Tandospirone citrate
(Synonyms: 坦度螺酮柠檬酸盐; SM-3997 citrate) 目录号 : GC37734
Tandospirone (SM-3997), a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM, has anxiolytic and antidepressant activities.
Cas No.:112457-95-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tandospirone (SM-3997), a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM, has anxiolytic and antidepressant activities.
[1] Hamik A, et al. Biol Psychiatry. 1990 Jul 15;28(2):99-109. [2] Huang X, et al. Oncotarget. 2017 Oct 27;8(60):102705-102720.
| Cas No. | 112457-95-1 | SDF | |
| 别名 | 坦度螺酮柠檬酸盐; SM-3997 citrate | ||
| Canonical SMILES | O=C1N(CCCCN2CCN(C3=NC=CC=N3)CC2)C([C@@]4([H])[C@](C5)([H])CC[C@]5([H])[C@@]14[H])=O.O=C(CC(C(O)=O)(O)CC(O)=O)O | ||
| 分子式 | C27H37N5O9 | 分子量 | 575.61 |
| 溶解度 | Water: 10.4 mg/mL (18.07 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7373 mL | 8.6864 mL | 17.3729 mL |
| 5 mM | 0.3475 mL | 1.7373 mL | 3.4746 mL |
| 10 mM | 0.1737 mL | 0.8686 mL | 1.7373 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Clinical Analysis on the Effects of Tandospirone citrate Assisted by Drawing Therapy on Medication Compliance and Sleep Quality in Patients with Anxiety Disorders
Emerg Med Int 2022 Aug 30;2022:9295627.PMID:36081955DOI:10.1155/2022/9295627.
Objective: To explore the clinical effects of Tandospirone citrate assisted by drawing therapy (DT) on medication compliance and sleep quality in patients with anxiety disorders. Methods: A total of 128 patients with anxiety disorders treated in the hospital were enrolled between January 2020 and January 2022. According to the random number table method, they were divided into the observation group (n = 64) and the control group (n = 64). The control group was treated with Tandospirone citrate, while the observation group was additionally treated with DT. The clinical curative effect and medication compliance after treatment, scores of Hamilton Anxiety Scale (HAMA), Pittsburgh Sleep Quality Index (PSQI), and the World Health Organization's Quality of Life Questionnaire-Brief Version (WHOQOL-BREF) before and after treatment were compared between the two groups. The occurrence of adverse reactions during treatment was recorded. Results: After treatment, the total response rate in the observation group was higher than that in the control group (96.88% vs 86.94%) (P < 0.05). After treatment, scores of HAMA and PSQI in both groups were decreased, which were lower in the observation group than in the control group (P < 0.05). After treatment, medication compliance in the observation group was higher than that in the control group (P < 0.05). After treatment, scores of environmental factors, social relations, physiological function, and psychological status in both groups were increased, which were higher in the observation group than in the control group (P < 0.05). During treatment, there was no significant difference in the incidence of adverse reactions between the two groups (P > 0.05). Conclusion: DT-assisted Tandospirone citrate can effectively improve the clinical symptoms of patients with anxiety disorders, improve medication compliance, sleep quality, and quality of life, and have a certain degree of safety.
Augmentation therapy with Tandospirone citrate in vascular depression patients with mild cognitive impairment: A prospective randomized clinical trial
J Psychiatr Res 2023 Mar;159:274-282.PMID:36774768DOI:10.1016/j.jpsychires.2022.12.023.
Cognitive impairment is a prominent clinical manifestation of vascular depression (VaDep). The current study aimed to assess the efficacy of Tandospirone citrate in VaDep cases with mild cognitive impairment (VaDep-MCI) as well as the role of plasma monoamine neurotransmitters during the treatment. In this single-blind, randomized controlled study, 116 participants were randomly assigned to the tandospirone (tandospirone citrate-escitalopram) and control (escitalopram) groups. The primary endpoints were changes in cognitive test scores from baseline to Week 8, including the Rey Auditory Verbal Learning Test (RAVLT), Semantic Verbal Fluency (SVF) test, Trail Making Test (TMT), Digital Span Test (DST) and Clock Drawing Test (CDT) scores. Generalized estimating equation models were used to examine repeated measures. The results showed that compared with the changes in the control group from baseline to Week 8, the tandospirone group showed more significant changes in SVF score at Weeks 4 (p < 0.05) and 8 (p < 0.001), and TMT (B-A) score at Week 8 (p < 0.05). RAVLT, DST and DCT scores were relatively stable in both groups during the study period. Moreover, mediation analysis showed that these results were not mediated by the alleviation of depression symptoms. Partial Spearman correlation analysis showed that only plasma 5-hydroxytryptamine (5-HT) was positively correlated with Hamilton Depression Rating Scale score after Bonferroni correction (r = 0.347, p < 0.001). Augmentation therapy with Tandospirone citrate improved the executive and language functions of VaDep-MCI patients. Additionally, plasma 5-HT levels may serve as a potential biomarker of VaDep severity. These findings may provide clinical insights into the treatment of vascular depression.
Efficacy of the 5-HT1A agonist Tandospirone citrate in improving symptoms of patients with functional dyspepsia: a randomized controlled trial
Am J Gastroenterol 2009 Nov;104(11):2779-87.PMID:19638966DOI:10.1038/ajg.2009.427.
