Benzothiazoles as probes for the 5HT1A receptor and the serotonin transporter (SERT): A search for new dual-acting agents as potential antidepressants
Public Deposited- Creator
- Zhu, Xue Y.
- Etukala, Jagan R.
- Eyunni, Suresh V.K.
- Setola, Vincent
- Roth, Bryan L.
- Ablordeppey, Seth Y.
- Abstract
- The synthesis and evaluation of several benzothiazole based compounds are described in an attempt to identify novel dual-acting 5HT1A receptor and SERT inhibitors as new antidepressants. Binding affinities at the 5HT1A 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 5HT1A 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 5HT2C receptor, which are desirable properties as selectivity for SERT (and not DAT or NET) is associated with an absence of cardiovascular side-effects.
- Date of publication
- 2012
- Keyword
- DOI
- Identifier
- PMID: 22520153
- PMCID: PMC3361616
- Publisher DOI: https://doi.org/10.1016/j.ejmech.2012.03.042
- Onescience id: 8f15d3e8bef7c9cd26414c7eb2863aee2d8e3717
- Resource type
- Article
- Rights statement
- In Copyright
- Journal title
- European Journal of Medicinal Chemistry
- Journal volume
- 53
- Page start
- 124
- Page end
- 132
- Language
- English
- ISSN
- 0223-5234
- 1768-3254
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