Abstract
The electrophysiological effects of Boc- D-Asp-Tyr(SO 3H)-Nle-D-Lys -Trp-Nle-Asp-Phe-NH 2 (compound I) and Boc-γ-D- Glu-Tyr(SO 3H)-Nle-D-Lys -Trp-Nle-Asp-Phe-NH 2 (compound II), two cyclic cholecystokinin analogs with high selectivity for CCK-B receptors, as well as the effects of the linear enzyme-resistant analog Boc-[Nle 28,Nle 31]-CCK7 (BDNL), were compared with those of CCK8 using extracellular recordings in rat hippocampal slices in vitro. Bath applications of the three synthetic compounds resulted in concentration-dependent and reversible increases in single-unit activity. Comparison of equieffective concentrations yielded the following potency rank order: BDNL > CCK8 > compound II > compound I. There was a close correlation (r=.96, slope=0.98) between the excitatory activities of the analogs and their potencies in displacing radiolabelled CCK8 from CCK-B receptors on rat brain membranes.
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