Synthesis and Infarction-Limiting Properties of Peptide Agonists of Opioid Receptors


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Three structurally different peptide agonists of opioid receptors, i.e., gludalan, deltolei, and dalargin, were synthesized and assessed for infarction-limiting effects in rats with coronary occlusion (45 min) and reperfusion (2 h). The opioid peptides dalargin and gludalan (0.1 mg/kg) and deltolei (0.03, 0.1, and 0.2 mg/kg) were injected 5 min before reperfusion. It was found that gludalan and deltolei at a dose of 0.1 mg/kg decreased the ratio of infarction size to the area at risk (IS/AAR) whereas dalargin did not affect the IS. The infarction-limiting effect of deltolei disappeared if the peptide dose was decreased (0.03 mg/kg) or increased (0.2 mg/kg). The opioid receptor antagonists naltrexone (5 mg/kg) or naloxone methiodide (5 mg/kg), which does not penetrate the blood—brain barrier, eliminated the infarction-limiting effect of gludalan.

作者简介

S. Tsibul’nikov

Cardiology Research Institute, Tomsk National Research Medical Center

Email: chem@folium.ru
俄罗斯联邦, Tomsk, 634009

A. Mukhomedzyanov

Cardiology Research Institute, Tomsk National Research Medical Center

Email: chem@folium.ru
俄罗斯联邦, Tomsk, 634009

L. Maslov

Cardiology Research Institute, Tomsk National Research Medical Center

Email: chem@folium.ru
俄罗斯联邦, Tomsk, 634009

M. Ovchinnikov

Peptide Synthesis Company

Email: chem@folium.ru
俄罗斯联邦, Moscow, 121552

M. Sidorova

Peptide Synthesis Company

Email: chem@folium.ru
俄罗斯联邦, Moscow, 121552

E. Kudryavtseva

Peptide Synthesis Company

Email: chem@folium.ru
俄罗斯联邦, Moscow, 121552

Yu. Bushov

Tomsk State University

Email: chem@folium.ru
俄罗斯联邦, Tomsk, 634050

Yu. Lishmanov

Cardiology Research Institute, Tomsk National Research Medical Center

Email: chem@folium.ru
俄罗斯联邦, Tomsk, 634009

I. Khaliulin

University of Bristol

Email: chem@folium.ru
英国, Bristol, BS8 1TH

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