Multiple receptor types for octopamine in the locust.

1. Three different pharmacological classes of octopamine receptor mediate the actions of octopamine on the locust extensor-tibiae neuromuscular preparation. A receptor classification scheme is proposed based on the results of detailed studies with agonists and antagonists. 2. Octopamine1 class receptors mediate the slowing of a myogenic rhythm found in a specialized proximal bundle of muscle fibres. Octopamine2A class receptors mediate the increase in amplitude of slow motoneurone twitch tension and octopamine2B class receptors mediate the increase in relaxation rate of twitch tension induced by firing either the fast or the slow motoneurones. 3. Octopamine1 receptors can be distinguished from the 2A and 2B classes since chlorpromazine (and yohimbine) are much better blocking agents than metoclopramide at the former receptors, whereas the converse is true for the latter class. Also clonidine is a more effective agonist than naphazoline for the former receptors and the converse is true for the latter class. 4. Octopamine 2A can be distinguished for octopamine 2B receptors since metoclopramide, mianserin and cyproheptadine show a strong preference for blocking the former class. Also naphazoline is a much better agonist than tolazoline at the former receptors and tolazoline is a much better agonist than clonidine at a latter. 5. The results are discussed in terms of the location of the various classes of octopamine receptors, their possible relationship to vertebrate alpha-adrenoreceptors, and the significance of the results for studies on octopamine receptors in the vertebrate central nervous system.