Comparison of the muscarinic cholinoceptors in the rabbit ciliary body and the guinea-pig ileum.

Interactions of several muscarinic drugs with their receptors were studied in the ciliary body smooth muscle of rabbits and the ileal longitudinal muscle of guinea-pigs, using pharmacological and biochemical procedures. The dissociation constants of carbachol, pilocarpine, atropine and pirenzepine estimated by these procedures indicate no heterogeneity of muscarinic receptors in either tissue; thus both are probably of the M2 type. However, the density of the receptors in the ciliary body is lower than in the ileum. Pilocarpine, with lower intrinsic efficacy, demonstrated a pronounced organ selectivity when compared to carbachol as it was a potent full agonist in the ileum and a competitive antagonist in the ciliary body. These results suggest the importance of both receptor density and threshold as determinants of agonist potency.