Mitragynine
(Synonyms: 帽柱木碱盐酸盐,(-)-Mitragynine) 目录号 : GC44208An Analytical Reference Material
Cas No.:4098-40-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Mitragynine is an indole alkaloid from the plant M. speciosa. It has stimulatory, antinociceptive, and opiate-like effects, acting through noradrenergic, serotonergic, and opioid receptors. Mitragynine has a higher affinity for the μ-opioid receptor than the δ- or κ-opioid receptors (pKi = 8.14, 7.22, and 5.96, respectively). Mitragynine and its derivatives have been identified in products sold as incense. The identification and quantification of mitragynine and related alkaloids, as well as their phase I and II metabolites, have been described. This product is intended for forensic applications. This product is a qualified Reference Material (RM) that has been manufactured and tested to meet ISO17025 and Guide 34 guidelines. These materials are tested using validated analytical methods on qualified instrumentation to ensure traceability of measurements. All traceable RMs may be distinguished by their CofAs and can be downloaded below using the batch number located on the product label. For a representative CofA please contact our technical support.
| Cas No. | 4098-40-2 | SDF | |
| 别名 | 帽柱木碱盐酸盐,(-)-Mitragynine | ||
| Canonical SMILES | O=C(OC)/C([C@H]([C@H](CC)C1)CC(N1CC2)C3=C2C4=C(OC)C=CC=C4N3)=C/OC | ||
| 分子式 | C23H30N2O4 | 分子量 | 398.5 |
| 溶解度 | Ethanol: 5 mg/ml,Methanol: 10 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5094 mL | 12.5471 mL | 25.0941 mL |
| 5 mM | 0.5019 mL | 2.5094 mL | 5.0188 mL |
| 10 mM | 0.2509 mL | 1.2547 mL | 2.5094 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。
The Chemical and Pharmacological Properties of Mitragynine and Its Diastereomers: An Insight Review
Front Pharmacol 2022 Feb 24;13:805986.PMID:35281925DOI:10.3389/fphar.2022.805986.
Mitragynine, is a naturally occurring indole alkaloid that can be isolated from the leaves of a psychoactive medicinal plant. Mitragyna speciosa, also known as kratom, is found to possess promising analgesic effects on mediating the opioid receptors such as µ (MOR), δ (DOR), and κ (KOR). This alkaloid has therapeutic potential for pain management as it has limited adverse effect compared to a classical opioid, morphine. Mitragynine is frequently regarded to behave like an opioid but possesses milder withdrawal symptoms. The use of this alkaloid as the source of an analgesic candidate has been proven through comprehensive preclinical and clinical studies. The present data have shown that Mitragynine is able to bind to opioid receptors, particularly MOR, to exhibit the analgesic effect. Moreover, the chemical and pharmacological aspects of Mitragynine and its diastereomers, speciogynine, speciociliatine, and mitraciliatine, are discussed. It is interesting to know how the difference in stereochemical configuration could lead to the difference in the bioactivity of the respective compounds. Hence, in this review, the updated pharmacological and toxicological properties of Mitragynine and its diastereomers are discussed to render a comprehensive understanding of the pharmacological properties of Mitragynine and its diastereomers based on their structure-activity relationship study.
Kratom-Associated Fatalities in Northern Nevada-What Mitragynine Level Is Fatal?
Am J Forensic Med Pathol 2021 Dec 1;42(4):341-349.PMID:34091497DOI:10.1097/PAF.0000000000000695.
Mitragyna speciosa, commonly known as the kratom tree, has been utilized in Southeast Asia for centuries for its opioid-like effects. Kratom has been available in the United States for the past decade and has grown increasingly popular despite a lack of clinical research to determine its safety. With its widespread use, there have been an increasing number of fatalities. This study aims to establish a potential lethal range for Mitragynine, the active compound in kratom, by investigating the toxicology reports of 35 deaths in Northern Nevada between 2015 and 2020. Mitragynine concentrations ranged from 8.7 to 1800 ng/mL (n = 27) in cases with drug toxicity as the cause of death; in 1 case, the sole intoxicant was Mitragynine with a blood concentration of 950 ng/mL. In cases with nonmitragynine causes of death, the concentration was 110 to 980 ng/mL (n = 8). There was no statistically significant difference in blood concentrations between cases where Mitragynine was not listed as a cause of death (mean, 315 ± 297.2 ng/mL) and cases in which Mitragynine contributed to death (mean, 269.4 ± 382.5 ng/mL; P < 0.201). A literature review is also presented.
Mitragynine improves cognitive performance in morphine-withdrawn rats
Psychopharmacology (Berl) 2022 Jan;239(1):313-325.PMID:34693456DOI:10.1007/s00213-021-05996-4.
