Ninomiya K, Saito T, Wakatsuki K, Saeki M, Kato T, Edano K, Kasai H, Kimura K, Fujii M
Pharmacological Research Laboratory, Tokyo Tanabe Co., Ltd., Japan.
Arzneimittelforschung. 1998 Jan;48(1):55-7.
The effects of loxiglumide (CAS 107097-80-3, CR 1505), a novel cholecystokinin-A(CCK-A) receptor antagonist, on pancreatic exocrine secretion stimulated by meal were examined in conscious dogs with chronic pancreatic fistula. Pancreatic exocrine secretion was stimulated by intraduodenal infusion of a liquid test meal and postprandial plasma CCK levels were apparently elevated. Loxiglumide inhibited the meal-stimulated outputs of pancreatic protein, amylase and bicarbonate at an intravenous dose of 10 mg/kg/h (p < 0.05). However, loxiglumide did not show apparent inhibition of pancreatic juice volume and trypsin output. These results show that the selective CCK-A antagonist loxiglumide may inhibit the increase of pancreatic exocrine secretion based on selective blockade of receptor binding of CCK endogenously induced by meal in dogs.
在患有慢性胰瘘的清醒犬中，研究了新型胆囊收缩素A（CCK-A）受体拮抗剂洛昔谷胺（CAS 107097-80-3，CR 1505）对进食刺激的胰腺外分泌的影响。通过十二指肠内输注液体试验餐刺激胰腺外分泌，餐后血浆CCK水平明显升高。静脉注射剂量为10mg/kg/h时，洛昔谷胺抑制了进食刺激的胰腺蛋白质、淀粉酶和碳酸氢盐的分泌量（p<0.05）。然而，洛昔谷胺对胰液量和胰蛋白酶分泌量没有明显抑制作用。这些结果表明，选择性CCK-A拮抗剂洛昔谷胺可能通过选择性阻断犬进食内源性诱导的CCK受体结合来抑制胰腺外分泌的增加。
