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Effects of the enantiomers of R,S-salbutamol on incompletely fused tetanic contractions of slow- and fast-twitch skeletal muscles of the guinea-pig
Authors:Chris Prior  Maureen B Leonard  John R McCullough
Affiliation:1.Department of Physiology and Pharmacology, University of Strathclyde, Royal College Building, 204 George Street, Glasgow G1 1XW, Scotland;2.Sepracor Inc., 111 Locke Drive, Marlborough, MA 01752, U.S.A.
Abstract:
  1. 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.
  2. 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.
  3. 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.
  4. 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
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