Antiarrhythmic action of naloxone: Direct, non-opiate effect on the rat heart

Sarne, Yosef; Hochman, Ilan; Eshed, M.; Oppenheimer, Edna

doi:10.1016/0024-3205(88)90513-9

Cited by 19 publications

(10 citation statements)

References 12 publications

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“…In our present model, as well as in our previous studies on adrenaline-induced arrhythmia (Sarne et al, 1988) and ouabain-induced arrhythmia (Sarne et al, unpublished observations), the antiarrhythmic activity of opiates was not stereospecific. Parratt & Sitsapesan (1986), on the other hand, observed some stereospecificity, albeit much lower than expected for opioid receptors.…”

Section: Discussionsupporting

confidence: 80%

“…This hypothesis was supported by our finding (Sarne et al, 1988) that (+)-naloxone, which is 1000-10,000 less potent as an opioid antagonist (Iijima et al, 1978) is equipotent as an antiarrhythmic agent. We decided to verify the results of our previous study which was carried out on adrenaline-induced arrhythmia, by testing it with the more conventional, coronary occlusion model used by Parrat & Sitsapesan.…”

Section: Discussionsupporting

confidence: 60%

See 1 more Smart Citation

Anti‐arrhythmic activities of opioid agonists and antagonists and their stereoisomers

Sarne¹,

Flitstein²,

Oppenheimer³

1991

British J Pharmacology

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1 A series of opioid agonists, antagonists and their (+)-stereoisomers were tested for antiarrhythmic activity in the rat coronary artery occlusion model. 2 Naloxone (0.01-2mgkg-') significantly reduced the incidence and severity of cardiac arrhythmias, in accordance with previous published studies. 3 The non-opioid stereoisomer, (+)-naloxone, was equipotent with naloxone against occlusion-induced arrhythmia. 4 Similar non-stereospecific antiarrhythmic effects were induced by another opioid antagonist, Win 44,441-3 and its stereoisomer Win 44,441-2. 5 The opioid agonists, morphine and levorphanol, protected against occlusion-induced arrhythmia as did the opioid antagonists, and the (+ )-stereoisomer, dextrorphan, was equipotent to levorphanol. 6 It is concluded that the antiarrhythmic effects of opioid drugs are not mediated by opioid receptors. A direct effect on ionic currents in cardiac muscle is suggested as the mechanism of opioid antiarrhythmic activity.

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Section: Discussionsupporting

confidence: 80%

Section: Discussionsupporting

confidence: 60%

Anti‐arrhythmic activities of opioid agonists and antagonists and their stereoisomers

Sarne¹,

Flitstein²,

Oppenheimer³

1991

British J Pharmacology

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show abstract

“…The determination of opioid receptor binding affinity for the active enantiomer, (−)-naloxone, range between 0.56 and 4.9 nM for and receptors [44]. When the stereoisomer, (+)-naloxone (with an opioid potency ∼1000-10,000 times less than that of (−)-naloxone) was used, it produced comparable antiarrhythmic activity [17,45]. The authors conclude that non-opioid pharmacological activity reduced arrhythmia incidence.…”

Section: Discussionmentioning

confidence: 97%

“…Other studies [8,16,17] suggest that these effects of naloxone are not mediated by interactions with opioid receptors. Instead, naloxone has direct effects on the heart [18] due to blockade of cardiac ion channels [19,20] similar to the effects of naloxone observed on Na and K currents in guinea pig atria [21] and morphine in the squid giant axon [22,23].…”

Section: Introductionmentioning

confidence: 94%

Ventricular arrhythmia incidence in the rat is reduced by naloxone

Hayes

Wang

Walker

2015

Pharmacological Research

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“…Opioid receptors have been implicated in the genesis of arrhythmias due to myocardial ischemia [1–4], and a variety of experiments involving the use of both agonist and antagonist opiates have been used to support such claims [3–10]. However, one complication in the use of such drugs is that many also have ancillary pharmacological actions unrelated to opioid receptors.…”

Section: Introductionmentioning

confidence: 99%