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Tandospirone
Systematic (IUPAC) name
(1R,2R,6S,7S)-4-{4-[4-(pyrimidin-2-yl)piperazin-1-yl]butyl}-4-azatricyclo[5.2.1.0 2,6]decane-3,5-dione
Identifiers
CAS number 112457-95-1
ATC code none
PubChem 91273
Chemical data
Formula C 21H29N5O2  
Mol. mass 383.487 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status Uncontrolled
Routes Oral

Tandospirone (Sediel) is a psychoactive drug and pharmaceutical medication of the piperazine and azapirone chemical classes. It is widely used as an anxiolytic and antidepressant agent in China and Japan, where it is marketed by Dainippon Sumitomo Pharma.

Contents

Pharmacology

Tandospirone acts as a potent and selective 5-HT1A receptor partial agonist, with a Ki affinity value of 27 ± 5 nM[1] and approximately 84-87% intrinsic activity.[2] [3] It has weak but 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 (SERT), and benzodiazepine (BDZ) allosteric site of the GABAA receptor (all of which are > 100,000).[1] 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.[4][5]

Pharmacokinetics

Tandpsirone citrate 5 mg capsules.

Tandospirone is typically used at a dose of 30 mg/daily[6] taken in divided doses of 10 mg three times per day due to its short half-life. Though originally considered a relatively weak anxiolytic agent,[6] a clinical study found that doubling the dose to 60 mg/daily resulted in a "remarkable anxiolytic effect with an early onset of action, and without significant adverse effects", as well as "excellent anxiolytic efficacy that is comparable to that of the benzodiazepines".[6] Even greater of doses may be progressively more useful, and in fact, human studies have gone as high as 160 mg delivered in a single administration without any significant adverse reactions mentioned.[7]

See also

References

  1. ^ a b Hamik (1990). "Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites". Biological psychiatry 28 (2): 99–109. doi:10.1016/0006-3223(90)90627-E. PMID 1974152.  
  2. ^ Tanaka (1995). "Effects of tandospirone on second messenger systems and neurotransmitter release in the rat brain". General pharmacology 26 (8): 1765–72. doi:10.1016/0306-3623(95)00077-1. PMID 8745167.  
  3. ^ Yabuuchi, Kazuki (2004). "Effects of tandospirone, a novel anxiolytic agent, on human 5-HT1A receptors expressed in Chinese hamster ovary cells (CHO cells)". Biogenic Amines 18: 319. doi:10.1163/1569391041501933.  
  4. ^ Blier (1991). "Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine--II. Effects of acute administration of 1-PP and long-term administration of tandospirone on noradrenergic neurotransmission". Neuropharmacology 30 (7): 691–701. doi:10.1016/0028-3908(91)90176-C. PMID 1681447.  
  5. ^ Miller (1992). "Kinetics, brain uptake, and receptor binding of tandospirone and its metabolite 1-(2-pyrimidinyl)-piperazine". Journal of clinical psychopharmacology 12 (5): 341–5. PMID 1362206.  
  6. ^ a b c Nishitsuji (2004). "Tandospirone in the treatment of generalised anxiety disorder and mixed anxiety-depression : results of a comparatively high dosage trial". Clinical drug investigation 24 (2): 121–6. PMID 17516698.  
  7. ^ Evans (1994). "Tandospirone and alprazolam: comparison of behavioral effects and abuse liability in humans". The Journal of pharmacology and experimental therapeutics 271 (2): 683–94. PMID 7965783.  







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