Effects of the enantiomers of R,S-salbutamol on incompletely fused tetanic contractions of slow- and fast-twitch skeletal muscles of the guinea-pig

Abstract

The effects of racemic R,S-salbutamol, and its individual enantiomers have been studied on incompletely fused (sub-tetanic) contractile responses of fast- and slow-contracting isolated skeletal muscles of the guinea-pig.
R,S-salbutamol (2–4 μM) decreased the peak force of sub-tetani in the slow-contracting soleus muscle and increased the peak force of sub-tetani in the fast-contracting peroneus longus muscle. It also increased the force of the first twitch of sub-tetani in both muscles. The decrease in the peak force of sub-tetani in the soleus muscle was due to defusion of the individual twitches caused by a shortening of their time course.
The effects of 4 μM of the racemate on both fast- and slow-contracting muscles were mimicked by 2 μM R-salbutamol (levalbuterol). However, 2 μM S-salbutamol was devoid of activity in both muscles.
We concluded that all the effects of R,S-salbutamol on guinea-pig skeletal muscles are due to the activity of the R-enantiomer. Thus there is a common enantiomeric profile for the skeletal muscle and bronchorelaxant activity of the compound.

Keywords: Salbutamol, levalbuterol, soleus muscle, peroneus longus muscle, isolated muscle tension recording, tetanic defusion, tremor