Zolazepam
(Synonyms: 唑拉西泮,Flupyrazapon) 目录号 : GC48273An Analytical Reference Standard
Cas No.:31352-82-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Zolazepam is an analytical reference standard categorized as a pyrazolodiazepinone.1 Zolazepam has anxiolytic and anticonvulsant properties. Formulations containing zolazepam in combination with tiletamine have been used as canine and feline anesthetics. This product is intended for research and forensic applications.
1.DeWald, H.A., Lobbestael, S., and Butler, D.E.Pyrazolodiazepines: 4-Aryl-1,3-dialkyl-6,8-dihydropyrazolo[3,4-e] [1,4]diazepin-7(1H)-ones as antianxiety and anticonvulsant agentsJ. Med. Chem.20(12)1562-1569(1977)
| Cas No. | 31352-82-6 | SDF | |
| 别名 | 唑拉西泮,Flupyrazapon | ||
| 化学名 | 4-(2-fluorophenyl)-6,8-dihydro-1,3,8-trimethyl-pyrazolo[3,4-e][1,4]diazepin-7(1H)-one | ||
| Canonical SMILES | O=C1CN=C(C2=C(F)C=CC=C2)C3=C(N(C)N=C3C)N1C | ||
| 分子式 | C15H15FN4O | 分子量 | 286.3 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 1 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml | 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 | 3.4928 mL | 17.4642 mL | 34.9284 mL |
| 5 mM | 0.6986 mL | 3.4928 mL | 6.9857 mL |
| 10 mM | 0.3493 mL | 1.7464 mL | 3.4928 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。
Dissociative anaesthesia in dogs and cats with use of tiletamine and Zolazepam combination. What we already know about it
Pol J Vet Sci 2021 Sep;24(3):451-459.PMID:34730303DOI:10.24425/pjvs.2021.138738.
This article is an attempt to gather available literature regarding the use of tiletamine and Zolazepam combination in anaesthesia in dogs and cats. Although tiletamine and Zolazepam mixture has been known in veterinary practice for a long time, the increased interest in these drugs has been observed only recently. Tiletamine, similarly to ketamine, is a drug which belongs to the phencyclidine group. Ketamine has considerable popularity in veterinary practice what suggests that other dissociative anaesthetic drugs, such as tiletamine, could also prove effective in cats' and dogs' anaesthetic care. Zolazepam is a widely used benzodiazepine known for its muscle relaxant and anticonvulsant properties. While conducting an electronic search for articles regarding the use of tiletamine-zolazepam combination in dogs and cats, it has been discovered that the literature on the subject (tiletamine-zolazepam combination in dogs and cats) is quite scarce. Very few articles were published after 2010. Databases used were: Google Scholar, Scopus, PubMed. Most of the adverse effects, including those affecting the cardiovascular, nervous, and respiratory systems, were strictly dose-dependent. Tiletamine-zolazepam combination can be safely used as a premedication agent, induction for inhalation anaesthesia, or an independent anaesthetic for short procedures. Contraindications using tiletamine-zolazepam mixture include central nervous system (CNS) diseases such as epilepsy and seizures, head trauma, penetrative eye trauma, cardiovascular abnormalities (hypertrophy cardiomyopathy in cats, arrythmias or conditions where increase of heart rate is inadvisable), hyperthyroidism, pancreatic deficiencies or kidney failure.
Determination of the effective dosage of tiletamine-zolazepam-ketamine-xylazine, with or without methadone, in dogs
Vet Anaesth Analg 2022 May;49(3):304-307.PMID:35337741DOI:10.1016/j.vaa.2022.02.005.
Objective: To determine the effective dosage of the combination tiletamine-zolazepam-ketamine-xylazine (TKX), with or without methadone, in dogs. Study design: Prospective, randomized, experimental study. Animals: A total of 29 dogs. Methods: Dogs were randomly administered TKX (group TKX, n = 13) or combined with 0.3 mg kg-1 of methadone (group TKXM, n = 16) intramuscularly. The TKX solution contained tiletamine (50 mg mL-1), Zolazepam (50 mg mL-1), ketamine (80 mg mL-1) and xylazine (20 mg mL-1). The effective dosages for immobility in 50% and 95% of the population (ED50 and ED95) were estimated using the up-and-down method. Approximately 20 minutes after drug administration, a skin incision was performed and the response was judged as positive or negative if the dogs moved or did not move, respectively. The TKX volume for the subsequent dog in the same group was increased or decreased by 0.005 mL kg-1 if the response of the previous dog was positive or negative, respectively. Heart and respiratory rates, and sedation/anesthesia scores (range 0-21) were recorded before and 15 minutes after drug administration. Results: Estimated ED50 and ED95 (95% confidence intervals) were: TKX, 0.025 (0.020-0.029) and 0.026 (0.010-0.042) mL kg-1; TKXM, 0.022 (0.018-0.025) and 0.033 (0.017-0.049) mL kg-1. Median (interquartile range) scores for sedation/anesthesia were 17 (16-18) and 17 (15-20), and times until lateral recumbency were 5 (4-6) and 6 (4-10) minutes in TKX and TKXM, respectively (p > 0.05). In both groups heart and respiratory rates decreased, but values remained acceptable for anesthetized dogs. Conclusions and clinical relevance: The results provide a guide for volumes of TKX and TKXM in dogs requiring restraint for minimally invasive procedures. Inclusion of methadone in the TKX combination did not influence ED50.
