Theodrenaline ((±)-Theodrenaline)
(Synonyms: 茶碱那林; (±)?-?Theodrenaline) 目录号 : GC32621
Theodrenaline ((±)-Theodrenaline) 是一种心脏兴奋剂，也可与咖啡碱一起用作抗低血压剂。
Cas No.:13460-98-5
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
Theodrenaline is a cardiac stimulant, also acts as an anti-hypotensive agent together with cafedrine.
Akrinor evokes a positive inotropic effect in human atrial trabeculae via stimulation of β-adrenoceptors (AR)[1].
AkrinorTM produces significant potentiation of FSK effects, conceivable by PDE-inhibition, only at very high, clinically irrelevant concentrations of 420 mg/L[1].
[1]. Kloth B, et al. AkrinorTM, a Cafedrine/ Theodrenaline Mixture (20:1), Increases Force of Contraction of Human Atrial Myocardium But Does Not Constrict Internal Mammary Artery In Vitro. Front Pharmacol. 2017 May 23;8:272.
| Cas No. | 13460-98-5 | SDF | |
| 别名 | 茶碱那林; (±)?-?Theodrenaline | ||
| Canonical SMILES | O=C(N1C)N(C)C2=C(N(CCNCC(C3=CC=C(O)C(O)=C3)O)C=N2)C1=O | ||
| 分子式 | C17H21N5O5 | 分子量 | 375.38 |
| 溶解度 | Soluble in DMSO | 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 | 2.664 mL | 13.3198 mL | 26.6397 mL |
| 5 mM | 0.5328 mL | 2.664 mL | 5.3279 mL |
| 10 mM | 0.2664 mL | 1.332 mL | 2.664 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。
Cafedrine/Theodrenaline (20:1) Is an Established Alternative for the Management of Arterial Hypotension in Germany-a Review Based on a Systematic Literature Search
Front Pharmacol 2017 Feb 21;8:68.PMID:28270765DOI:10.3389/fphar.2017.00068.
A 20:1 combination of cafedrine:Theodrenaline (Akrinor®) is widely used in Germany for the treatment of hypotensive states during anesthesia and in emergency medicine. Although this drug formulation has been available since 1963, there are few studies relating to its use and many of the data are only available in German. In this article, we summarize the available data and propose mechanisms for the effects of cafedrine/Theodrenaline on cardiac muscle cells and vascular smooth muscle cells. Cafedrine/Theodrenaline leads to a rapid increase in mean arterial pressure that is characterized by increased cardiac preload, stroke volume, and cardiac output. Systemic vascular resistance and heart rate remain mostly unchanged. Factors which impact the effects of cafedrine/Theodrenaline are gender, high arterial pressure at baseline, use of β-blockers, and heart failure. Importantly, the drug is frequently used in obstetric anesthesia without detrimental effects on umbilical cord pH or APGAR score.
Cafedrine/Theodrenaline in anaesthesia: influencing factors in restoring arterial blood pressure
Anaesthesist 2015 Mar;64(3):190-6.PMID:25757552DOI:10.1007/s00101-015-0005-y.
Background: Hypotensive states that require fast stabilisation of blood pressure can occur during anaesthesia. In 1963, the 20:1 mixture of cafedrine/Theodrenaline (Akrinor) was introduced in Germany for use in anaesthesia and emergency medicine in the first-line management of hypotensive states. Though on the market for many years, few pharmacodynamic data are available on this combination net beta-mimetic agent. Aim: This study aimed to examine the drug combination in real-life clinical practice and recorded time to 10 % mean arterial blood pressure (MAP) increase and heart rate. Furthermore, potential factors that influence drug effectiveness under anaesthesia were assessed. Methods: Data were collected within a standardised anaesthesia protocol. A total of 353 consecutive patients (female/male = 149/204) who received cafedrine/Theodrenaline after a drop in MAP ≥ 5% were included in the study. The time to 10 % increase in MAP, dosage of cafedrine/Theodrenaline, volume loading, blood pressure and heart rate were monitored over time. Results: Patients were a mean (standard deviation) of 64.4 ± 15.1 years old with a baseline MAP of 82 ± 14 mmHg, which dropped to a mean of 63 ± 10 mmHg during anaesthesia without gender differences. Cafedrine/Theodrenaline (1.27 ± 1.0 mg/kg; 64 ± 50 µg/kg) significantly increased MAP (p < 0.001) by 11 ± 16 mmHg within 5 min, reaching peak values within 17.4 ± 9.0 min. Heart rate was not affected in a clinically significant manner. Cafedrine/Theodrenaline induced a 10% MAP increase after 7.2 ± 4.6 min (women) and after 8.6 ± 6.3 min (men) (p = 0.018). Independent of gender, the dose of cafedrine/Theodrenaline required to achieve the observed MAP increase of 14 ± 16 mmHg at 15 min was significantly different in patients with heart failure [1.78 ± 1.67 mg/kg (cafedrine)/89.0 ± 83.5 µg/kg (Theodrenaline)] compared with healthy patients [1.16 ± 0.77 mg/kg (cafedrine)/58.0 ± 38.5 µg/kg (Theodrenaline)] (p = 0.005). Concomitant medication with beta-blocking agents significantly prolonged the time to 10 % MAP increase [9.0 ± 7.0 vs. 7.3 ± 4.3 min (p = 0.008)]. Conclusion: Cafedrine/Theodrenaline quickly restores MAP during anaesthesia. Female gender is associated with higher effectiveness, while heart failure and beta-blocker administration lower the anti-hypotonic effect. Prospective studies in defined patient populations are warranted to further characterise the effect of cafedrine/Theodrenaline.
