L-708,474: The C5-cyclohexyl analogue of L-365,260, a selective high affinity ligand for the CCKB/gastrin receptor

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Abstract

The C5-cyclohexyl analogue of the cholecystokinin type-B (CCKB) receptor antagonist L-365,260 has been prepared. This derivative has significantly higher CCKB affinity and markedly improved CCKB/CCKA receptor selectivity (6,500 v. 87-fold) than the parent compound. It is one of the most potent and selective CCKB ligands reported to date.

The synthesis of several C5-cycloalkyl benzodiazepines are described and their affinities for CCK receptors has been determined. The C5-cyclohexyl analogue (L-708,474) is one of the most potent and selective CCKB receptor ligands yet reported.

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