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- W2011647029 abstract "Tifluadom, a benzodiazepine κ-opiate agonist, stereoselectively inhibited the binding of 125I-CCK to pancreatic membranes (IC50=47 nM). Several other opiate agonists were ineffective. Scatchard analysis indicated the inhibition of CCK binding by tifluadom was competitive in nature. Tifluadom (1 μM) did not displace 125I-CCK binding to brain tissue or 125I-gastrin binding to fundic glands. In the isolated guinea pig gallbladder, tifluadom antagonized CCK-8 induced contractions with an estimated pA2 of 6.8. These data demonstrate that tifluadom is a peripherally selective CCK antagonist. This unique action could contribute to its reported analgesic and appetite stimulatory properties." @default.
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- W2011647029 date "1986-12-01" @default.
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- W2011647029 title "Tifluadom, a κ-opiate agonist, acts as a peripheral cholecystokinin receptor antagonist" @default.
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- W2011647029 doi "https://doi.org/10.1016/0304-3940(86)90082-0" @default.
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