L-743,345 - THE C5-(3-AZABICYCLO[3.2.2.]NONAN-3-YL) ANALOG OF DEVAZEPIDE, A SELECTIVE, HIGH-AFFINITY ANTAGONIST FOR THE CHOLECYSTOKININ-A RECEPTOR

Recent knowledge that replacement of the CS-phenyl group in a series o f 1,4-benzodiazepines by CS-aza(bi)cycloalkyl groups gave high affinit y, selective, water-soluble CCKB/gastrin receptor antagonists has been extended to the CCKA receptor subtype. This communication describes t he synthesis and in vitro biological profile of L-743,345 -1,4-benzodi azepin-3-yl)-1H-indole-2-carboxamide), a selective and high affinity l igand for the CCKA receptor. Single crystal x-ray crystallography conf irmed the absolute configuration to be 3S, the same as Devazepide.