Objectives: Functional dyspepsia (FD) is a common condition in the general population; however, its treatment remains a challenge. The aim of this study was to examine the efficacy of Tandospirone citrate, a new partial agonist of the 5-hydroxytryptamine 1A (5-HT1A) receptor, in improving the symptoms of patients with FD. Methods: In this double-blind, placebo-controlled, multicenter study, FD patients were randomized to treatment with 10 mg t.i.d. Tandospirone citrate or to placebo for 4 weeks. The primary end point was change in abdominal symptom scores. The difference in the proportion of responders (a total abdominal symptom score of 0 or 1) was also assessed. The quality-of-life questionnaire, the SF-8, and a psychological test questionnaire, the State-Trait Anxiety Inventory (STAI), were completed at baseline and at weekly intervals. Results: Data were available for 144 patients: 73 for tandospirone and 71 for placebo. Improvements in total abdominal scores were significantly larger with tandospirone than placebo at weeks 1, 2, and 4. Significantly greater improvements in the tandospirone group were observed in upper abdominal pain (P=0.02) and discomfort (P=0.002) at week 4. The proportion of responders was significantly greater in the active treatment arm at weeks 3 (P=0.017) and 4 (P=0.0016). Significant improvements in STAI (P<0.0001) were reported in both arms, as well as in the majority of questions in the SF-8 (P=0.04). No serious adverse events were reported, with similar rates in both study arms. Conclusions: Despite a considerable placebo effect, the benefits of tandospirone were shown in terms of improvement in abdominal symptom scores.
Tandospirone and alprazolam: comparison of behavioral effects and abuse liability in humans
J Pharmacol Exp Ther 1994 Nov;271(2):683-94.PMID:7965783doi
Tandospirone is a novel nonbenzodiazepine anxiolytic/antidepressant that acts primarily at the serotonin-1A receptor. In the present study, the behavioral effects and abuse liability of tandospirone were characterized relative to those of the benzodiazepine, alprazolam. In an outpatient setting, the acute effects of placebo, Tandospirone citrate (40, 80 and 160 mg) and alprazolam (0.5, 1.0 and 2.0 mg) were assessed with a double-blind, cross-over design in 14 male volunteers with histories of sedative drug abuse. Drug effects were assessed on behavioral performance tasks; observer ratings of drug effect; and subject ratings of strength of drug effect, mood and drug liking. Both alprazolam and tandospirone produced comparable dose-related increases in subject- and observer-rated strength of drug effect. The peak drug effect occurred approximately 2 hr after drug administration; the time to peak did not differ between the two drugs. Alprazolam produced greater impairments on psychomotor performance than did tandospirone. Alprazolam produced dose-related increases in subject-rated drug liking; tandospirone, in contrast, produced dose-related increases in subject-rated drug disliking. The highest dose of alprazolam was predominantly classified by subjects as being a benzodiazepine or a barbiturate (71%) in contrast to the highest dose of tandospirone (29%). Across subjects, tandospirone plasma concentrations after a single dose of 160 mg were significantly correlated with several subjective and behavioral measures. The present study demonstrates that tandospirone and alprazolam can be clearly differentiated on the basis of subjective effects and performance measures. The overall profile indicates that tandospirone has a significantly lower abuse liability than does alprazolam.
[Tandospirone citrate, a selective 5-HT1A agonist, alleviates L-DOPA-induced dyskinesia in patients with Parkinson's disease]
No To Shinkei 2002 Feb;54(2):133-7.PMID:11889759doi
A rapid and excessive increase in extracellular dopamine(DA) after L-DOPA administration is considered one of the major causes for L-DOPA-induced peak-dose dyskinesia. Therefore, inhibition of excessive rise in L-DOPA-derived DA is likely to be an ideal treatment for L-DOPA-induced dyskinesia. Based on our previous experimental studies that 8-OH-DPAT, a potent 5-HT1A agonist, attenuates an increase in L-DOPA-induced extracellular DA in the striatum of the rat model of Parkinson's disease, we hypothesized that L-DOPA-induced dyskinesia in patients with Parkinson's disease is alleviated by a 5-HT1A agonist. In the present study, we administered Tandospirone citrate, a selective 5-HT1A agonist, to patients with Parkinson's disease suffering from L-DOPA-induced dyskinesia. Tandospirone(15-60 mg/day) was administered to 10 patients with L-DOPA-induced peak-dose dyskinesia. Twelve weeks after tandospirone treatment, duration of dyskinesia, subjective and objective severity of dyskinesia, and parkinsonian features were evaluated. Severity of dyskinesia was decreased in 5 patients; among these, 3 patients experienced slight worsening of parkinsonian features. Four patients showed no change in dyskinesia; among these, 2 patients showed worsening of parkinsonian features. One patient had slight worsening of dyskinesia without any change in parkinsonian features. The present study demonstrated that tandospirone is effective in alleviating L-DOPA-induced dyskinesia in 50% of the patients. However, at the same time 50% patients showed slight worsening of parkinsonian features. Both the anti-dyskinetic effect and the worsening of parkinsonian features are thought to be induced by tandospirone's potent 5-HT1A agonistic activity. Diverse effect of tandospirone may be caused by its partial agonist activity on 5-HT1A receptors, or may indicate that other causes for the expression of dyskinesia exist apart from excessive rise in brain DA levels. Administration of a 5-HT1A agonist is a choice for patients with dyskinesia if the care is taken so as not to induce worsening of parkinsonian features. Further studies such as double-blind trials are needed to confirm the usefulness of a 5-HT1A agonist for L-DOPA-induced dyskinesia.