Eribis Peptide 94 Mimics Ischemic Preconditioning in Rats with an Acute Myocardial Infarction and has Cardioprotective Effects during Prolonged Ischemia
Journal Title: Journal of Pharmaceutics & Pharmacology - Year 2014, Vol 2, Issue 1
Abstract
Objectives: Previously, we demonstrated that a novel enkephalin analogue, Eribis Peptide 94 (EP94), produces a reduction of myocardial infarct size in rats and pigs administrated during occlusion. Since a complete dose-response relationship and the opioid receptor subtype activated by EP94 was not been clearly established, the following study was undertaken. It was also determined if multiple doses of EP94 could produce greater cardioprotective effects similar to those observed with single versus multiple ischemic preconditioning (IPC) stimuli.Methods: We used adult male Sprague-Dawley rats subjected to either 25 or 40 minutes of coronary occlusion followed by 120 minutes of reperfusion.Key findings: A single and triple bolus of 1 μg/kg of EP94 administered iv prior occlusion produced a reduction of infarct size (IS/AAR) by 39% and 45%, correspondingly. Dose-response relationship has been established. All of the opioid receptor antagonists (naloxone, CTOP, naltrindole, nor-BNI) blocked the effect of EP94.Conclusion: EP94 produces a potent cardioprotective effect in rats following single or multiple injections administrated prior occlusion via effects on μ, δ, and κ opioid receptors. Repeated bolus injections of EP94 produced a reduction of IS/AAR when the ischemic period was increased from 25 to 40 minutes.
Authors and Affiliations
Irina Bobrova
Keywords
Related Articles
- EP ID EP198012
- DOI 10.13188/2327-204X.1000008
- Views 90
- Downloads 0
Mathematical Model of Pharmacokinetic Behavior of Orally Administered Prednisolone in Healthy Volunteers
The objective of the current study was to develop mathematical models that described the pharmacokinetic behavior of prednisolone in healthy subjects after the oral administration of prednisolone. The current study is a...
Prevention of Crystal Formation during Formulation of Acyclovir Powder for Solution for Infusion
Aims and objectives: The main objective of the present work is to develop acyclovir powder for solution for infusion with clear solution upon half sealing and formation of stable cake after freezing drying programme. Dur...
Development of Controlled- Release Solid Dispersion Granules Containing a Poorly Water-Soluble Drug, Porous Calcium Silicate, and the Water-Soluble Polymer Polyvinylpyrrolidone
Objectives: This study sought to develop controlled-release solid dispersion granules containing a poorly water-soluble drug, porous calcium silicate (PCS), and a water-soluble polymer. Methods: Nifedipine (NIF) and ind...
Phytochemical Analysis of Polygonum amplexicaule Essential Oil from Pithoragarh, Uttarakhand, India
Introduction: Polygonum amplexicaule (Polygonaceae) is an herbal drug used to treat fractures, rheumatism, osteoporosis, muscle injuries and pain. It has also been reported to be effective to treat atherosclerosis and it...
Potential Impact of Cyclodextrin-Containing Formulations in Toxicity Evaluation of Novel Compounds in Early Drug Discovery
Cyclodextrins (CDs) are widely used as enabling excipients to improve in vivo drug delivery. The ability of CDs to form inclusion complexes with drugs and thereby improving solubility and stability of drugs is well estab...