Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites

@article{Hamik1990AnalysisOT,
  title={Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites},
  author={Anne Hamik and Donna Oksenberg and Christine T. Fischette and Stephen J. Peroutka},
  journal={Biological Psychiatry},
  year={1990},
  volume={28},
  pages={99-109}
}
The interactions of tandospirone (formerly called SM-3997) with 5-HT and other neurotransmitter receptor binding sites were determined in brain homogenates. Tandospirone is most potent at the 5-HT1A receptor, displaying a Ki value of 27 +/- 5 nM. The agent is approximately two to three orders of magnitude less potent at 5-HT2, 5-HT1C, alpha 1-adrenergic, alpha 2-adrenergic, and dopamine D1 and D2 receptors (Ki values ranging from 1300 to 41000 nM). Tandospirone is essentially inactive at 5-HT1B… Expand
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It is concluded that 1-PP acts as an antagonist at somatodendritic and terminal alpha 2-adrenergic autoreceptors, as well as at postsynaptic alpha 2 -adrenoceptor agonists, in the central nervous system of the rat. Expand
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Results indicate that tandospirone potentiates the fluoxetine-induced increase in dopamine release via 5-HT(1A) receptors in the rat medial frontal cortex, and suggest that t andospir one may have therapeutic potential for the treatment of depression. Expand
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It is concluded that desensitization of somatodendritic 5-HT autoreceptors permits5-HT neurones to regain their physiological rate of firing during long-term treatment with tandospirone and, consequently, to release a normal amount of 5- HT into the synaptic cleft. Expand
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Tandospirone could be a therapeutic candidate for impulsivity-related disorders and may be due to the antagonistic action of the 5-HT1A receptor. Expand
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The agonist properties of trazodone and its active metabolite, m-chlorophenylpiperazine (m-CPP), at 5-HT1A receptors are elucidated by means of the guanosine-5′-O-(3-[ 35S]thio)-triphosphate ([35S]GTPγS) binding assay. Expand
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The dose-response curves from buspirone and tandospirone demonstrated enough dissimilarity to the dose- response curves from gepirone and ipsapirone to suggest differences in their rates of absorption, and/or differences in the production of active and inactive metabolites. Expand
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The results are the first evidence that systemic 5-HT1A receptor agonist administration produces a rapid increase in p-ERK levels in vivo, providing further insight into the signaling mechanisms of the 5- HT1A receptors. Expand
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