Mabuterol
(Synonyms: 马布台诺) 目录号 : GC44112A β2-adrenergic receptor agonist
Cas No.:56341-08-3
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
Mabuterol is an agonist of the β2-adrenergic receptor (β2-AR). It induces relaxation of isolated tracheal muscle in guinea pigs and inhibits bronchoconstriction in a guinea pig model of experimental asthma. Administration of mabuterol decreases blood pressure and increases heart rate in a dose-dependent manner in rats, cats, and dogs. These effects are reversed by the selective β2-AR antagonist ICI 118551 , indicating mabuterol is acting at β2-ARs. At concentrations ≥1 μM, mabuterol acts as a β1-AR antagonist in isolated dog right atria.
| Cas No. | 56341-08-3 | SDF | |
| 别名 | 马布台诺 | ||
| Canonical SMILES | ClC1=C(N)C(C(F)(F)F)=CC(C(O)CNC(C)(C)C)=C1 | ||
| 分子式 | C13H18ClF3N2O | 分子量 | 310.7 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 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 | 3.2185 mL | 16.0927 mL | 32.1854 mL |
| 5 mM | 0.6437 mL | 3.2185 mL | 6.4371 mL |
| 10 mM | 0.3219 mL | 1.6093 mL | 3.2185 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。
Toxicology of Mabuterol
Arzneimittelforschung 1984;34(11A):1680-4.PMID:6152161doi
The acute, subacute and chronic toxicity of dl-1- (4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butyl-amino-ethanol hydrochloride (Mabuterol), a new beta 2-selective adrenoceptor stimulant, was studied in mouse, rat, rabbit and dog. The acute oral LD50 was between 199.9 and 319.3 mg/kg in all four species used and did not differ significantly between the sexes. Intravenous LD50 was between 18.3 and 51.1 mg/kg (four species), i.p. between 60 and 78.3 mg/kg and s.c. between 113 and 125.7 mg/kg (mouse and rat only). In subacute and chronic studies in Wistar rats, Mabuterol was dosed by gavage at 0, 10, 20, 40, 80 and 120 mg/kg for 1 month, and 0, 1, 2.5, 10 and 40 mg/kg for 3 (interim) and 6 months or in food at 0, 2.5, 10 and 40 mg/kg for 6 (interim) and 12 months. Beagle dogs were dosed by gelatine capsule with 0, 0.05, 0.5, 5 and 50 (25) mg/kg for 6 (interim) and 24 months. In rats, 1 and 2.5 mg/kg were well tolerated. At 10 mg/kg and above, irritability and hypersalivation were seen dependent on dose. Two males and one female given 120 mg/kg died from the test substance. In dogs, 0.05, 0.5 and 5 mg/kg were well tolerated. 50 mg/kg caused vomiting, diarrhoea, tonic-clonic convulsions and increased salivation. One male had to be killed because of severe convulsions. At term, 3 of 56 female rats of the one-year study had benign mesovarian leiomyomas. No other substance-related changes were discovered but all findings belonged to the spontaneous pathology of rat and dog, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)
Enantioselective pharmacokinetics of Mabuterol in rats studied using sequential achiral and chiral HPLC
Biomed Chromatogr 2005 Nov;19(9):703-8.PMID:16206140DOI:10.1002/bmc.584.
The enantioselective pharmacokinetics of Mabuterol was studied in six rats after single oral dose administration of Mabuterol racemate. Serial plasma samples were collected and the pharmacokinetic behavior of each enantiomer in rats was characterized using a sequential achiral and chiral liquid chromatographic method. This method involved the separation of Mabuterol racemate from endogenous substances on an achiral ODS column and enantiomeric separation on a Chirobiotic V column. The plasma-concentration data were analyzed for individual Mabuterol enantiomer using 3P97 software. After i.g. administration of Mabuterol racemate at a dose of 10 mg/kg, both enantiomers were slowly absorbed, reaching mean C(max) of 266.8 and 277.9 ng/mL at t(max) of 5.3 and 5.7 h for R- and S-mabuterol, respectively. The AUC(0-infinity) (5,938.9 ng h/mL) of R-mabuterol was significantly higher than that (4,446.1 ng h/mL) of S-mabuterol, and the half-life (14.5 h) was longer than that (9.6 h) of S-mabuterol (p < 0.001 and p < 0.01, respectively), showing that enantioselective pharmacokinetics between Mabuterol enantiomers occur during the metabolism phase.
Enzyme immunoassay for Mabuterol, a selective beta 2-adrenergic stimulant in the trachea
J Immunoassay 1985;6(3):261-76.PMID:3900139DOI:10.1080/01971528508063033.
