Terbutaline
(Synonyms: 特布他林) 目录号 : GC45993A β2-adrenergic receptor agonist
Cas No.:23031-25-6
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
Terbutaline is a short-acting β2-adrenergic receptor (β2-AR) agonist and an active metabolite of bambuterol .[1],[2],[3] It binds to β1-, β2-, and β3-ARs (Ki = 31.3, 15.4, and 79.8 nM, respectively) and selectively increases adenylyl cyclase activity in CHO cell membranes expressing recombinant human β2- or β3- over β1-ARs at concentrations 100-fold greater than the respective Ki values.[1] Terbutaline inhibits histamine release induced by ovalbumin in isolated guinea pig lung mast cells.[2] It also inhibits airway obstruction induced by methacholine or leukotriene D4 in anesthetized guinea pigs.[4] Formulations containing terbutaline have been used in the treatment of asthma.
Reference:
[1]. Hoffmann, C., Leitz, M.R., Oberdorf-Maass, S., et al. Comparative pharmacology of human β-adrenergic receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch. Pharmacol. 369(2), 151-159 (2004).
[2]. Lau, H.Y.A., Wong, P.L., and Lai, C.K.W. Effects of β2-adrenergic agonists on isolated guinea pig lung mast cells. Agents Actions 42(3-4), 92-94 (1994).
[3]. Olsson, O.A.T., and Svenson, L.-•. New lipophilic terbutaline ester prodrugs with long effect duration. Pharm. Res. 1(1), 19-23 (1984).
[4]. Salonen, R.O. Actions of bronchodilator drugs, glucocorticoid, and their combinations on airways in rats and guinea pigs. Acta. Pharmacol. Toxicol. (Copenh) 57(Suppl. 3), 1-38 (1985).
| Cas No. | 23031-25-6 | SDF | |
| 别名 | 特布他林 | ||
| 化学名 | 5-[2-[(1,1-dimethylethyl)amino]-1-hydroxyethyl]-1,3-benzenediol | ||
| Canonical SMILES | OC1=CC(O)=CC(C(O)CNC(C)(C)C)=C1 | ||
| 分子式 | C12H19NO3 | 分子量 | 225.3 |
| 溶解度 | DMSO: slightly soluble,Methanol: slightly soluble,Water: 100 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 | 4.4385 mL | 22.1926 mL | 44.3853 mL |
| 5 mM | 0.8877 mL | 4.4385 mL | 8.8771 mL |
| 10 mM | 0.4439 mL | 2.2193 mL | 4.4385 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。
Terbutaline attenuates LPS-induced injury of pulmonary microvascular endothelial cells by cAMP/Epac signaling
Drug Dev Res 2022 May;83(3):699-707.PMID:34846077DOI:10.1002/ddr.21901.
Acute lung injury (ALI), characterized by an acute onset of severe hypoxemia, is a common and devastating syndrome usually triggered by lipopolysaccharide (LPS) infection from bacteria. This study is intended to explore whether Terbutaline can alleviate LPS-induced human pulmonary microvascular endothelial cell (HPMVEC) injury through cAMP/Epac signaling. LPS was utilized to induce ALI in HPMVECs, and after exposure of LPS-induced HPMVECs to Terbutaline, the cellular functions including cell viability and apoptosis were measured by cell counting kit-8 and terminal deoxynucleotidyl transferase dUTP nick-end labeling. The protein expression related to cAMP/Epac signaling, apoptosis, and that of tight junction and inflammatory factors were evaluated at the same time. The effects of Terbutaline on cellular functions were confirmed again after the addition of antagonists of cAMP and Epac, respectively. The levels of both cAMP and Epac reduced by LPS was concentration-dependently increased by Terbutaline. The apoptosis and endothelial cell permeability damage of LPS-induced HPMVECs were enhanced after the addition of KT-5720 and ESI-09. The beneficial effects of Terbutaline on alleviating the inflammation and apoptosis in HPMVECs injured by LPS are mediated by cAMP/Epac signaling, and this evidence would demonstrate the potential of Terbutaline in the treatment of ALI.
Effectiveness of Terbutaline pump for the prevention of preterm birth. A systematic review and meta-analysis
PLoS One 2012;7(2):e31679.PMID:22363704DOI:10.1371/journal.pone.0031679.
