02 Mabuterol powder (56341-08-3) video
03 Mabuterol powder (56341-08-3) Base Information
|Chemical name||4-Amino-alpha-((tert-butylamino)methyl)-3-chloro-5-(trifluoromethyl)benzyl alcohol|
|Molecular Weight||310.74 g/mol|
|Appearance||Yellow to light orange powder|
|Solubility||Chloroform (Slightly), Methanol (Slightly)|
|Storage Condition||0 – 4 C for short term (days to weeks), or -20 C for long term (months).|
|Application||Mabuterol is a selective β2 adrenoreceptor agonist, used as a bronchodilator/antiasthmatic.|
04 Mabuterol powder (56341-08-3) General Description
Mabuterol powder is a selective β2 adrenoreceptor agonist. Mabuterol has a specific effect on beta 2-adrenoceptors with no beta 1-stimulation. Mabuterol inhibited the positive inotropic effect of isoprenaline at 10(-7) g/ml and decreased the maximum driving frequency at 3 X 10(-6) g/ml. Mabuterol was 3 times more potent in relaxing the isolated rat uterus, but 700 times less potent than isoprenaline in relaxing the rabbit jejunum. Mabuterol (p.o.) depressed the intestinal propulsion and was equipotent to isoprenaline and 2.5 times less potent than salbutamol.
05 Mabuterol (56341-08-3) History
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.2 Administration of mabuterol decreases blood pressure and increases heart rate in a dose-dependent manner in rats, cats, and dogs.3 These effects are reversed by the selective β2-AR antagonist ICI 118551 (Item No. 15591), indicating mabuterol is acting at β2-ARs.1 At concentrations ≥1 μM, mabuterol acts as a β1-AR antagonist in isolated dog right atria.
06 Mabuterol (56341-08-3) Mechanism Of Action
Mabuterol is a long acting βeta 2-adrenergic agonist which stimulates adenylyl cyclase activity and the closing of calcium channels. Studies indicate that the R enantiomer of mabuterol is more potent than the S enantiomer. In addition, the half-life is longer in the R enantiomer than the S. Studies conducted on rats and dogs show that mabuterol acts as a bronchodilator. At high concentrations mabuterol can also antagonize beta1 adrenoceptors in guinea pig
07 Mabuterol (56341-08-3) Application
The administration of β-agonists as growth promoters has been strictly prohibited in most countries of the world. β-Agonists are usually used as therapeutic treatments for asthma in humans. However, because of their significant nutrition redistribution function, β-agonists have been used in the livestock industry, including pigs and ruminants, to reduce the carcass fat and increase the muscle mass while improving the growth and feed conversion rates.
08 Mabuterol (56341-08-3) More research
The enantiomeric resolution of adrenergic β2‐Agonists (clenbuterol, cimaterol, and mabuterol) on different Chirobiotic columns (Chirobiotic V, T, and TAG) has been achieved with methanol‐acetonitrile‐triethylamine (80 : 20 : 0.05, v/v/v) as mobile phase. The α values of the resolved enantiomers of clenbuterol, cimaterol, and mabuterol were 1.10 to 4.26 while the values of Rs varied from 1.0 to 2.10. The resolution was in the order of Chirobiotic V > Chirobiotic TAG > Chirobiotic T whereas the enantioselectivity was in the order of Chirobiotic TAG > Chirobiotic V > Chirobiotic T. The enantiomeric resolution of adrenergic β2‐agonists on Chirobiotic columns is governed by a complex mechanism involving various types of steric interactions.
09 Mabuterol (56341-08-3) Document Download
10 Mabuterol (56341-08-3) Reference
Akahane, K., Furukawa, Y., Ogiwara, Y., et al. β-adrenoceptor blocking effects of a selective β2-agonist, mabuterol, on the isolated, blood-perfused right atrium of the dog Br. J. Pharmacol. 97(3), 709-716 (1989).
Murai, T., Maejima, T., and Osada, E. Pharmacological studies of mabuterol, a new selective beta 2-stimulant. I: Bronchodilating effect Arzneimittelforschung 34(11A), 1633-1640 (1984).
Osada, E., Murai, T., Ishizaka, Y., et al. Pharmacological studies of mabuterol, a new selective beta 2-stimulant. II: Effects on the cardiovascular system and smooth muscle organs Arzneimittelforschung 34(11A), 1641-1651 (1984).
- 01. Overview
- 02. Mabuterol powder (56341-08-3) video
- 03. Mabuterol powder (56341-08-3) Base Information
- 04. Mabuterol powder (56341-08-3) General Description
- 05. Mabuterol (56341-08-3) History
- 06. Mabuterol (56341-08-3) Mechanism Of Action
- 07. Mabuterol (56341-08-3) Application
- 08. Mabuterol (56341-08-3) More research
- 09. Mabuterol (56341-08-3) Document Download
- 10. Mabuterol (56341-08-3) Reference