Tiospirone

Tiospirone

Clinical data
ATC code	none
Legal status
Legal status	Development terminated
Pharmacokinetic data
Metabolism	Hepatic
Elimination half-life	1.4 hours
Excretion	Urine
Identifiers
IUPAC name 8-[4-[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]butyl]-8-azaspiro[4.5]decane-7,9-dione
CAS Number	87691-91-6
PubChem CID	55752
IUPHAR/BPS	101
ChemSpider	50348
UNII	35C6UMO5SR
ChEMBL	ChEMBL35057
CompTox Dashboard (EPA)	DTXSID90236558
Chemical and physical data
Formula	C24H32N4O2S
Molar mass	440.61 g·mol−1

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-HT_1A receptor partial agonist, 5-HT_2A, 5-HT_2C, and 5-HT₇ receptor inverse agonist, and D₂, D₄, and α₁-adrenergic receptor antagonist.

Binding profile

See also

• Azapirone