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S(-)和R(+)舒必利、甲氧氯普胺、西沙必利和多潘立酮对小肠的作用表明,多巴胺2型(DA2)受体参与大鼠小肠转运时间的控制。

The effects of S(-) and R(+) sulpiride, metoclopramide, cisapride and domperidone on the small intestine suggest DA2-receptors are involved in the control of small intestinal transit time in rats.

作者信息

Zuccato E, Bertolo C, Salomoni M, Forgione A, Mussini E

机构信息

Istituto di Ricerche Farmacologiche Mario Negri, Milano, Italy.

出版信息

Pharmacol Res. 1992 Sep;26(2):179-85. doi: 10.1016/s1043-6618(05)80131-8.

Abstract

To study the effect of intraperitoneal S(-)sulpiride (1-15 mg/kg), R(+)sulpiride (5-10 mg/kg), metoclopramide (1-15 mg/kg), cisapride (10 mg/kg) and domperidone (5-10 mg/kg) on intestinal progression, rats were given the test drug followed by oral lactulose. Their hydrogen excretion was used to calculate the small bowel transit time (SBTT) and maximum peak time (MPT). Metoclopramide (7.5 mg/kg) had the greatest effect on SBTT (-25%), followed by S(-)sulpiride and domperidone. S(-)sulpiride (10 mg/kg) had the greatest activity on the MPT (-35.2%) followed by metoclopramide. R(+)sulpiride and cisapride did not modify SBTT and MPT. In conclusion S(-)sulpiride is the isomer active on intestinal transit and DA2-receptors seem important targets in the modulation of intestinal progression, since S(-)sulpiride, metoclopramide and domperidone are DA2-receptor antagonists, and R(+)sulpiride and cisapride are not. The H2 breath test proved a valid method for measuring the effect of drugs on the small intestine in animals.

摘要

为研究腹腔注射S(-)舒必利(1 - 15毫克/千克)、R(+)舒必利(5 - 10毫克/千克)、甲氧氯普胺(1 - 15毫克/千克)、西沙必利(10毫克/千克)和多潘立酮(5 - 10毫克/千克)对肠道蠕动的影响,给大鼠注射受试药物后口服乳果糖。通过它们呼出氢气量来计算小肠通过时间(SBTT)和最大峰值时间(MPT)。甲氧氯普胺(7.5毫克/千克)对SBTT影响最大(-25%),其次是S(-)舒必利和多潘立酮。S(-)舒必利(10毫克/千克)对MPT活性影响最大(-35.2%),其次是甲氧氯普胺。R(+)舒必利和西沙必利对SBTT和MPT无影响。总之,S(-)舒必利是对肠道转运有活性的异构体,DA2受体似乎是调节肠道蠕动的重要靶点,因为S(-)舒必利、甲氧氯普胺和多潘立酮是DA2受体拮抗剂,而R(+)舒必利和西沙必利不是。氢气呼气试验证明是一种测量药物对动物小肠作用的有效方法。

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