Effects of KSG-504, a New Cholecystokinin-A-Receptor Antagonist, on Pancreatic Exocrine and Endocrine Secretions in Rats

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概要

• 論文の詳細を見る

• The effects of KSG-504 ((<I>S</I>)-arginium (<I>R</I>)-4-[<I>N</I>-(3-methoxypropyl)-<I>N</I>-pentylcarbamoyl]-5-(2naphthylsulfonyl) pentanoate monohydrate), a new cholecystokinin (CCK)-A-receptor antagonist, on pancreatic exocrine secretion in anesthetized rats and endocrine secretion in conscious rats were studied. Intravenous injection of KSG-504 inhibited the pancreatic amylase output stimulated by intravenous infusion of CCK-8 in a dose-dependent manner (ED<SUB>50</SUB>: 18 μg/kg/min). Moreover, KSG-504 significantly reduced the CCK-8-stimulated increases in pancreatic juice volume and outputs of protein, trypsin and lipase. Intraduodenal infusion of casein increased the plasma CCK concentration and the pancreatic amylase output. KSG-504 significantly inhibited the pancreatic amylase output stimulated by casein. Pancreatic juice volume and bicarbonate output were significantly stimulated by intravenous infusion of secretin, but were not changed by KSG-504. When pancreatic exocrine secretion was stimulated by secretin plus CCK-8, KSG-504 suppressed the increases in juice volume and bicarbonate output to the level stimulated by secretin alone. Basal pancreatic amylase output was decreased by KSG-504. KSG-504 decreased the level of plasma immunoreactive insulin (IRI) stimulated by glucose plus CCK-8, but had no effect on IRI stimulated by glucose alone and the basal IRI. These in vivo studies suggest that KSG-504 has significant inhibitory effects both on the pancreatic exocrine and endocrine secretion stimulated by CCK, but has no effect on the exocrine secretion stimulated by secretin.

• 社団法人 日本薬理学会の論文
• 1996-02-01

著者

• Yamazaki Yoshinobu

  Division Of Discovery Research Central Research Laboratory Kissei Pharmaceutical Co. Ltd

• Yamazaki Yoshinobu

  Central Research Laboratory Kissei Pharmaceutical Co. Ltd.

• TAKEDA Hiroo

  Division of Discovery Research, Central Research Laboratory, Kissei Pharmaceutical Co., Ltd

• AKAHANE Masuo

  Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,

• KOBAYASHI Mamoru

  Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,

• TAKEDA Hiroo

  Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,

• AJISAWA Yukiyoshi

  Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.,

• Takeda Hiroo

  Division Of Discovery Research Central Research Laboratory Kissei Pharmaceutical Co. Ltd

• Akahane M

  Kissei Pharmaceutical Co. Ltd. Nagano Jpn

• Ajisawa Yukiyoshi

  Central Research Laboratories Kissei Pharmaceutical Co. Ltd.

• Kobayashi Mamoru

  Central Research Laboratories Kissei Pharmaceutical Co. Ltd.

• AKAHANE Masuo

  Central Research Laboratories, Kissei Pharmaceutical Co., Ltd.

関連論文

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• Characterization of β-Adrenoceptor Subtype in Bladder Smooth Muscle in Cynomolgus Monkey
• Effects of KSG-504, a New Cholecystokinin-A-Receptor Antagonist, on Pancreatic Exocrine and Endocrine Secretions in Rats
• Cholecystokinin - A Specific Antagonism of KSG - 504 to Chlecystokinin Receptor Binding and Pancreatic Secretion in Mammals
• Effects of ritodrine hydrochloride, a beta2-adrenoceptor stimulant, on uterine motilities in late pregnancy.

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