Tiospirone (BMY-13,859), also sometimes called tiaspirone or tiosperone, is an atypical antipsychotic of the azapirone class.[1] 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.[2][3][4][5] However, development was halted and it was not marketed. Perospirone, another azapirone derivative with antipsychotic properties, was synthesized and assayed several years after tiospirone.[6] It was found to be both more potent and more selective in comparison and was commercialized instead.[6]
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Metabolism | Hepatic |
Elimination half-life | 1.4 hours |
Excretion | Urine |
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Formula | C24H32N4O2S |
Molar mass | 440.61 g·mol−1 |
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.[7][8][9][10][11][12]
Binding profile[13]
Receptor | Ki (nM) |
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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 |