|AHFS/Drugs.com||International Drug Names|
|Elimination half-life||2–3 hours (3–5 hours for metabolite 1-PP)|
|Excretion||Urine (70%; 0.1% as unchanged drug)|
|Chemical and physical data|
|Molar mass||383.487 g/mol|
|3D model (JSmol)|
Tandospirone (brand name Sediel) is an anxiolytic and antidepressant drug used in China and Japan, where it is marketed by Dainippon Sumitomo Pharma. It is a member of the azapirone class of drugs and is closely related to other azapirones like buspirone and gepirone.
Anxiety and depression
Tandospirone is most commonly used as a treatment for anxiety and depressive disorders, such as generalised anxiety disorder and dysthymia respectively. For both indications it usually takes a couple of weeks for therapeutic effects to be start being seen, although at higher doses more rapid anxiolytic responses have been seen. It has also been used successfully as a treatment for bruxism.
- Gastrointestinal disorders
- Dry mouth
It is not believed to be addictive but it is known to produce mild withdrawal effects (e.g. anorexia) after abrupt discontinuation.
Tandospirone acts as a potent and selective 5-HT1A receptor partial agonist, with a Ki affinity value of 27 ± 5 nM and approximately 55 to 85% intrinsic activity. It has weak and clinically negligible affinity for the 5-HT2A (1,300 ± 200), 5-HT2C (2,600 ± 60), α1-adrenergic (1,600 ± 80), α2-adrenergic (1,900 ± 400), D1 (41,000 ± 10,000), and D2 (1,700 ± 300) receptors, and is essentially inactive at the 5-HT1B, 5-HT1D, β-adrenergic, and muscarinic acetylcholine receptors, serotonin transporter, and benzodiazepine allosteric site of the GABAA receptor (all of which are > 100,000). There is evidence of tandospirone having low but significant antagonistic activity at the α2-adrenergic receptor through its active metabolite 1-(2-pyrimidinyl)piperazine (1-PP), however.
In February of 2018, a study was conducted by researchers at the Queensland University of Technology and published in the journal Scientific Reports. Researchers found that tandospirone helped reverse brain deficits caused by chronic alcohol exposure in mice. The study was the first of its kind and brought interest in the drug for possible treatment of alcohol withdrawal symptoms.
Society and culture
Tandospirone has also been known as metanopirone.
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- "5-HT1A receptor-dependent modulation of emotional and neurogenic deficits elicited by prolonged consumption of alcohol". Scientific Reports. 2018. doi:10.1038/s41598-018-20504-z.
- "New drug could reverses binge drinking effects on brain, help alcoholics: scientists". ABC.net.au. Retrieved 8 February 2018.