(1)-benzyltryptamines at h5-HT(6) serotonin receptors, several isotryptamines and indene analogs were examined. The affinity of 3-benzyl-N(1)-(N,N-dimethylaminoethyl)indole (5, K(i)=32nM) and 1-benzyl-3-(N,N-dimethylaminoethyl)indene (11, K(i)=3nM) indicates that the indolic nitrogen atom is not essential for binding.

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Year:  2005        PMID： 15808453     DOI： 10.1016/j.bmcl.2005.02.070

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


  6 in total

1.  Stereoselective Synthesis of Trisubstituted Vinyl Bromides by Addition of Alkynes to Oxocarbenium Ions.

Authors:  Andrew R Ehle; Melissa G Morris; Bryan D Klebon; Glenn P A Yap; Mary P Watson
Journal:  Synlett       Date:  2015-09-14       Impact factor: 2.454

2.  [3,3]-Sigmatropic rearrangement/5-exo-dig cyclization reactions of benzyl alkynyl ethers: synthesis of substituted 2-indanones and indenes.

Authors:  Armen A Tudjarian; Thomas G Minehan
Journal:  J Org Chem       Date:  2011-03-25       Impact factor: 4.354

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.  Further Optimization and Evaluation of Bioavailable, Mixed-Efficacy μ-Opioid Receptor (MOR) Agonists/δ-Opioid Receptor (DOR) Antagonists: Balancing MOR and DOR Affinities.

Authors:  Aubrie A Harland; Larisa Yeomans; Nicholas W Griggs; Jessica P Anand; Irina D Pogozheva; Emily M Jutkiewicz; John R Traynor; Henry I Mosberg
Journal:  J Med Chem       Date:  2015-11-13       Impact factor: 7.446

5.  Antidepressant potential of nitrogen-containing heterocyclic moieties: An updated review.

Authors:  Nadeem Siddiqui; Sandhya Bawa; Ruhi Ali; Obaid Afzal; M Jawaid Akhtar; Bishmillah Azad; Rajiv Kumar
Journal:  J Pharm Bioallied Sci       Date:  2011-04

6.  Synthesis of Spiroindenyl-2-Oxindoles through Palladium-Catalyzed Spirocyclization of 2-Bromoarylamides and Vinyl Bromides.

Authors:  Shuai Yang; Yanghui Zhang
Journal:  Molecules       Date:  2021-12-10       Impact factor: 4.411
  6 in total

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