A number of new 1, 4-benzodiazepin-2-one-based gastrin/CCK-B receptor antagonists related to the archetypal analogue L-365,260, and more closely to the recently reported compound YM022, have been synthesized and evaluated for biological activity. The compounds were screened for their ability to inhibit the binding of [125I] CCK-8 to gastrin/CCK-B receptors prepared from rat brains and that of [3H] L-364,718 to CCK-A ...