Fig. 4.

Similar OP inhibitor specificity profiles for inhibition of [³H]CPO binding to CPO-BP and FP-rhodamine labeling of KIAA1363. (A) FP-biotin and CPO inhibit [³H]CPO binding. Mouse brain membranes and CPO or FP-biotin were incubated together for 15 min before addition of 1 nM [³H]CPO and further incubation for 15 min before filtration. (B) Correlation plot for inhibition of [³H]CPO binding to CPO-BP and FP-rhodamine labeling of KIAA1363. Data are given in Table 3. (C) Inhibition of FP-rhodamine labeling for 11 compounds at 100 nM compared with the control (0). Membranes were incubated with inhibitors for 10 min before addition of 100 nM FP-rhodamine for 10 min. KIAA1363 appears as two glycosylated forms at ≈50 kDa. Some OPs also inhibit FAAH (63 kDa) as discussed in the text. The OP compounds (1-11) are identified in Table 1.