Diprotin A, an inhibitor of dipeptidyl aminopeptidase IV(EC 3.4.14.5) produces naloxone-reversible analgesia in rats.

Ronai AZ; Timar J; Mako E; Erdo F; Gyarmati Z; Toth G; Orosz G; Furst S; Szekely JI

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Diprotin A, an inhibitor of dipeptidyl aminopeptidase IV(EC 3.4.14.5) produces naloxone-reversible analgesia in rats.

机译：Diprotin A，一种二肽基氨基肽酶IV（EC 3.4.14.5）的抑制剂，可在大鼠中产生纳洛酮可逆的镇痛作用。

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The dipeptidyl aminopeptidase IV (DP IV) inhibitor Diprotin A produces a full, dose-dependent, short-lasting and naloxone-reversible analgesia in the rat tail-flick test when given intracerebroventricularly, with an ED50 of 295 nmol/rat but it has no direct opioid agonist activity in the longitudinal muscle strip of guinea-pig ileum bioassay. Two of the potential DP IV substrates, morphiceptin and endomorphin 1, identified recently in bovine brain were also analgesic given by similar route. The action of endomorphin 1 was more potent (ED50 = 7.9 nmol/rat) and slightly but significantly more sustained than that of Diprotin A. Diprotin A neither potentiated nor prolonged the effect of a marginally analgesic dose of endomorphin 1. The distinct time course and the lack of potentiation indicate that in the analgesic effect of Diprotin A in rats the protection of a brain Tyr-Pro-peptide other than endomorphin 1 is involved.

机译：当在脑室内进行大鼠甩尾试验时，二肽基氨基肽酶IV（DP IV）抑制剂Diprotin A可产生完全，剂量依赖性，持续时间短且纳洛酮可逆的镇痛作用，ED50为295 nmol /大鼠，但无豚鼠回肠生物测定的纵向肌条中直接的阿片类激动剂活性。最近在牛脑中发现的两种潜在的DP IV底物吗啡肽和内啡肽1也以相似的途径镇痛。内啡肽1的作用比Diprotin A更有效（ED50 = 7.9 nmol /大鼠），并且稍持久，但持续时间更长。DiprotinA既不增强也不延长边缘镇痛剂量的内啡肽1的作用。缺乏增强作用表明，在大鼠中Diprotin A的镇痛作用中，除内啡肽1外还涉及对脑Tyr-Pro-肽的保护。

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来源
《Life sciences》 |1999年第2期|共8页
作者
Ronai AZ; Timar J; Mako E; Erdo F; Gyarmati Z; Toth G; Orosz G; Furst S; Szekely JI;
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正文语种 eng
中图分类生命的起源;生命科学总论;
关键词
Analgesia; Dipeptidyl Peptidases; Naloxone; Oligopeptides; endomorphin-1; 镇痛; 二肽肽酶类; 纳洛酮; 寡肽类;

机译：Analgesia;Dipeptidyl Peptidases;Naloxone;Oligopeptides;endomorphin-1;镇痛;二肽肽酶类;纳洛酮;寡肽类;

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1. Diprotin A, an inhibitor of dipeptidyl aminopeptidase IV(EC 3.4.14.5) produces naloxone-reversible analgesia in rats. [J] . Ronai AZ, Timar J, Mako E, Life sciences . 1999,第2期

机译：Diprotin A，一种二肽基氨基肽酶IV（EC 3.4.14.5）的抑制剂，可在大鼠中产生纳洛酮可逆的镇痛作用。
2. The dipeptidyl peptidase IV (CD26, EC 3.4.14.5) inhibitor vildagliptin is a potent antihyperalgesic in rats by promoting endomorphin-2 generation in the spinal cord. [J] . Kiraly K, Lambeir AM, Szalai J, European Journal of Pharmacology: An International Journal . 2011,第1期

机译：二肽基肽酶IV（CD26，EC 3.4.14.5）抑制剂维格列汀通过促进脊髓内吗啡肽2的生成，是一种有效的抗痛觉过敏药。
3. The dipeptidyl peptidase IV (CD26, EC 3.4.14.5) inhibitor vildagliptin is a potent antihyperalgesic in rats by promoting endomorphin-2 generation in the spinal cord. [J] . Kiraly K, Lambeir AM, Szalai J, European Journal of Pharmacology: An International Journal . 2011,第1期

机译：二肽基肽酶IV（CD26，EC 3.4.14.5）抑制剂维格列汀通过促进脊髓内吗啡肽2的生成，是一种有效的抗痛觉过敏药。
4. Classification analysis using support vector machine, decision tree, and neural network with principal component analysis to determine molecular structure relationship from its biological activity on dipeptidyl peptidase IV inhibitors [C] . Haris Hamzah, Alhadi Bustamam, Arry Yanuar, International Conference on Science and Applied Science . 2020

机译：使用支撑向量机，决策树和神经网络具有主成分分析的分类分析，从而确定二肽基肽酶IV抑制剂的生物活性分子结构关系
5. Screening, Extraction, Isolation and Characterization of a Dipeptidyl Peptidase-IV (DPP-IV) Inhibitor From Ayurvedic and Chinese Herbs [D] . Dai, Fangteng 2018

机译：阿育吠陀和中草药中二肽基肽酶-IV（DPP-IV）抑制剂的筛选，提取，分离和表征
6. Inhibition of dipeptidyl aminopeptidase IV (DP-IV) by Xaa-boroPro dipeptides and use of these inhibitors to examine the role of DP-IV in T-cell function. [O] . G R Flentke, E Munoz, B T Huber, 1991

机译：Xaa-boroPro二肽对二肽基氨基肽酶IV（DP-IV）的抑制作用并使用这些抑制剂来检查DP-IV在T细胞功能中的作用。
7. THE INCREASED RAT AGGRESSIVENESS INDUCED BY NEONATAL EXPOSURE TO THE INHIBITOR OF DIPEPTIDYL PEPTIDASE IV DIPROTIN A REMAINS FOR A LONG TIME [O] . N.N. Khlebnikova, S.D. Shirenova, N.A. Krupina 2019

机译：通过新生儿暴露于二肽肽酶IV Diprotin A抑制剂诱导的大鼠侵袭性仍然长时间

Diprotin A, an inhibitor of dipeptidyl aminopeptidase IV(EC 3.4.14.5) produces naloxone-reversible analgesia in rats.

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