| 摘 要： | Ohmefentanyl (F 7302, N[1-(β-hydroxy-β-phenylethyt)-3-methyl-4-piperidyl]-N-phenylpropionamide) is a potent synthetic analgesic agent. The analgesic activity of ohmefentanyl in mice is 6300 times more potent than that of morphine. The potency of ohmefentanyl in competing with specific binding of ~3H-naloxone is reduced by Na~ (100 mM) and GTP(50μM), thus suggesting the agonist properties of this compound. Binding characteristics of ~3Hohmefentanyl with mice brain P_2 fraction are studied. An important saturable, specific and reversible binding is demonstrated. Scatchard analysis indicates the existence of two classes of binding sites (KD_1=0.32nM, KD_2=3.91nM). Various opiate drugs strongly inhibit the binding of ~3H-ohmefentanyl, but nonopiate drugs have negligible affinity. Comparison of the relative potencies of morphine, DSTLE(Tyr-D-Ser-Gly-Phe-Leu-Thr, a specific ligand for the δ-opiate receptor) and ohmefentanyl in competing with ~3H-dihydromorphine (μ) and ~3H[D-Ala~2, D-Leu~5]-enkephalin (
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