类蛙皮素样肽对肠道和大脑发挥活性的结构要求

Structural requirements of ceruletide-like peptides for activity on gut and brain.

作者信息

de Castiglione R

出版信息

Peptides. 1981;2 Suppl 2:61-3. doi: 10.1016/0196-9781(81)90012-7.

Abstract

A series of ceruletide analogues were tested in order to evaluate the structural requirements for activity on gut and brain. The effects studied were: contraction of the guinea pig gallbladder and stimulation of the exocrine pancreatic secretion in the dog after intravenous (IV) administration, for activity on the gut; analgesia (hot plate test) and sedation (reduction of spontaneous rearing activity) in mice by subcutaneous (SC) route, for activity on the brain. The structural requirements were roughly the same for central and peripheral activities. Possible mechanisms for the antinociceptive effects of ceruletide in humans were proposed.

摘要

为了评估对肠道和大脑产生作用的结构要求，对一系列蛙皮素类似物进行了测试。所研究的效应包括：静脉注射（IV）后豚鼠胆囊收缩以及犬外分泌性胰腺分泌的刺激，用于评估对肠道的作用；皮下注射（SC）后小鼠的镇痛作用（热板试验）和镇静作用（自发竖毛活动减少），用于评估对大脑的作用。中枢和外周活性的结构要求大致相同。提出了蛙皮素在人体内产生抗伤害感受作用的可能机制。