Characterization of cholecystokinin receptors in canine intestinal circular muscle.

We localized and characterized the binding of [3H](+/-)-L364,718 in canine small intestine circular muscle. The highest densities of [3H]L364,718 binding were located in the fraction enriched in deep muscular plexus synaptosomal membranes. In this fraction [3H]L364,718 binding was of high density (Bmax 136.78 +/- 53.66 fmol/mg) and high affinity (Kd 1.67 +/- 0.74 nM). Kinetics studies revealed that binding was reversible and yielded a similar Kd value. L364,718, CCK-8-S, and L365,260 fully displaced [3H]L364,718 binding, but ligands at CCKB receptors, gastrin-17, and YM022 did not. Therefore, CCKA receptors in canine intestine circular muscle are located on nerve endings.