Background: Subcutaneous Terbutaline (SQ Terbutaline) infusion by pump is used in pregnant women as a prolonged (beyond 48-72 h) maintenance tocolytic following acute treatment of preterm contractions. The effectiveness and safety of this maintenance tocolysis have not been clearly established. We aimed to systematically evaluate the effectiveness and safety of subcutaneous (SQ) Terbutaline infusion by pump for maintenance tocolysis. Methodology/principal findings: MEDLINE, EMBASE, CINAHL, the Cochrane Library, the Centre for Reviews and Dissemination databases, post-marketing surveillance data and grey literature were searched up to April 2011 for relevant experimental and observational studies. Two randomized trials, one nonrandomized trial, and 11 observational studies met inclusion criteria. Non-comparative studies were considered only for pump-related harms. We excluded case-reports but sought FDA summaries of post-marketing surveillance data. Non-English records without an English abstract were excluded. Evidence of low strength from observational studies with risk of bias favored SQ Terbutaline pump for the outcomes of delivery at <32 and <37 weeks, mean days of pregnancy prolongation, and neonatal death. Observational studies of medium to high risk of bias also demonstrated benefit for other surrogate outcomes, such as birthweight and neonatal intensive care unit (NICU) admission. Several cases of maternal deaths and maternal cardiovascular events have been reported in patients receiving Terbutaline tocolysis. Conclusions/significance: Although evidence suggests that pump therapy may be beneficial as maintenance tocolysis, our confidence in its validity and reproducibility is low, suggesting that its use should be limited to the research setting. Concerns regarding safety of therapy persist.
Terbutaline Accumulates in Blood and Urine after Daily Therapeutic Inhalation
Med Sci Sports Exerc 2017 Jun;49(6):1236-1243.PMID:28072631DOI:10.1249/MSS.0000000000001199.
Purpose: This study investigated pharmacokinetics of Terbutaline after single and seven consecutive days of inhalation in exercising trained men. Methods: Twelve healthy trained men underwent two pharmacokinetic trials comparing single dose (2 mg) and seven consecutive days (2 mg·d) of inhaled Terbutaline. After inhalation of Terbutaline at each trial, subjects performed 90 min of bike ergometer exercise at 55%-65% of maximal oxygen consumption after which they stayed inactive. Blood and urine samples were collected before and after inhalation of Terbutaline. Samples were analyzed by high-performance liquid chromatography-tandem mass spectrometry. Results: Maximum serum concentration of Terbutaline (Cmax) (6.4 ± 1.2 vs 4.9 ± 1.2 ng·mL, P = 0.01) (mean ± 95% confidence interval) and area under serum concentration-time curve from 0 to 4 h after inhalation (AUC0-4) (16 ± 3 vs 13 ± 2 ng·mL·h, P ≤ 0.005) were higher after 7 d of inhalation compared with the first day. Seven days of Terbutaline inhalation resulted in accumulation of Terbutaline in urine, in which total urine excretion of Terbutaline was higher after 7 d of inhalation compared with the first day (274 ± 43 vs 194 ± 33 μg, P ≤ 0.001). These differences were partly attributed to systemic accumulation of Terbutaline after consecutive days of inhalation, in that baseline serum and urine samples revealed incomplete elimination of Terbutaline. Conclusion: Terbutaline accumulates in serum and urine after consecutive days of inhalation. For doping control purposes, these observations are of relevance if a urine threshold and decision limit is to be introduced for Terbutaline on the World Anti-Doping Agency's list of prohibited substances because asthmatic athletes may use their bronchorelievers for consecutive days.
[Pulmonary function tests with the bronchodilator Terbutaline]
Acta Med Austriaca Suppl 1979;14:1-39.PMID:161461doi
The acute bronchodilator effect of the beta 2-adrenoceptor agonist Terbutaline was tested single-blind cross-over in out-patients with chronic obstructive airways disease (intrinsic asthma). In 7 series comparisons were made with other marketed bronchodilators. Airways resistance was measured by whole body plethysmography. In another 3 series the effect on heart rate of Terbutaline and other adrenocepter agonists was tested in healthy volunteers. Terbutaline and the adrenoceptor agonists clenbuterol, epinephrine, fenoterol, hexoprenaline, isoprenaline, metaproterenol, reproterol and salbutamol, the vagolytics atropine, ipratropium bromide and AA 22-263, the xanthinederivative theophylline ethylenediamine and one combined substance drug were used.
Terbutaline and ephedrine in asthmatic children
Pediatrics 1977 Jul;60(1):14-9.PMID:327422doi
The effects of Terbutaline, ephedrine, and placebo on the cardiovascular and pulmonary systems have been compared in 24 asthmatic children. Ephedrine and Terbutaline were both found to be effective bronchodilators, with onset of action within 30 minutes. The bronchodilator effect of ephedrine was maintained for three hours, while Terbutaline was active for five hours. Terbutaline caused significantly greater improvement in pulmonary functions than did ephedrine. Both Terbutaline and ephedrine were associated with clinically insignificant changes in blood pressure and pulse rate. The only significant side effect observed was hand tremor in children receiving Terbutaline and this appeared only early in the course of drug treatment. There was no evidence of tolerance to the bronchodilator effect of ephedrine or Terbutaline after eight weeks of therapy.