Tiletamine/Zolazepam and dexmedetomidine with tramadol provide effective general anesthesia in rats
Animal Model Exp Med 2021 Jan 2;4(1):40-46.PMID:33738435DOI:10.1002/ame2.12143.
Background: Tiletamine/Zolazepam is a dissociative anesthetic combination commonly used in small animals but information is limited in rats. The alpha-2 agonist, dexmedetomidine, has gained popularity in laboratory animal anesthesia. Tramadol is a weak opioid mu agonist. The aim of this study was to assess whether the tiletamine/Zolazepam/dexmedetomidine (ZD) combination effectively provides a surgical anesthesia plane comparable to tiletamine/Zolazepam/dexmedetomidine with tramadol (ZDT) in a minor procedure in rats. Methods: Rats were induced with ZD or ZDT. After the loss of paw withdrawal, a small incision was made on the rats' left thighs as a surgical stimulus. Rats were maintained under a surgical anesthesia plane by assessing the loss of the paw withdrawal reflex for 45 minutes, then atipamezole was administered. Monitored anesthesia parameters included: (a) physiological parameters - pulse rate (PR), respiratory rate (RR), tissue oxygen saturation (%SpO2), and body temperature; (b) duration parameters - induction time, onset and duration of surgical anesthesia plane, onset of recovery, and recovery time. Results: PR was significantly lower at 10 minutes in ZD and 5 minutes in ZDT groups. No difference was observed for RR, %SpO2, and body temperature. Likewise, there were no differences for duration parameters: induction time was less than 3 minutes; onset and duration of surgical anesthesia plane were approximately 5 and 45 minutes, respectively; onset of recovery (time to move) was 51 minutes; and recovery time was 52 minutes, respectively. Conclusion: These data suggest the ZD combination provides a surgical anesthesia plane comparable to ZDT in a rat incisional pain model.
The abuse liability of the NMDA receptor antagonist-benzodiazepine (tiletamine-zolazepam) combination: evidence from clinical case reports and preclinical studies
Drug Test Anal 2016 Aug;8(8):760-7.PMID:27341080DOI:10.1002/dta.1987.
The tiletamine-zolazepam (TZ) combination is an anaesthetic drug commonly used in veterinary medicine. It is an equal amount combination of tiletamine, a dissociative anaesthetic pharmacologically classified as an N-methyl-D-aspartate (NMDA) receptor antagonist, and Zolazepam, a benzodiazepine tranquilizer. There are concerns regarding the safety profile of this drug combination due to incidents of human misuse/abuse. In this paper, we discuss the abuse liability of this drug combination based on currently available scientific evidence. We performed an in-depth search of medical and scientific literature and found seven reported cases of human abuse of the TZ combination, two of which resulted in fatal outcomes. In most of these cases, drug administration was intentional indicating that the TZ combination was abused by humans. This finding is bolstered by the results of preclinical studies showing that the TZ combination produces rewarding effects in rats, although manifested only in pretreated subjects. Further studies revealed that the addictive effects of the TZ combination are influenced by pre-exposure to other psychoactive drugs. Pre-exposure to ketamine, diazepam, propofol, or ethanol facilitated the expression of the rewarding effects of the TZ combination. These findings support the hypothesis that the TZ combination was and can be used as a substitute or replacement drug. Altogether, the compiled evidence indicates that the TZ combination can potentially be abused by humans. Thus, careful use, dispensation, and monitoring of the TZ combination and associated substances are strongly advocated. Copyright © 2016 John Wiley & Sons, Ltd.
Xylazine and tiletamine-zolazepam anesthesia in horses
Am J Vet Res 1989 May;50(5):737-42.PMID:2729719doi
The cardiopulmonary and anesthetic effects of xylazine in combination with a 1:1 mixture of tiletamine and Zolazepam were determined in 6 horses. Each horse was given xylazine IV or IM, as well as tiletamine-zolazepam IV on 4 randomized occasions. Anesthetics were administered at the rate of 1.1 mg of xylazine/kg of body weight, IV, 1.1 mg of tiletamine-zolazepam/kg, IV (treatment 1); 1.1 mg of xylazine/kg, IV, 1.65 mg of tiletamine-zolazepam/kg, IV (treatment 2); 1.1 mg of xylazine/kg, IV, 2.2 mg of tiletamine-zolazepam/kg, IV (treatment 3); and 2.2 mg of xylazine/kg, IM, 1.65 mg of tiletamine-zolazepam/kg, IV (treatment 4). Tiletamine-zolazepam doses were the sum of tiletamine plus Zolazepam. Xylazine, when given IV, was given 5 minutes before tiletamine-zolazepam. Xylazine, when given IM, was given 10 minutes before tiletamine-zolazepam. Tiletamine-zolazepam induced recumbency in all horses. Duration of recumbency in group 1 was 31.9 +/- 7.2 (mean +/- 1 SD) minutes. Increasing the dosage of tiletamine-zolazepam (treatments 2 and 3) significantly (P less than 0.05) increased the duration of recumbency. Xylazine caused significant (P less than 0.05) decreases in heart rate and cardiac output and significant (P less than 0.05) increases in central venous pressure and mean pulmonary artery pressure 5 minutes after administration. Respiratory rate was decreased. Arterial blood pressures increased significantly (P less than 0.05) after xylazine was administered IV in treatments 1 and 3, but the increases were not significant in treatment 2. Xylazine administered IM caused significant (P less than 0.05) increases in central venous pressure and significant (P less than 0.05) decreases in cardiac output.(ABSTRACT TRUNCATED AT 250 WORDS)