FIGURE 4.
Receptor fractional occupancy, RA/Rtot, for an interstitial receptor, when there is hindered delivery of the agonist and competition for it from lower-affinity transporters and enzymes in the interstitial space (ISF). Agonist was delivered at high flow into the plasma space with a slowly rising concentration and permeated the capillary with a PS of 0.2 mL/(g·min). The actual receptor KD = 1 μM and the competing enzyme dissociation constant KE = 10 mM, 10,000 times lower affinity. The four curves to the left show RA/Rtot versus interstitial concentration [agonist]ISF. The group of four curves to the right show RA/Rtot versus plasma concentration [agonist]pl.