Activities of Octopamine and Synephrine Stereoisomers on Octopaminergic Receptor Subtypes in Locust Skeletal Muscle

Abstract

The activities of the (-) and (+)- forms of p-, m- and o-octopamine and p- and m-synephrine have been compared on the different subtypes of octopamine receptor present in the extensor-tibiae neuromuscular preparation from the locust hindleg. The rank order of potency of the (-)-forms on the OCTOPAMINE2A receptors was p-synephrine greater than p-octopamine greater than m-octopamine greater than o-octopamine greater than m-synephrine whilst the rank order of the (+)-forms was p-synephrine greater than p-octopamine greater than m-octopamine. (+)-m-Synephrine and (+)-o-octopamine had no effect on this class of receptor when tested up to a concentration of 10(-3) M. The rank order of potency of the (-)-forms on the OCTOPAMINE2B receptors was p-synephrine greater than p-octopamine greater than m-synephrine greater than m-octopamine greater than o-octopamine whilst the rank order of the (+)-forms was p-octopamine greater than p-synephrine greater than m-octopamine greater than o-octopamine. (+)-m-Synephrine again had no effect up to a concentration of 10(-3) M. The rank order of potency of the (-)-forms on the OCTOPAMINE1 receptors was p-synephrine greater than p-octopamine greater than m-synephrine greater than m-octopamine greater than o-octopamine, whilst the rank order of the (+)-forms was p-synephrine greater than p-octopamine greater than o-octopamine greater than m-synephrine greater than m-octopamine.(ABSTRACT TRUNCATED AT 250 WORDS)