AI Article Synopsis
- Researchers developed new flexible arylpiperazine compounds (1a-3a) that target 5-HT1A and 5-HT2A receptors with low affinity for D2 receptors and exhibit either agonistic or partial agonistic activity specifically on 5-HT1A receptors.
- They then created more rigid versions of these compounds (1b-3b) that showed selective binding to 5-HT1A receptors, mostly acting as agonists or partial agonists.
- These findings suggest potential applications for these compounds in treating conditions related to serotonin dysregulation.
Article Abstract
Novel, flexible arylpiperazine gepirone analogs (1a-3a) with a mixed 5-HT1A/5-HT2A receptor profile, low D2 receptor affinity, and agonistic (2a) or partial agonistic (1a, 3a) activity toward 5-HT1A receptor sites were synthesized. Their conformationally restricted counterparts (1b-3b) were selective 5-HT1A ligands (over 5-HT2A and D2 receptors), which turned out to be agonists (2b, 3b), or partial agonist (1b) of 5-HT1A receptors.
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| http://dx.doi.org/10.1016/j.bmc.2004.11.019 | DOI Listing |
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