多种神经降压素-（8-13）类似物对麻醉大鼠热诱导性水肿的抑制效力。

Potencies of various neurotensin-(8-13) analogs for inhibition of heat-induced edema in the anesthetized rat.

作者信息

Gao G C, Wei E T

机构信息

School of Public Health, University of California, Berkeley 94720-7360, USA.

出版信息

Regul Pept. 1995 Mar 7;56(1):41-8. doi: 10.1016/0167-0115(95)00004-u.

DOI:10.1016/0167-0115(95)00004-u

PMID:7770632

Abstract

Peptides of the neurotensin (NT) and xenopsin (XP) families inhibit vascular leakage in various models of tissue injury. In this study, we measured the potency of NT fragments, NT analogs and NT-(8-13) analogs for inhibition of thermal edema induced by immersion of the anesthetized rat's paw in 58 degrees C water for 1 min. The pattern of anti-edema potencies seen with sixteen NT-(8-13) analogs correlated well with the pattern of activities obtained in binding measurements to rat brain membrane preparations and to activities in isolated organ preparations. Replacement of Tyr11 with Trp in NT-(8-13) and Arg8 with D-Arg resulted in an analog [D-Arg8, Trp11]NT-(8-13) which was 5-times more potent than NT-(8-13). Substitution of D-Arg for Arg8 and Arg9 in NT-(8-13) produced analogs that retained anti-edema activity but with decreased effects on gut motility and hypotension.

摘要

神经降压素（NT）和异视蛋白（XP）家族的肽类在各种组织损伤模型中可抑制血管渗漏。在本研究中，我们测定了NT片段、NT类似物和NT-(8-13)类似物对麻醉大鼠 paw 浸入58摄氏度水中1分钟所诱导的热水肿的抑制效力。十六种NT-(8-13)类似物的抗水肿效力模式与在大鼠脑膜制剂结合测量中获得的活性模式以及在离体器官制剂中的活性模式密切相关。用Trp取代NT-(8-13)中的Tyr11以及用D-Arg取代Arg8，产生了一种类似物[D-Arg8, Trp11]NT-(8-13)，其效力比NT-(8-13)高5倍。用D-Arg取代NT-(8-13)中的Arg8和Arg9产生的类似物保留了抗水肿活性，但对肠道蠕动和低血压的影响减弱。