Literature DB >> 23867168

Structure activity relationship study of benzo[d]thiazol-2(3H)one based σ receptor ligands.

Rohit Bhat1, James A Fishback, Rae R Matsumoto, Jacques H Poupaert, Christopher R McCurdy.   

Abstract

Herein we report the SAR study which involved structural modifications to the linker length, aryl substitution and alkylamine ring size of the benzo[d]thiazol-2(3H)one based sigma receptor (σ) ligands. Many compounds in this series displayed low nanomolar affinity for the σ receptor subtypes. In particular, 8a showed high affinity (σ-1 Ki = 4.5 nM) for σ-1 receptors and moderately high selectivity (483-fold) over σ-2 receptors.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  96 Well; Benzothiazolone; Sigma receptors

Mesh：

Substances：

Year:  2013        PMID： 23867168      PMCID： PMC3762478          DOI： 10.1016/j.bmcl.2013.06.032

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


  23 in total

1.  Involvement of sigma 1 receptors in methamphetamine-induced behavioral sensitization in rats.

Authors:  S Takahashi; T Miwa; K Horikomi
Journal:  Neurosci Lett       Date:  2000-07-28       Impact factor: 3.046

Review 2.  Sigma receptors: potential medications development target for anti-cocaine agents.

Authors:  Rae R Matsumoto; Yun Liu; Megan Lerner; Eric W Howard; Daniel J Brackett
Journal:  Eur J Pharmacol       Date:  2003-05-23       Impact factor: 4.432

3.  A proposal for the classification of sigma binding sites.

Authors:  R Quirion; W D Bowen; Y Itzhak; J L Junien; J M Musacchio; R B Rothman; T P Su; S W Tam; D P Taylor
Journal:  Trends Pharmacol Sci       Date:  1992-03       Impact factor: 14.819

4.  σ1 receptors are involved in the visceral pain induced by intracolonic administration of capsaicin in mice.

Authors:  Rafael González-Cano; Manuel Merlos; José M Baeyens; Cruz M Cendán
Journal:  Anesthesiology       Date:  2013-03       Impact factor: 7.892

5.  The antidepressant-like effect induced by sigma(1)-receptor agonists and neuroactive steroids in mice submitted to the forced swimming test.

Authors:  A Urani; F J Roman; V L Phan; T P Su; T Maurice
Journal:  J Pharmacol Exp Ther       Date:  2001-09       Impact factor: 4.030

6.  Sigma1 receptor modulation of opioid analgesia in the mouse.

Authors:  Jianfeng Mei; Gavril W Pasternak
Journal:  J Pharmacol Exp Ther       Date:  2002-03       Impact factor: 4.030

7.  Involvement of the sigma1 receptor in the cocaine-induced conditioned place preference.

Authors:  P Romieu; R Martin-Fardon; T Maurice
Journal:  Neuroreport       Date:  2000-09-11       Impact factor: 1.837

8.  Involvement of sigma receptors in the behavioral effects of cocaine: evidence from novel ligands and antisense oligodeoxynucleotides.

Authors:  Rae R Matsumoto; Kari A McCracken; Buddy Pouw; Ying Zhang; Wayne D Bowen
Journal:  Neuropharmacology       Date:  2002-06       Impact factor: 5.250

Review 9.  Sigma(1) (sigma(1)) receptor antagonists represent a new strategy against cocaine addiction and toxicity.

Authors:  Tangui Maurice; Rémi Martin-Fardon; Pascal Romieu; Rae R Matsumoto
Journal:  Neurosci Biobehav Rev       Date:  2002-06       Impact factor: 8.989

10.  New positron emission tomography (PET) radioligand for imaging σ-1 receptors in living subjects.

Authors:  Michelle L James; Bin Shen; Cristina L Zavaleta; Carsten H Nielsen; Christophe Mesangeau; Pradeep K Vuppala; Carmel Chan; Bonnie A Avery; James A Fishback; Rae R Matsumoto; Sanjiv S Gambhir; Christopher R McCurdy; Frederick T Chin
Journal:  J Med Chem       Date:  2012-09-20       Impact factor: 7.446
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  1 in total

1.  Exploring 1-adamantanamine as an alternative amine moiety for metabolically labile azepane ring in newly synthesized benzo[d]thiazol-2(3H)one σ receptor ligands.

Authors:  Sebastiano Intagliata; Hebaalla Agha; Theresa A Kopajtic; Jonathan L Katz; Shyam H Kamble; Abhisheak Sharma; Bonnie A Avery; Christopher R McCurdy
Journal:  Med Chem Res       Date:  2020-07-08       Impact factor: 1.965
  1 in total

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