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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Tifluadom, a kappa-opiate agonist, acts as a peripheral cholecystokinin receptor antagonist.

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.[1]

References

  1. Tifluadom, a kappa-opiate agonist, acts as a peripheral cholecystokinin receptor antagonist. Chang, R.S., Lotti, V.J., Chen, T.B., Keegan, M.E. Neurosci. Lett. (1986) [Pubmed]
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