Literature DB >> 19101959

(2,2-Diphenyl-[1,3]oxathiolan-5-ylmethyl)-(3-phenyl-propyl)-amine: a potent and selective 5-HT(1A) receptor agonist.

Silvia Franchini1, Annalisa Tait, Adolfo Prandi, Claudia Sorbi, Rossella Gallesi, Michela Buccioni, Gabriella Marucci, Carla De Stefani, Antonio Cilia, Livio Brasili.   

Abstract

Starting from compound 1, a previously reported alpha(1D)-adrenoceptors antagonist, a new series of ligands acting at 5-HT(1A) serotonin receptor were identified through simple structure modifications. Among them (2,2-diphenyl-[1,3]oxathiolan-5-yl-methyl)-(3-phenyl-propyl)amine (19) exhibits outstanding activity (pK(i)=8.72, pD(2)=7.67, E(max)=85) and selectivity (5-HT(1A)/alpha(1D)>150), and represents an as yet unidentified 5-HT(1A) agonist scaffold.

Entities:  

Mesh：

Substances：

Year:  2009        PMID： 19101959     DOI： 10.1002/cmdc.200800276

Source DB:  PubMed          Journal:  ChemMedChem        ISSN： 1860-7179            Impact factor:   3.466


  3 in total

1.  Classification of 5-HT(1A) receptor agonists and antagonists using GA-SVM method.

Authors:  Xue-lian Zhu; Hai-yan Cai; Zhi-jian Xu; Yong Wang; He-yao Wang; Ao Zhang; Wei-liang Zhu
Journal:  Acta Pharmacol Sin       Date:  2011-10-03       Impact factor: 6.150

2.  Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices Analysis (CoMSIA) studies on α(1A)-adrenergic receptor antagonists based on pharmacophore molecular alignment.

Authors:  Xin Zhao; Minsheng Chen; Biyun Huang; Hong Ji; Mu Yuan
Journal:  Int J Mol Sci       Date:  2011-10-20       Impact factor: 5.923

3.  Exhaustive CoMFA and CoMSIA analyses around different chemical entities: a ligand-based study exploring the affinity and selectivity profiles of 5-HT1A ligands.

Authors:  Sara Guariento; Silvia Franchini; Michele Tonelli; Paola Fossa; Claudia Sorbi; Elena Cichero; Livio Brasili
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.