Rationale: The treatment of opiate addiction is an unmet medical need. Repeated exposure to opiates disrupts cognitive performance. Opioid substitution therapy, with, e.g., methadone, may further exacerbate the cognitive deficits. Growing evidence suggests that Mitragynine, the primary alkaloid from the Kratom (Mitragyna speciosa) leaves, may serve as a promising alternative therapy for opiate addiction. However, the knowledge of its health consequences is still limited. Objectives: We aimed to examine the cognitive effects of Mitragynine substitution in morphine-withdrawn rats. Furthermore, we asked whether neuronal addiction markers like the brain-derived neurotrophic factor (BDNF) and Ca2+/calmodulin-dependent kinase II alpha (αCaMKII) might mediate the observed effects. Methods: Male Sprague-Dawley rats were given morphine at escalating doses before treatment was discontinued to induce a spontaneous morphine withdrawal. Then, vehicle or Mitragynine (5 mg/kg, 15 mg/kg, or 30 mg/kg) substitution was given for 3 days. A vehicle-treated group was used as a control. Withdrawal signs were scored after 24 h, 48 h, and 72 h, while novel object recognition (NOR) and attentional set-shifting (ASST) were tested during the substitution period. Results: Discontinuation of morphine significantly induced morphine withdrawal signs and cognitive deficit in the ASST. The substitution with Mitragynine was able to alleviate the withdrawal signs. Mitragynine did not affect the recognition memory in the NOR but significantly improved the reversal learning deficit in the morphine-withdrawn rats. Conclusions: These data support the idea that Mitragynine could be used as safe medication therapy to treat opiate addiction with beneficial effects on cognitive deficits.
Respiratory effects of oral Mitragynine and oxycodone in a rodent model
Psychopharmacology (Berl) 2022 Dec;239(12):3793-3804.PMID:36308562DOI:10.1007/s00213-022-06244-z.
Rationale: Kratom derives from Mitragyna speciosa (Korth.), a tropical tree in the genus Mitragyna (Rubiaceae) that also includes the coffee tree. Kratom leaf powders, tea-like decoctions, and commercial extracts are taken orally, primarily for health and well-being by millions of people globally. Others take kratom to eliminate opioid use for analgesia and manage opioid withdrawal and use disorder. There is debate over the possible respiratory depressant overdose risk of the primary active alkaloid, Mitragynine, a partial μ-opioid receptor agonist, that does not signal through ß-arrestin, the primary opioid respiratory depressant pathway. Objectives: Compare the respiratory effects of oral Mitragynine to oral oxycodone in rats with the study design previously published by US Food and Drug Administration (FDA) scientists for evaluating the respiratory effects of opioids (Xu et al., Toxicol Rep 7:188-197, 2020). Methods: Blood gases, observable signs, and Mitragynine pharmacokinetics were assessed for 12 h after 20, 40, 80, 240, and 400 mg/kg oral Mitragynine isolate and 6.75, 60, and 150 mg/kg oral oxycodone hydrochloride. Findings: Oxycodone administration produced significant dose-related respiratory depressant effects and pronounced sedation with one death each at 60 and 150 mg/kg. Mitragynine did not yield significant dose-related respiratory depressant or life-threatening effects. Sedative-like effects, milder than produced by oxycodone, were evident at the highest Mitragynine dose. Maximum oxycodone and Mitragynine plasma concentrations were dose related. Conclusions: Consistent with Mitragynine's pharmacology that includes partial µ-opioid receptor agonism with little recruitment of the respiratory depressant activating β-arrestin pathway, Mitragynine produced no evidence of respiratory depression at doses many times higher than known to be taken by humans.
Mini review: Potential therapeutic values of Mitragynine as an opioid substitution therapy
Neurosci Lett 2022 Mar 16;773:136500.PMID:35114335DOI:10.1016/j.neulet.2022.136500.
Opioid use disorder (OUD) has become a significant public health issue worldwide. Methadone and buprenorphine are the most common medications used for treating OUD. These drugs have the potential to assist many patients in managing their opioid dependence and withdrawal but they are currently misused and associated with certain compliance issues, side effects, and risk of relapse. As an opioid-like herbal supplement, Mitragyna speciosa Korth or kratom has received increased attention for managing chronic pain and opioid withdrawal symptoms. Nevertheless, the use of kratom as a self-treatment medication for opioid dependence continues to be controversial due to concerns raised about its effectiveness, safety, and abuse liability. The main active alkaloid constituent of the plant, Mitragynine, has been shown to act as a partial mu-opioid agonist. Given this pharmacology, studies have been focusing on this psychoactive compound to examine its potential therapeutic values as medication-assisted therapy (MAT). This review aims to provide a current preclinical overview of Mitragynine as a prospective novel option for MAT and summarise the recent developments in determining if the plant's active alkaloid could provide an alternative to opioids in the treatment of OUD.