A novel amperometric detection procedure was developed to determine the ability of the catechol, 2-hydroxyestradiol (2OHE2), to diffuse through and be O-methylated during its passage from the lumen to the adventitial surface of the rabbit ear artery. The diffusion and O-methylation of d-norepinephrine (d-NE) also was determined. When arteries were perfused with either 2OHE2 or d-NE (10 microM), the bulk of the material effluxing from the adventitial surface was O-methylated. The vessel wall offered a considerable barrier to the diffusion of both NE and 2OHE2, because the concentrations of NE and 2OHE2 found in the solution perfusing the adventitial surface were as much as 1,000-fold lower than their concentration in the intralumenal perfusion stream. It is concluded that the blood vessel wall offers a significant physical and metabolic barrier to the penetration of unchanged 2OHE2 and NE.

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