Tiospirone (BMY-13,859), also sometimes called tiaspirone or tiosperone, is an atypical antipsychotic of the azapirone class. It was investigated as a treatment for schizophrenia in the late 1980s and was found to have an effectiveness equivalent to those of typical antipsychotics in clinical trials but without causing extrapyramidal side effects. However, development was halted and it was not marketed. Perospirone, another azapirone derivative with antipsychotic properties, was synthesized and assayed several years after tiospirone. It was found to be both more potent and more selective in comparison and was commercialized instead.
Pharmacology
Pharmacodynamics Tiospirone acts as a 5-HT1A receptor partial agonist, 5-HT2A, 5-HT2C, and 5-HT7 receptor inverse agonist, and D2, D4, and α1-adrenergic receptor antagonist.
Binding profile Receptor Ki (nM) 5-HT2A 0.06 5-HT2C 9.73 5-HT6 950 5-HT7 0.64 M1 630 M2 180 M3 1290 M4 480 M5 3900 D2 0.5 D4 13.6
See also Azapirone List of investigational antipsychotics
References