Arteriolar endothelial cell barrier separates two populations of muscarinic receptors.

The endothelium of arterioles can function as a barrier to diffusion of hydrophilic molecules when studied in vitro. Thus a substance applied to one side of the arteriole is relatively ineffective in reaching receptors on the opposite side of the vessel wall unless it is lipid soluble. To study the receptor populations on the two sides of the arteriolar endothelium, we used micropipettes to apply methacholine (MCh; 1.0 microM), either luminally or adventitially, for 5 s to the arterioles of the cheek pouch of pentobarbital-anesthetized hamsters. MCh equally dilated the arterioles regardless of the side of application. That different populations of receptors are located on either side of the arteriole was shown by the fact that adventitially applied hydrophilic methscopolamine was ineffective in blocking the effects of the luminally applied MCh but completely blocked the effects of abluminally applied MCh. In contrast, the luminal population of receptors was easily blocked by adventially applied scopolamine, which is lipophilic. Separate and independent populations of receptors in the vessel wall suggests the potential for differential control between humoral and adventitial sources of vasoactive metabolites.