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The cholinergic receptors in rabbit isolated rectus muscle preparations were characterized by means of cholinergic agonists and antagonists. The concentration-dependent contraction induced by acetylcholine, carbachol or oxotremorine remained uninfluenced by atropine (10(-5) M), whereas the nicotinic receptor antagonist hexamethonium caused a parallel shift of the concentration-response curve. The agonists pilocarpine, methacholine and aceclidine, which are selective muscarinic receptor stimulants, did not cause contraction of the muscle preparation. However, the nicotinic receptor stimulant 1,1-dimethyl-4-phenylpiperazine iodide (DMPP) caused contraction similar to that induced by acetylcholine. DMPP-induced contractions were inhibited by hexamethonium, causing a parallel rightward shift of the concentration-response curve. This shift could be quantified by means of a Schild plot, indicating competitive antagonism with a PA2 value of 4.63 for hexamethonium. Atropine when applied together with hexamethonium did not cause a further shift of the concentration-response curve. The present results clearly indicate that the cholinergic receptors which mediate contraction in the rabbit isolated extraocular muscle preparation belong to the nicotinic subtype.
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