Inverse agonists and neutral antagonists at µ opioid receptor (MOR): possible role of basal receptor signaling in narcotic dependence
نویسندگان
چکیده
منابع مشابه
Basal signaling activity of mu opioid receptor in mouse brain: role in narcotic dependence.
Narcotic analgesics cause addiction by poorly understood mechanisms, involving mu opoid receptor (MOR). Previous cell culture studies have demonstrated significant basal, spontaneous MOR signaling activity, but its relevance to narcotic addiction remained unclear. In this study, we tested basal MOR-signaling activity in brain tissue from untreated and morphine-pretreated mice, in comparison to ...
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The mu opioid receptor (MOR, OPRM)--the principal receptor involved in narcotic addiction--has been shown to display basal (spontaneous, constitutive) signaling activity. Interaction with other signaling proteins, such as calmodulin, regulates basal MOR activity. Providing a mechanism for long-lasting regulation, basal MOR activity potentially plays a key role in addiction, in combination with ...
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Cannabinoid receptor agonists, such as Δ(9)-tetrahydrocannabinol (Δ(9)-THC), enhance the antinociceptive effects of μ-opioid receptor agonists, which suggests that combining cannabinoids with opioids would improve pain treatment. Combinations with lower efficacy agonists might be preferred and could avoid adverse effects associated with large doses; however, it is unclear whether interactions b...
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Opioid receptors like other G-protein-coupled receptors undergo specific rearrangements of structure upon activation by agonists. Such processes proceed via several steps ruled by different molecular switches. In order to reveal the first steps of receptor activation concurrent with ligand binding, we investigated μ opioid receptor complexes with antagonists naltrexone and -FNA, and two closely...
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ژورنال
عنوان ژورنال: Journal of Neurochemistry
سال: 2001
ISSN: 0022-3042,1471-4159
DOI: 10.1046/j.1471-4159.2001.00362.x