The cardioprotective and antiarrhythmic effects of a selective kappa1-opioid receptor agonist U-50,488 were studied during experimental 45-min total ischemia and 30-min reperfusion of isolated rat heart. The opioid had no effect on the incidence and type of reperfusion arrhythmias. U-50,488 in a concentration of 0.1 microM inhibited reperfusion-induced release of creatine phosphokinase and decreased cAMP concentration in the myocardium by 2 times. These parameters remained unchanged after treatment with U-50,488 in a concentration of 1 microM. The cardioprotective effect of U-50,488 was probably associated with a decrease in cAMP concentration in heart cells. U-50,488 in a concentration of 1 microM produced no cardioprotective effect, which can be explained by its interaction with an unknown non-opioid receptor in cardiomyocytes.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1007/s10517-007-0007-0 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Coexpressed -, -, and -Opioid Receptors Modulate Voltage-Gated Ca Channels in Gastric-Projecting Vagal Afferent Neurons.
Mol Pharmacol
February 2024
Departments of Neural and Behavioral Sciences (H.J.G., S.L.S., L.B.W., G.M.H.) and Anesthesiology and Perioperative Medicine (V.R.-V.), Penn State University College of Medicine, Hershey, Pennsylvania
Opioid analgesics are frequently associated with gastrointestinal side effects, including constipation, nausea, dysphagia, and reduced gastric motility. Though it has been shown that stimulation of opioid receptors expressed in enteric motor neurons contributes to opioid-induced constipation, it remains unclear whether activation of opioid receptors in gastric-projecting nodose ganglia neurons contributes to the reduction in gastric motility and emptying associated with opioid use. In the present study, whole-cell patch-clamp recordings were performed to determine the mechanism underlying opioid receptor-mediated modulation of Ca currents in acutely isolated gastric vagal afferent neurons.
View Article and Find Full Text PDFOpioid receptor activation modulates the calcium current in the cochlear outer hair cells of the rat.
Eur J Neurosci
July 2022
Instituto de Fisiología, Benemérita Universidad Autónoma de Puebla, Puebla, Mexico.
Previous works showed that opioid peptides are produced by olivocochlear efferent neurons, while cochlear hair cells express opioid receptors. It has been proposed that opioids protect the auditory system from damage by intense stimulation, although their use for therapeutic or illicit purposes links to hearing impairment. Therefore, it is relevant to study the effect of opioids in the auditory system to define their functional expression and mechanism of action.
View Article and Find Full Text PDFOxytocin Is a Positive Allosteric Modulator of κ-Opioid Receptors but Not δ-Opioid Receptors in the G Protein Signaling Pathway.
Cells
October 2021
Department of Pain Control Research, The Jikei University School of Medicine, Tokyo 105-8461, Japan.
Oxytocin (OT) influences various physiological functions such as uterine contractions, maternal/social behavior, and analgesia. Opioid signaling pathways are involved in one of the analgesic mechanisms of OT. We previously showed that OT acts as a positive allosteric modulator (PAM) and enhances μ-opioid receptor (MOR) activity.
View Article and Find Full Text PDFQuantification of kappa opioid receptor ligand potency, efficacy and desensitization using a real-time membrane potential assay.
Biomed Pharmacother
November 2021
Department of Pharmacology and Neuroscience, School of Medicine, Creighton University, Omaha, NE, USA.
We explored the utility of the real-time FLIPR Membrane Potential (FMP) assay as a method to assess kappa opioid receptor (KOR)-induced hyperpolarization. The FMP Blue dye was used to measure fluorescent signals reflecting changes in membrane potential in KOR expressing CHO (CHO-KOR) cells. Treatment of CHO-KOR cells with kappa agonists U50,488 or dynorphin [Dyn (1-13)NH] produced rapid and concentration-dependent decreases in FMP Blue fluorescence reflecting membrane hyperpolarization.
View Article and Find Full Text PDFAnalysis of the Illicit Opioid U-48800 and Related Compounds by LC-MS-MS and Case Series of Fatalities Involving U-48800.
J Anal Toxicol
February 2022
Department of Toxicology, The Center for Forensic Science Research and Education (CFSRE), 2300 Stratford Ave, Willow Grove, PA 19090, USA.
We report a method for the detection and quantitation of 12 drugs and 2 metabolites in the same structural class as the illicit mu-opioid agonist U-47700 in human whole blood. These substances are either known or suspected to be present as potential novel opioids in illicit drug markets. The general class of these drugs was developed in pharmaceutical research programs in the 1970s, but these drugs have recently become of concern for overdoses and death in opioid users in the USA and internationally.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!