AI Article Synopsis
- The study focused on the binding affinities and functional activities of these compounds at serotonin (5-HT) and dopamine (D) receptors, with compounds 1 and 4 showing the best activity at the 5-HT receptor.
- The pharmacological testing in mouse models indicated that compounds 1 and 4 affect the serotonergic system, and compound 4 demonstrated antinociceptive effects likely linked to its anti-inflammatory properties.
Article Abstract
Four 2-(1H-indol-3-yl)ethylthiourea derivatives were prepared by condensation of 2-(1H-indol-3-yl)ethanamine with the corresponding aryl/alkylisothiocyanates in a medium-polarity solvent. Their structures were confirmed by spectral techniques, and the molecular structure of 3 was determined by X-ray crystal analysis. For all derivatives, the binding affinities at the 5-HT and 5-HT receptors, as well as their functional activities at the 5-HT and D receptors, were determined. The arylthioureas 1 and 4 were the most active at the 5-HT receptor, showing, at the same time, significant selectivity over the studied 5-HT and D receptor subtypes. The compounds were tested for their pharmacological activities within the central nervous system in relevant mouse models. The involvement of the serotonergic system in the activity of 1 and 4 was indicated. The antinociceptive action of 4 was linked to its anti-inflammatory activity.
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| http://dx.doi.org/10.1002/ardp.201900218 | DOI Listing |
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