The presence of mu-, delta-, and kappa-opioid receptors in human heart tissue (2024)

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The differential effects of a selective kappa-opioid receptor agonist, u50488, in Guinea pig heart tissues

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Chi-Feng Hung

The differential effects of a selective kappa- (κ-) opioid receptor agonist, U50488, were elucidated by monitoring the contraction of isolated guinea pig atrial and ventricular muscles. In electrically driven left atria, U50488 in nanomolar concentration range decreased the contractile force. Norbinaltorphimine (norBNI), a selective κ-receptor antagonist, and pertussis toxin (PTX) abolished the negative inotropic effect of U50488. In contrast, the inhibitory effect was not affected by the pretreatment of atropine or propranolol. Even though U50488 exerted a negative inotropic effect in the left atrium, it did not affect the contractile force of the right atrium and ventricles paced at 2 Hz. Similarly, the beating rate of the spontaneously beating right atrium was also unaffected by U50488. These results indicate that the activation of κ-opioid receptors can only produce negative inotropic effect in left atria via activation of PTX-sensitive G protein in guinea pigs. The absence of n...

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American Journal of Physiology-Heart and Circulatory Physiology

Mediating δ-opioid-initiated heart protection via the β2-adrenergic receptor: role of the intrinsic cardiac adrenergic cell

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Michael Hughes

Stimulation of cardiac β2-adrenergic receptor (β2-AR) or δ-opioid receptor (DOR) exerts a similar degree of cardioprotection against myocardial ischemia in experimental models. We hypothesized that δ-opioid-initiated cardioprotection is mediated by the intrinsic cardiac adrenergic (ICA) cell via enhanced epinephrine release. Using immunohistochemical and in situ hybridization methods, we detected in situ tyrosine hydroxylase (TH) mRNA and TH immunoreactivity that was colocalized with DOR immunoreactivity in ICA cells in human and rat hearts. Western blot analysis detected DOR protein in ICA cells isolated from rat ventricular myocytes. The physiology of DOR expression was examined by determining changes of cytosolic Ca2+ concentration ([Ca2+]i) transients in isolated rat ICA cells using fluorescence spectrophotometry. Exposing the selective δ-opioid agonist d-[Pen2,5]enkephalin (DPDPE) to ICA cells increased [Ca2+]i transients in a concentration-dependent manner. Such an effect was ...

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Journal of The American College of Cardiology

Delta opioid receptor stimulation mimics ischemic preconditioning in human heart muscle

2000 •

Asha Patel

OBJECTIVESThe objective of this study was to examine whether the delta (δ) opioid receptor isoform is expressed in the human heart and whether this receptor improves contractile function after hypoxic/reoxygenation injury.BACKGROUNDDelta opioid receptor agonists mimic preconditioning (PC) in rat myocardium, corresponding to known cardiac δ opioid receptor expression in this species.METHODSThe messenger RNA transcript encoding the δ opioid receptor was identified in human atria and ventricles. To evaluate the cardioprotective role of the opioid receptor, human atrial trabeculae from patients undergoing coronary bypass grafting were isolated and superfused with Tyrode’s solution. A control group underwent 90 min of simulated ischemia and 120 min of reoxygenation. A second group was preconditioned with 3 min simulated ischemia and 7 min reoxygenation. Additional groups included: superfusion with the δ receptor agonist (DADLE) (10 nM), with the δ receptor antagonist naltrindole (10 nM) and with the mitochondrial KATP channel blocker 5-hydroxydecanoate (5HD) (100 μM) either with or without PC, respectively. A final group was superfused with 5HD before DADLE. The end point used was percentage of developed force after 120 min of reoxygenation.RESULTSResults, expressed as means ± SEM, were: control = 32.6 ± 3.8%; PC = 50.5% ± 1.8∗; DADLE = 46.0 ± 3.9%∗; PC + naltrindole = 25.5 ± 3.9%; naltrindole alone = 25.5 ± 4.3%; 5HD + PC = 28.9 ± 7.4%; 5HD alone = 24.1 ± 3.0%; 5HD + DADLE = 26.9 ± 4.4% (∗p < 0.001 vs. controls).CONCLUSIONSHuman myocardium expresses the δ opioid receptor transcript. Stimulation of this receptor appears to protects human muscle from simulated ischemia, similar to PC, and via opening of the mitochondrial KATP channel.

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British Journal of Pharmacology

Peripheral sympatho-inhibitory cardiovascular effects of opioid peptides in anaesthetized rabbits

1988 •

Bela Szabo

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Journal of Neurophysiology

Glycinergic Inputs to Cardiac Vagal Neurons in the Nucleus Ambiguus Are Inhibited by Nociceptin and -Selective Opioids

2003 •

Priya Venkatesan

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The presence of mu-, delta-, and kappa-opioid receptors in human heart tissue (2024)
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