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Naunyn Schmiedebergs Arch Pharmacol. 2004 Nov;370(5):404-13. Epub 2004 Oct 8.

New CCK2 agonists confirming the heterogeneity of CCK2 receptors: characterisation of BBL454.

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Faculté des Sciences Pharmaceutiques et Biologiques, U266 INSERM, FRE 2463CNRS, 4, avenue de l'Observatoire, 75270 Paris Cedex 06, France.


Pharmacological studies were undertaken with a new series of cholecystokinin(2) CCK(2) agonists in order to assign to them a CCK(2A) or CCK(2B) pharmacological profile. The open-field test was chosen as the discrimination test of CCK(2B) agonists. The most interesting agonist, BBL454 (0.03-300 microg/kg) induced hyperactivity which was blocked by a CCK(2) antagonist, the D1 antagonist SCH23390, the delta-opioid antagonist naltrindole, but not a CCK(1) antagonist. All compounds active in the open-field test are characterised by a common structural feature, -COCH(2)CO-Trp-NMeNle-Asp-Phe-NH(2), whereas inactive compounds do not possess such a motive. Therefore, this feature can be considered crucial for CCK(2B) activity. BBL454 (0.03-3 microg/kg) improved memory in a two-trial memory test while it was very weakly active on the peripheral CCK(2) receptor, and did not evoke anxiogenic effects in the plus-maze test. The synthesis of BBL454 is simple, its minimal active dose is 30 ng/kg and no "bell-shaped" responses were observed. These results suggest that BBL454 could be considered to be the new CCK(2B) reference agonist.

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