Reporting dinaciclib and Theodrenaline as a multitargeted inhibitor against SARS-CoV-2: an in-silico study
J Biomol Struct Dyn 2022 Apr 22;1-11.PMID:35451934DOI:10.1080/07391102.2022.2060308.
Severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) is one of the rapid spreading coronaviruses that belongs to the Coronaviridae family. The rapidly evolving nature of SARS-CoV-2 results in a variety of variants with a capability of evasion to existing therapeutics and vaccines. So, there is an imperative need to discover potent drugs that can able to disrupt the function of multiple drug targets to tackle the SARS-CoV-2 menace. Here in this study, we took the different targets of SARS-CoV-2 prepared in the Schrodinger maestro. The library of the DrugBank database is screened against the selected crucial targets. Our molecular docking, Molecular Mechanics/Generalized Born Surface Area (MMGBSA), and molecular dynamics simulation studies led to identifying dinaciclib and Theodrenaline as potential drugs against multiple drug targets: main protease, NSP15-endoribonuclease and papain-like-protease, of SARS-CoV-2. Dinaciclib with papain-like protease and NSP15-endoribonuclease show the docking score of -7.015 and -8.737, respectively, while the Theodrenaline with NSP15-endoribonuclease and main protease produced the docking score of -8.507 and -7.289, respectively. Furthermore, the binding free energy calculations with MM/GBSA and molecular dynamics simulation studies of the complexes confirm the reliability of the drugs. The selected drugs are capable of binding to multiple targets simultaneously, thus withstanding their activity of target disruption in different variants of SARS-CoV-2. Although, the repurposed drugs are showing potent activity, but may need further in-vitro and in-vivo validations.Communicated by Ramaswamy H. Sarma.
Phenylephrine versus cafedrine/Theodrenaline (Akrinor) for the treatment of spinal anaesthesia-induced maternal hypotension during caesarean section: a retrospective single-centre cohort study
BMJ Open 2022 Nov 16;12(11):e062512.PMID:36385024DOI:10.1136/bmjopen-2022-062512.
Objective: The main objective of this study was to assess the impact of phenylephrine and cafedrine/Theodrenaline on the mother and newborn after spinal anaesthesia for caesarean section. Setting: University teaching hospital. Design: A single-centre retrospective data cohort study. Patients: All obstetric patients who were scheduled for caesarean section in a 2-year period. Interventions: Administration of either intravenous phenylephrine prophylactically or cafedrine/Theodrenaline (Akrinor) reactively to maintain blood pressure after spinal anaesthesia. Main outcome measure: Maternal hypotension, heart rate during caesarean section and after admission to IMC, fetal arterial cord pH and base excess levels, maternal volume resuscitation and the use of rescue medication. Results: 852 data sets could be included: n=440 Akrinor, n=412 in the phenylephrine cohort. During caesarean section blood pressure was slightly higher in the phenylephrine group compared with the Akrinor group, while hypotension <100 mm Hg systolic blood pressure (SBP) occurred significantly more often during arrival at the IMC after surgery when phenylephrine was used. Heart rate was lower and rescue medication was significantly more frequently given in the phenylephrine cohort. Irrespective of the medication used, women with baseline levels of <120 mm Hg SBP had a high risk to develop hypotension <100 mm Hg after spinal anaesthesia for caesarean section. While there was no statistical difference in mean umbilical arterial pH levels, the incidence of acidosis, defined as pH <7.2, was significantly higher with phenylephrine. Conclusion: Phenylephrine was not superior to Akrinor to treat spinal anaesthesia-induced maternal hypotension during caesarean section. Trial registration number: DRKS00025795.
[Hemodynamic effects of cafedrine/Theodrenaline on anesthesia-induced hypotension]
Anaesthesist 2018 Oct;67(10):766-772.PMID:30132111DOI:10.1007/s00101-018-0472-z.
Background: There is insufficient knowledge about the hemodynamic effects of cafedrine/Theodrenaline (caf/theo), a commercially available drug combination, to treat hypotension. Methods: This prospective observational study investigated the hemodynamic effects of caf/theo on anesthesia-induced hypotension in 20 patients scheduled for elective major abdominal surgery. After induction of total intravenous anesthesia (TIVA) with propofol and remifentanil, a decrease in mean arterial blood pressure (MAP) below 60 mm Hg (n = 12) was treated with 60 mg/3 mg caf/theo. The systemic vascular resistance index (SVRI), cardiac index (CI), global end-diastolic index (GEDI), maximum pressure increase in the aorta (dPmx) and global ejection fraction (GEF) were assessed by transpulmonary thermodilution (PiCCO2-Monitor). Results: The MAP increased by approximately 60% 10 min after administration of caf/theo. The increase in MAP was a result of the simultaneous effects on various cardiovascular determinants. An increase in peripheral resistance (SVRI +42%) and CI (+17%) could be determined. Data further indicated that the increase in CI was a consequence of an increase in both dPmx (+31%) and GEDI (+9%) but the GEF remained constant. Conclusion: In anesthesia-induced hypotension caf/theo effectively increased the mean arterial blood pressure by combined effects on preload, contractility, and afterload without altering cardiovascular efficiency.