Clenbuterol is an agonist at the beta-2 adrenergic receptor, which is a member of the 7-transmembrane receptor superfamily and activates adenylate cyclase. This results in relaxing the smooth bronchial muscles and decreasing airway obstruction.
Its activation of beta-2 adrenergic receptors on Skeletal Muscle and adipose tissue is thought to be responsible for the anabolic and lipolytic properties observed in research models.
Although the stimulation of lipolysis is the classic cyclic AMP-dependent pathway, exactly how beta 2- adrenergic receptor agonism increases skeletal muscle size is not entirely clear.
In animal models, a reduction in calcium, ATP-dependent proteolysis, and an increase in protein synthesis has been demonstrated with clenbuterol. These potential anabolic effects in skeletal muscle have sparked interest in using clenbuterol and similar agents as a possible treatment for muscle wasting.
A pilot study recently found that clenbuterol may improve motor function in animals with spinal and bulbar muscular atrophy.
PHARMACOLOGY OF CLENBUTEROL
Clenbuterol is a beta-2 agonist similar in some structural respects to salbutamol. Agonism of the beta-2 receptor stimulates adenylyl cyclase activity leading to downstream effects of smooth muscle relaxation in the bronchioles.
SIDE EFFECTS OF CLENBUTEROL
Clenbuterol may produce excessive beta-adrenergic stimulation at high doses resulting in:
- Atypical sweating
- Raised body temperature
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- Ryall JG, Gregorevic P, Plant DR, Sillence MN, Lynch GS: Beta 2-agonist fenoterol has greater effects on contractile function of rat skeletal muscles than clenbuterol. Am J Physiol Regul Integr Comp Physiol. 2002 Dec;283(6): R1386-94. Epub 2002 Sep 5. [Article]
- Choo JJ, Horan MA, Little RA, Rothwell NJ: Anabolic effects of clenbuterol on skeletal muscle are mediated by beta 2-adrenoceptor activation. Am J Physiol. 1992 Jul;263(1 Pt 1): E50-6. [Article]
- Sillence MN, Matthews ML, Spiers WG, Pegg GG, Lindsay DB: Effects of clenbuterol, ICI118551, and sotalol on the growth of cardiac and skeletal muscle and n beta 2-adrenoceptor density in female rats. Naunyn Schmiedebergs Arch Pharmacol. 1991 Oct;344(4):449-53. [Article]
- Mazzanti G, Di Sotto A, Daniele C, Battinelli L, Brambilla G, Fiori M, Loizzo S, Loizzo A: A pharmacodynamic study on clenbuterol-induced toxicity: beta1- and beta2-adrenoceptors involvement in guinea-pig tachycardia in an in vitro model. Food Chem Toxicol. 2007 Sep;45(9):1694-9. Epub 2007 Mar 12. [Article]
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