Tiospirone (BMY-13,859), also sometimes called tiaspirone or tiosperone, is an
atypical antipsychotic
The atypical antipsychotics (AAP), also known as second generation antipsychotics (SGAs) and serotonin–dopamine antagonists (SDAs), are a group of antipsychotic drugs (antipsychotic drugs in general are also known as major tranquilizers and ne ...
of the
azapirone
Azapirones are a class of drugs used as anxiolytics, antidepressants, and antipsychotics. They are commonly used as add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs).
Medical uses
Azapirones have shown ...
class.
It was investigated as a treatment for
schizophrenia
Schizophrenia is a mental disorder characterized by continuous or relapsing episodes of psychosis. Major symptoms include hallucinations (typically hearing voices), delusions, and disorganized thinking. Other symptoms include social wit ...
in the late 1980s and was found to have an effectiveness equivalent to those of
typical antipsychotic
Typical antipsychotics (also known as major tranquilizers, and first generation antipsychotics) are a class of antipsychotic drugs first developed in the 1950s and used to treat psychosis (in particular, schizophrenia). Typical antipsychotics ma ...
s in
clinical trial
Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...
s but without causing
extrapyramidal side effect
In medicine, a side effect is an effect, whether therapeutic or adverse, that is secondary to the one intended; although the term is predominantly employed to describe adverse effects, it can also apply to beneficial, but unintended, consequence ...
s.
However, development was halted and it was not marketed.
Perospirone
Perospirone (Lullan) is an atypical antipsychotic of the azapirone family. It was introduced in Japan by Dainippon Sumitomo Pharma in 2001 for the treatment of schizophrenia and acute cases of bipolar mania.
Medical uses
Its primary uses are i ...
, 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
In pharmacology, partial agonists are drugs that bind to and activate a given receptor, but have only partial efficacy at the receptor relative to a full agonist. They may also be considered ligands which display both agonistic and antagonis ...
,
5-HT2A,
5-HT2C, and
5-HT7 receptor inverse agonist, and
D2,
D4, and
α1-adrenergic receptor antagonist.
Binding profile
See also
*
Azapirone
Azapirones are a class of drugs used as anxiolytics, antidepressants, and antipsychotics. They are commonly used as add-ons to other antidepressants, such as selective serotonin reuptake inhibitors (SSRIs).
Medical uses
Azapirones have shown ...
References
{{Navboxes
, title =
Pharmacodynamics
Pharmacodynamics (PD) is the study of the biochemical and physiologic effects of drugs (especially pharmaceutical drugs). The effects can include those manifested within animals (including humans), microorganisms, or combinations of organisms ...
, titlestyle = background:#ccccff
, list1 =
{{Adrenergic receptor modulators
{{Dopamine receptor modulators
{{Serotonin receptor modulators
{{Sigma receptor modulators
Abandoned drugs
Antipsychotics
Azapirones
Benzothiazoles
Piperazines