The cardiovascular responses to mu opioid agonist and antagonist in conscious normal and obese rats

Hill-Pryor, Crystal; Lindsey, D. C.; Lapanowski, Karen; Dunbar, Joseph C.

doi:10.1016/j.peptides.2005.10.012

Cited by 6 publications

(5 citation statements)

References 14 publications

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“…At this dose, there was also an increase in heart rate and blood pressure most likely due to the concurrent incidence of nausea and vomiting. It is, however, possible that these changes could be linked to antagonism of μ‐opioid receptors in specific brain areas associated with cardiovascular control, although the exact mechanisms have not been identified 46 , 47 . Although the 100‐mg dose was considered to be the highest well‐tolerated dose based on the adverse event profile, the dose range predicted to be clinically effective (between 5 and 25 mg) is approximately 4‐ to 20‐fold lower and hence expected to have a good tolerability profile with minimal effects on fatigue, alertness, and mood.…”

Section: Discussionmentioning

confidence: 99%

Opioid Receptor Modulation of Hedonic Taste Preference and Food Intake: A Single‐Dose Safety, Pharmacokinetic, and Pharmacodynamic Investigation With GSK1521498, a Novel μ‐Opioid Receptor Inverse Agonist

Nathan

O’Neill

Bush³

et al. 2012

The Journal of Clinical Pharma

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Endogenous opioids and µ-opioid receptors have been linked to hedonic and rewarding aspects of palatable food intake. The authors examined the safety, pharmacokinetic, and pharmacodynamic profile of GSK1521498, a µ-opioid receptor inverse agonist that is being investigated primarily for the treatment of overeating behavior in obesity. In healthy participants, GSK1521498 oral solution and capsule formulations were well tolerated up to a dose of 100 mg. After single doses (10-150 mg), the maximum concentration (C(max)) and area under the curve (AUC) in plasma increased in a dose-proportional manner. GSK1521498 selectively reduced sensory hedonic ratings of high-sugar and high-fat dairy products and caloric intake of high-fat/high-sucrose snack foods. These findings provide encouraging data in support of the development of GSK1521498 for the treatment of disorders of maladaptive ingestive behavior or compulsive consumption.

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Section: Discussionmentioning

confidence: 99%

Opioid Receptor Modulation of Hedonic Taste Preference and Food Intake: A Single‐Dose Safety, Pharmacokinetic, and Pharmacodynamic Investigation With GSK1521498, a Novel μ‐Opioid Receptor Inverse Agonist

Nathan

O’Neill

Bush³

et al. 2012

The Journal of Clinical Pharma

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“…2 ) may be suggested as the possible mechanisms for this role. Previous studies have demonstrated that some opioid receptors (µ-type) mediate a pressor response [13, 14], while other receptors (κ-type) mediate a depressor response [13]. Fontana et al .…”

Section: Discussionmentioning

confidence: 99%

The Effect of Passive Opium Smoking on Cardiovascular Indices of Rabbits with Normal and Ischemic Hearts

Joukar¹,

Najafipour²,

Afshar³

et al. 2010

TOCMJ

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Some Asian people believe that opium can protect the cardiovascular system. To assess this belief, we investigated the effect of passive opium smoking (POS) on cardiovascular indices in rabbits with ischemic and non-ischemic hearts.Rabbits (n = 43) were divided into control (CTL), short term opium (SO) and long term opium (LO) groups. SO and LO groups were exposed to opium smoking for 3 days and 4 weeks, respectively. ECG, blood pressure (BP), left ventricular pressure and cardiac troponin I levels were recorded. Isoproterenol (ISO) was injected to induce cardiac ischemia and after 4 h the above variables were measured along with cardiac histopathology assessment.All groups showed significant increments in troponin I level (P < 0.05) except the CTL group. This trend was more obvious in ISO-treated groups. Mean arterial pressure (MAP) significantly decreased in all groups (p< 0.05) except the LO group. Opium exposure attenuated ISO-induced myodegeneration but augmented tissue congestion and hemorrhage.In conclusion, higher troponin I serum level and ECG changes were found in passive opium smoking groups. This evidence is against the belief that opium can protect the cardiovascular system.

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“…The initial pathophysiology of arrhythmia is related to dysfunction in the conduction system. Opioid receptors in the ventricles and atria may play an essential role in the development of different arrhythmias [87,88] by increasing heart rate and causing changes in heart rhythm [89,90]. It has also been claimed that the μ-1 opioid receptor causes tachycardia, and μ-2 causes bradycardia [91].…”

Section: Potential Mechanismsmentioning

confidence: 99%

The effects of opium on the cardiovascular system: a review of side effects, uses, and potential mechanisms

Nakhaee

Ghasemi

Karimzadeh

et al. 2020

Subst Abuse Treat Prev Policy

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Background: In Iran, as in many other Asian and Middle Eastern countries, some believe that opium has beneficial effects on cardiovascular system. Dependent patients suppose that opium has positive effects on cardiovascular function and can prevent or improve cardiovascular diseases; however, only few comprehensive studies evaluating such effects have been performed. Objectives: In this study, we sought to clarify the effect of opium on cardiovascular problems by incorporating the previous findings and the current information on the issue and to explain the possible mechanisms of this effect. Methods: The available human studies published up to October 30, 2019, were searched in different databases. Case-control, cohort, and cross-sectional studies were retrieved. Papers published in English or those with an English abstract were included. The risk of bias for each included study was assessed based on the Newcastle-Ottawa Scale (NOS). We then categorized the effects of opium on cardiovascular problems along with its probable underlying mechanisms of action. Results: In this study, most of the published articles suggested the adverse effects of opium on the cardiovascular system, including atherosclerosis, myocardial infarction, arrhythmia, low ejection fraction, and cardiovascular mortality; however, some articles reported the beneficial or impartial effects of opium on the cardiovascular system. In this article, we have categorized all the effects of opium on cardiovascular system; also, the proposed mechanisms of action of opium in each of the above-mentioned disorders are summarized. Conclusion: Although the available evidences were incoherent, it was mostly suggested that opium use does not protect against or improve cardiovascular problems.

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The cardiovascular responses to mu opioid agonist and antagonist in conscious normal and obese rats

Cited by 6 publications

References 14 publications

Opioid Receptor Modulation of Hedonic Taste Preference and Food Intake: A Single‐Dose Safety, Pharmacokinetic, and Pharmacodynamic Investigation With GSK1521498, a Novel μ‐Opioid Receptor Inverse Agonist

Opioid Receptor Modulation of Hedonic Taste Preference and Food Intake: A Single‐Dose Safety, Pharmacokinetic, and Pharmacodynamic Investigation With GSK1521498, a Novel μ‐Opioid Receptor Inverse Agonist

The Effect of Passive Opium Smoking on Cardiovascular Indices of Rabbits with Normal and Ischemic Hearts

The effects of opium on the cardiovascular system: a review of side effects, uses, and potential mechanisms

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