ArticleEuropean journal of medicinal chemistry2012
Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): a search for new dual-acting agents as potential antidepressants.
Article in European journal of medicinal chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 29 citations in OpenAlex.
- Highly Potent and Selective Dopamine DJournal of medicinal chemistry · 2022Article
- Vilazodone for Major Depression in Adults: Pharmacological Profile and an Updated Review for Clinical Practice.Neuropsychiatric disease and treatment · 2022Review
- Synthesis and Antidepressant Activity Profile of Some Novel Benzothiazole Derivatives.Molecules (Basel, Switzerland) · 2017Article
- Synthesis and evaluation of the structural elements in alkylated tetrahydroisoquinolines for binding to CNS receptors.Bioorganic & medicinal chemistry · 2016Article
- Development of CNS multi-receptor ligands: Modification of known D2 pharmacophores.Bioorganic & medicinal chemistry · 2016Article
- Identification of a new selective dopamine D4 receptor ligand.Bioorganic & medicinal chemistry · 2014Article
- 2-(Adamantan-1-yl)-N-(6-meth-oxy-1,3-benzo-thia-zol-2-yl)acetamide.Acta crystallographica. Section E, Structure reports online · 2013Article
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
Abstract
The synthesis and evaluation of several benzothiazole-based compounds are described in an attempt to identify novel dual-acting 5HT(1A) receptor and SERT inhibitors as new antidepressants. Binding affinities at the 5HT(1A) receptor and the serotonin transporter do not appear to be congruent and other areas of the binding sites would need to be explored in order to improve binding simultaneously at both sites. Compounds 20 and 23 show moderate binding affinity at the 5HT(1A) receptor and the SERT site and thus, have the potential to be further explored as dual-acting agents. In addition, compound 20 binds with low affinity to the dopamine transporter (DAT), the norepinephrine transporter (NET) and 5HT(2C) receptor, which are desirable properties as selectivity for SERT (and not DAT or NET) is associated with an absence of cardiovascular side effects.
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Registered trials
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