Chang R S, Lotti V J, Chen T B, Keegan M E
Neurosci Lett. 1986 Dec 12;72(2):211-4. doi: 10.1016/0304-3940(86)90082-0.
Tifluadom, a benzodiazepine kappa-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 microM) 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.