A sensitive double antibody and heterologous enzyme immunoassay for Mabuterol was established. For competitive reactions, antibody raised against diazotized mabuterol-human serum albumin was incubated with a mixture of diazotized Mabuterol analog (RC-1) labeled with beta-D-galactosidase and standard or sample. Free and antibody-bound enzyme hapten were separated using anti-rabbit IgG immobilized on polystyrene balls. Activity of the enzyme on the solid phase was fluorometrically determined. The present immunoassay allows detection of 0.5 to 100 pg/tube of Mabuterol. Pharmacokinetic behavior of this agent in human plasma and urine was studied after a single oral administration (50 micrograms). The maximum level was achieved after 2-3 hrs with approximately 280 pg Mabuterol /ml of plasma and the half life of Mabuterol was estimated to be 19.5 hrs. Cumulative amount of Mabuterol in the first 72 hrs urine was 64.3 +/- 13.2% of the administered dose.
Inhibitory effect of Mabuterol on proliferation of rat ASMCs induced by PDGF-BB via regulating [Ca2+]i and mitochondrial fission/fusion
Chem Biol Interact 2019 Jul 1;307:63-72.PMID:31009640DOI:10.1016/j.cbi.2019.04.023.
This study is aimed to investigate whether Mabuterol (Mab) inhibits proliferation of airway smooth muscle cells (ASMCs) induced by platelet-derived growth factor BB (PDGF-BB) and how far it is related to mitochondrial fission/fusion and intracellular calcium if it comes into play. To explore the mechanism of Mab's antagonizing the proliferation, Mdivi-1, DRP1 inhibitor, which has an inhibitory effect on mitochondrial fission, is used to compare with Mab. Cell viability was measured by either MTT or CCK-8. The inhibitory effect of Mab on S phase of ASM cell cycle induced by PDGF-BB was analyzed by flow cytometry (FCM). Fluo-3/AM, Ca2+ fluorescent probe, was used to detect Ca2+ fluorescence intensity by inverted microscope and flow cytometry. The gene expression of Drp-1 and Mfn-2 was observed with Real time PCR and the proteins of Drp-1, Mfn-2, PCNA and cyclin D1 were assessed by Western Blot. Mab and Mdivi-1 both suppressed the proliferation induced by PDGF-BB. The results from inverted microscope and flow cytometry showed that Mab inhibited [Ca2+]i in rat ASMCs induced by PDGF-BB. Cell cycle concept map illustrated that Mab significantly controlled the S phase of ASM cell cycle induced by PDGF-BB. As a consequence, Real time PCR and Western blot revealed the fact that Mab decreased the expression of Drp-1 mRNA and protein, and promoted the expression of Mfn-2 mRNA and protein. These findings suggested that Mab placed restrictions on the proliferation of rat ASMCs induced by PDGF-BB and the mechanism might be associated with the intracellular calcium inhibited and the mitochondrial fission/fusion regulated by Mab.
Beta-adrenoceptor blocking effects of a selective beta 2-agonist, Mabuterol, on the isolated, blood-perfused right atrium of the dog
Br J Pharmacol 1989 Jul;97(3):709-16.PMID:2474351DOI:10.1111/j.1476-5381.1989.tb12007.x.
1. Effects of (+/-)-1-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.- butylamino-ethanol hydrochloride (Mabuterol) on pacemaker activity and atrial contractility were investigated in the isolated and blood-perfused right atrium of the dog. 2. Mabuterol, injected into the sinus node artery of the isolated atrium, dose-dependently increased atrial rate and contractile force at doses of 0.01-10 nmol but the responses to over 10 nmol of Mabuterol gradually decreased and Mabuterol at higher doses induced biphasic cardiac responses, i.e., negative followed by positive cardiac responses. 3. The maximal increases in atrial rate and contractile force induced by Mabuterol were 41.4% and 12.9%, respectively, of the maximal chronotropic and inotropic effects of isoprenaline. 4. Positive chronotropic and inotropic responses to Mabuterol were dose-dependently inhibited by a selective beta 2-adrenoceptor antagonist, ICI 118,551. These responses were only slightly attenuated by atenolol. 5. Mabuterol (1-300 nmol) dose-dependently inhibited both dobutamine- and procaterol-induced positive chronotropic and inotropic responses. 6. These results indicate that Mabuterol causes weak positive chronotropic and inotropic effects on the perfused canine right atrium by activating beta 2-adrenoceptors, and that higher concentrations non-selectively block both beta 1-and beta 2-adrenoceptors.