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Chemical Compound Review:

TIOSPIRONE 8-[4-[4-(7-thia-8- azabicyclo[4.3.0]nona-1...

Synonyms: Tiospirona, tiaspirone, tiospyrone, Tiospironum, CHEMBL35057, ...

Roth, B.L. et al., Robertson, G.S. et al., Sumiyoshi, T. et al., Hyslop, D.K. et al., Arolfo, M.P. et al.

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High impact information on TIOSPIRONE

Higher ratios of potency in occupying 5-HT2 versus D2 receptors were found for clozapine, RMI-81512, and tiospirone compared to haloperiodol and pimozide [1].
Clozapine and several related atypical antipsychotic agents (rilapine, olanzepine, tiospirone, fluperlapine, clorotepine and zotepine) had high affinities for the newly discovered 5-HT6 receptor (Kis < 20 nM) [2].
The 5-HT7 receptor bound clozapine, rilapine, fluperlapine, clorotepine, zotepine and risperidone but not tiospirone and olanzepine, with affinities less than 15 nM [2].
Consistent with the hypothesis that the prefrontal cortex may be a target for some antipsychotic actions, FLI was elevated in this structure by clozapine, ICI 204,636, fluperlapine, RMI-81,582, remoxipride, molindone, melperone and tiospirone [3].

Associations of TIOSPIRONE with other chemical compounds

Effects of amperozide and tiospirone, atypical antipsychotic 5-HT2 drugs, on food-reinforced behavior in rats [4].

Analytical, diagnostic and therapeutic context of TIOSPIRONE

Plasma levels of tiospirone were also obtained by high-performance liquid chromatography assay at similar time points [5].

References

Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy. Sumiyoshi, T., Suzuki, K., Sakamoto, H., Yamaguchi, N., Mori, H., Shiba, K., Yokogawa, K. Neuropsychopharmacology (1995) [Pubmed]
Binding of typical and atypical antipsychotic agents to 5-hydroxytryptamine-6 and 5-hydroxytryptamine-7 receptors. Roth, B.L., Craigo, S.C., Choudhary, M.S., Uluer, A., Monsma, F.J., Shen, Y., Meltzer, H.Y., Sibley, D.R. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
Induction patterns of Fos-like immunoreactivity in the forebrain as predictors of atypical antipsychotic activity. Robertson, G.S., Matsumura, H., Fibiger, H.C. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
Effects of amperozide and tiospirone, atypical antipsychotic 5-HT2 drugs, on food-reinforced behavior in rats. Arolfo, M.P., McMillen, B.A. Physiol. Behav. (1999) [Pubmed]
Radioreceptor assay of dopamine binding activity in human serum after tiospirone administration. Hyslop, D.K., Westrick, M.L., Shukla, U.A., Taylor, D.P. Therapeutic drug monitoring. (1989) [Pubmed]

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