Summary
In order to clarify the mechanism of action of the putative nonbenzodiazepine anxiolytic TVX Q 7821 [2-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-1,2-benzisothiazol-3-(2H)one-1,1-dioxidehydrochloride], binding studies with the radio labelled compound were performed.3H-TVX Q 7821 bound apidly, reversibly and in a saturable manner with high affinity to calf brain structures with preference for the hippocampus (K D 1.62 nmol/l;B max 320 fmol/mg protein).3H-TVX Q 7821 binding was displaced only by 5-hydroxytryptamine and its agonists and antagonists including spiperone, but was not displaced by a variety of other neurotransmitters and drugs. The 5-HT2 receptor antagonist ketanserin was a weak displacer. The hippocampal binding sites for3H-TVX Q 7821 were pharmacologically very similar to the 5-HT1-binding sites in this region. TVX Q 7821 is likely to be an important tool in research on functional aspects of 5-HT1 binding sites.
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References
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Dompert, W.U., Glaser, T. & Traber, J. 3H-TVX Q 7821: identification of 5-HT1 binding sites as target for a novel putative anxiolytic. Naunyn-Schmiedeberg's Arch. Pharmacol. 328, 467–470 (1985). https://doi.org/10.1007/BF00692918
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DOI: https://doi.org/10.1007/BF00692918