Literature DB >> 15081042

Indoline derivatives as 5-HT(2C) receptor agonists.

J M Bentley1, D R Adams, D Bebbington, K R Benwell, M J Bickerdike, J E P Davidson, C E Dawson, C T Dourish, M A J Duncton, S Gaur, A R George, P R Giles, R J Hamlyn, G A Kennett, A R Knight, C S Malcolm, H L Mansell, A Misra, N J T Monck, R M Pratt, K Quirk, J R A Roffey, S P Vickers, I A Cliffe.   

Abstract

A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT(2C) receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for all of the compounds at 5-HT(2) receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration.

Entities:  

Mesh：

Substances：

Year:  2004        PMID： 15081042     DOI： 10.1016/j.bmcl.2003.05.001

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


  9 in total

Review 1.  Serotonergic drugs : effects on appetite expression and use for the treatment of obesity.

Authors:  Jason C G Halford; Joanne A Harrold; Emma J Boyland; Clare L Lawton; John E Blundell
Journal:  Drugs       Date:  2007       Impact factor: 9.546

2.  Synthesis and structure-affinity relationships of novel small molecule natural product derivatives capable of discriminating between serotonin 5-HT1A, 5-HT2A, 5-HT2C receptor subtypes.

Authors:  David F Cummings; Diana C Canseco; Pratikkumar Sheth; James E Johnson; John A Schetz
Journal:  Bioorg Med Chem       Date:  2010-05-15       Impact factor: 3.641

3.  Repeated 7-Day Treatment with the 5-HT2C Agonist Lorcaserin or the 5-HT2A Antagonist Pimavanserin Alone or in Combination Fails to Reduce Cocaine vs Food Choice in Male Rhesus Monkeys.

Authors:  Matthew L Banks; S Stevens Negus
Journal:  Neuropsychopharmacology       Date:  2016-11-18       Impact factor: 7.853

4.  Endocrine and neurochemical effects of 3,4-methylenedioxymethamphetamine and its stereoisomers in rhesus monkeys.

Authors:  K S Murnane; W E Fantegrossi; J R Godfrey; M L Banks; L L Howell
Journal:  J Pharmacol Exp Ther       Date:  2010-05-13       Impact factor: 4.030

5.  Pharmacological characterisation of the agonist radioligand binding site of 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors.

Authors:  Antony R Knight; Anil Misra; Kathleen Quirk; Karen Benwell; Dean Revell; Guy Kennett; Mike Bickerdike
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2004-07-30       Impact factor: 3.000

6.  Support for 5-HT2C receptor functional selectivity in vivo utilizing structurally diverse, selective 5-HT2C receptor ligands and the 2,5-dimethoxy-4-iodoamphetamine elicited head-twitch response model.

Authors:  Clinton E Canal; Raymond G Booth; Drake Morgan
Journal:  Neuropharmacology       Date:  2013-01-23       Impact factor: 5.250

7.  Palladium(0)-catalyzed Heck reaction/C-H activation/amination sequence with diaziridinone: a facile approach to indolines.

Authors:  Huaiji Zheng; Yingguang Zhu; Yian Shi
Journal:  Angew Chem Int Ed Engl       Date:  2014-09-04       Impact factor: 15.336

8.  From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells.

Authors:  Irina N Gaisina; Franck Gallier; Andrei V Ougolkov; Ki H Kim; Toru Kurome; Songpo Guo; Denise Holzle; Doris N Luchini; Sylvie Y Blond; Daniel D Billadeau; Alan P Kozikowski
Journal:  J Med Chem       Date:  2009-04-09       Impact factor: 7.446

Review 9.  Pharmacological targeting of the serotonergic system for the treatment of obesity.

Authors:  Alastair S Garfield; Lora K Heisler
Journal:  J Physiol       Date:  2008-11-24       Impact factor: 5.182
  9 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.