Tandospirone

Tandospirone (SM-3997; sediel ) is an anxiolytic and antidepressant [1].

Tandospirone has been reported to produce a significant increase in number of shocks at doses of 5 and 10mg/kg, i .p. or 20 and 40 mg/kg, p.o.. 10mg/kg, i.p. of Tandospirone has been revealed to produce a significant increase in the number of shocks following the repeated treatment for 5 or 10 days. In addition, has been noted to impair rota-rod performance at relatively high doses with ED50 values of 207 mg/kg, p.o. and 300mg/kg, p.o. in mice and rats, respectively. Besides, Tandospirone has been evaluated to enhance the duration of the hexobarbital-induced anesthesia with an ED50 value of 212mg/kg, p.o. [1].

References:
[1] Shimizu H1, Hirose A, Tatsuno T, Nakamura M, Katsube J. Pharmacological properties of SM-3997: a new anxioselective anxiolytic candidate. Jpn J Pharmacol. 1987 Dec; 45(4):493-500.

5-HT1A receptor agonists, xaliproden and tandospirone, inhibit the increase in the number of cutaneous mast cells involved in the exacerbation of mechanical allodynia in oxaliplatin-treated mice.[Pubmed:27562704]

J Pharmacol Sci. 2016 Aug;131(4):284-7.

Oxaliplatin causes peripheral neuropathy as a major dose-limiting side effect, and the control of this neuropathy is difficult. This study was designed to investigate whether prophylactic repetitive administration of 5-HT1A receptor agonists inhibits oxaliplatin-induced mechanical allodynia in mice. Repetitive administration of 5-HT1A receptor agonists (xaliproden and Tandospirone) inhibited mechanical allodynia induced by a single intraperitoneal injection of oxaliplatin. These agonists also inhibited oxaliplatin-induced mast cell migration, which is involved in the induction of mechanical allodynia. These results suggest that the prophylactic repetitive administration of 5-HT1A receptor agonists attenuates oxaliplatin-induced mechanical allodynia by inhibiting the cutaneous mast cell migration.

Rapid and highly sensitive analysis of benzodiazepines and tandospirone in human plasma by automated on-line column-switching UFLC-MS/MS.[Pubmed:28081789]

Leg Med (Tokyo). 2017 Jan;24:36-55.

A high-throughput method was developed for the detection of 31 benzodiazepine drugs and Tandospirone in human plasma by on-line column-switching ultra-fast liquid chromatography-tandem mass spectrometry. Plasma samples (100mul) spiked with the 32 drugs and oxazepam-d5 (internal standard) were diluted with 300mul of 13.3mM ammonium acetate/acetonitrile (33:67, v/v). After centrifugation and filtration, the clear supernatant was injected directly onto the extraction column (Oasis HLB cartridge column). The following procedure was fully automated. The analytes retained on the extraction column were eluted by backflushing of the extraction column and introduced into an analytical column (SUMIPAX ODS D-Swifter column, 30mmx3.0mm i.d.; particle size 2mum) by column switching. Quantification was performed by multiple reaction monitoring with positive-ion electrospray ionization. Distinct peaks appeared for each drug and the internal standard on each channel within 7min, including the extraction time. All drugs spiked into plasma showed recoveries of 83-95%. The regression equations for the 32 drugs showed excellent linearities in the range of 50-2000pg/ml of plasma and the limits of detection ranged from 20 to 50pg/ml. The lower and upper limits of quantitation were 50-100ng/ml and 2000pg/ml, respectively. Intra- and interday coefficients of variation for none of the drugs were greater than 13.6%. The accuracies of quantitation were 87-112%. The multiple reaction monitoring information-dependent acquisition of enhanced product ions method enabled the quantification and confirmation of diazepam, triazolam, and lorazepam obtained from actual plasma.

Photolytic and photocatalytic degradation of tandospirone: Determination of kinetics, identification of transformation products and in silico estimation of toxicity.[Pubmed:28292608]

Sci Total Environ. 2017 Jul 15;590-591:775-798.

The photolytic and photocatalytic transformation of Tandospirone with the use of TiO2 and H2O2 was investigated. A micro-scale method for simultaneous irradiation with simulated full solar spectrum of multiple samples in photostability chamber was proposed. RP-UHPLC-DAD coupled with ESI-Q-TOF mass spectrometer was used for the quantitative and qualitative analysis of the processes. The developed method was fully validated and the kinetic parameters of Tandospirone photodegradation were compared. The structures of eighteen photoproducts as well as phototransformation pathways were proposed. Based on the elucidated structures, computational toxicity assessment with the use of various software was performed and most of the photoproducts were found as less or similarly toxic to the parent compound. Nevertheless, several products, including one of the drug main metabolites, were significantly more toxic than the parent drug. The multivariate chemometric method (principal component analysis) was used to compare the toxicity of phototransformation products as well as the toxicity of the assessment methods.

Randomized Trial to Evaluate Tandospirone in Geographic Atrophy Secondary to Age-Related Macular Degeneration: The GATE Study.[Pubmed:26310670]

Am J Ophthalmol. 2015 Dec;160(6):1226-34.

PURPOSE: To determine the safety and efficacy of AL-8309B (Tandospirone) in the management of patients with geographic atrophy (GA) secondary to age-related macular degeneration (AMD) and obtain standardized data on GA lesion growth progression. DESIGN: Prospective, controlled, double-masked, randomized, multicenter phase 3 clinical trial. METHODS: setting: Forty-eight clinical sites. PATIENTS: Patients with GA associated with AMD were enrolled. All patients were followed for a minimum of 30 months, and up to 36 months. intervention procedures: Patients were randomized (1:1:1) to receive AL-8309B ophthalmic solution 1.0%, 1.75%, or vehicle, administered as a twice-daily topical ocular drop. MAIN OUTCOME MEASURES: The primary efficacy endpoint was mean annualized lesion enlargement from baseline as assessed with fundus autofluorescence (FAF) imaging. RESULTS: A total of 768 eyes of 768 patients were enrolled and treated with AL-8309B 1.0% (n = 250), AL-8309B 1.75% (n = 258), or vehicle (n = 260). An increase in mean lesion size was observed in both the AL-8309B and vehicle treatment groups, and growth rates were similar in all treatment groups. Annualized lesion growth rates were 1.73, 1.76, and 1.71 mm(2) for AL-8309B 1.0%, AL-8309B 1.75%, and vehicle, respectively. CONCLUSIONS: AL-8309B 1.0% and 1.75% did not affect lesion growth in eyes with GA secondary to AMD. There were no clinically relevant safety issues identified for AL-8309B. The large natural history dataset from this study is a valuable repository for future comparisons.

Tandospirone(SM-3997) is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).

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