Iwatsuki K, Horiuchi A, Yonekura H, Haruta K, Homma N, Chiba S
Department of Pharmacology, Shinshu University School of Medicine, Matsumoto, Japan.
Jpn J Pharmacol. 1989 Jan;49(1):77-82. doi: 10.1254/jjp.49.77.
The effects of DN-9693, a synthesized phosphodiesterase inhibitor, on the secretion of pancreatic juice were investigated in preparations of the isolated and blood-perfused dog pancreas. DN-9693 injected intraarterially caused a dose-dependent increase in the secretion of pancreatic juice and decrease in the perfusion pressure. The threshold doses to increase the pancreatic secretion and to decrease the perfusion pressure were about 100 micrograms and 1 microgram, to decrease the perfusion pressure were about 100 micrograms and 1 micrograms, respectively. Thus, the secretory response was less effective than the vascular response. The secretory activity of DN-9693 (0.3 mg) was approximately equal to that of 0.03 mg of 3-isobutyl-1-methylxanthine, 0.5 mg of papaverine, 5 mg of theophylline, 0.08 0.5 mg of papaverine, 5 mg of theophylline, 0.08 units of secretin and 0.2 units of cholecystokinin. The concentration of bicarbonate in the pancreatic juice induced by DN-9693 was increased, but protein concentration was not. DN-9693-induced pancreatic secretion was not modified by pretreatments with phentolamine, propranolol, atropine, sulpiride and cimetidine. Secretin-induced pancreatic secretion was significantly potentiated by infusion of DN-9693 (10 micrograms/min), but cholecystokinin-induced one was not. From these results, it is concluded that DN-9693 may produce an increase in pancreatic secretion by acting directly on the pancreatic exocrine gland of the dog, which might be mediated through an increase of intracellular cyclic AMP concentration by inhibiting phosphodiesterase activity.
在离体且有血液灌注的犬胰腺标本中,研究了合成的磷酸二酯酶抑制剂DN - 9693对胰液分泌的影响。动脉内注射DN - 9693可引起胰液分泌呈剂量依赖性增加以及灌注压降低。增加胰液分泌和降低灌注压的阈剂量分别约为100微克和1微克。因此,分泌反应比血管反应的效果要弱。DN - 9693(0.3毫克)的分泌活性大约等同于0.03毫克的3 - 异丁基 - 1 - 甲基黄嘌呤、0.5毫克的罂粟碱、5毫克的茶碱、0.08单位的促胰液素和0.2单位的缩胆囊素。DN - 9693诱导的胰液中碳酸氢盐浓度升高,但蛋白质浓度未升高。用酚妥拉明、普萘洛尔、阿托品、舒必利和西咪替丁预处理不会改变DN - 9693诱导的胰腺分泌。输注DN - 9693(10微克/分钟)可显著增强促胰液素诱导的胰腺分泌,但对缩胆囊素诱导的胰腺分泌则无此作用。从这些结果可以得出结论,DN - 9693可能通过直接作用于犬的胰腺外分泌腺来增加胰腺分泌,这可能是通过抑制磷酸二酯酶活性增加细胞内环磷酸腺苷浓度来介导的。