Bock M G, DiPardo R M, Rittle K E, Evans B E, Freidinger R M, Veber D F, Chang R S, Chen T B, Keegan M E, Lotti V J
J Med Chem. 1986 Oct;29(10):1941-5. doi: 10.1021/jm00160a024.
Seventeen analogues of the selective, competitive cholecystokinin (CCK) antagonist asperlicin 1 were prepared. These compounds were tested as inhibitors of the binding of [125I]CCK to rat pancreas and guinea pig brain receptors. Compounds 4, 7, and 8 were more potent than asperlicin on the pancreatic CCK receptor. One analogue, 17, displayed potency equivalent to asperlicin on the pancreas CCK receptor and showed a marked improvement in aqueous solubility, thereby facilitating the use of this class of CCK antagonists in physiological and pharmacological studies.
制备了17种选择性、竞争性胆囊收缩素（CCK）拮抗剂阿斯匹林1的类似物。这些化合物作为[125I]CCK与大鼠胰腺和豚鼠脑受体结合的抑制剂进行了测试。化合物4、7和8在胰腺CCK受体上比阿斯匹林更有效。一种类似物17在胰腺CCK受体上显示出与阿斯匹林相当的效力，并且在水溶性方面有显著改善，从而便于这类CCK拮抗剂在生理学和药理学研究中的应用。
