Binding of 3H-β-endorphin to rat brain membranes: Characterization of opiate properties and interaction with ACTH
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Brain effects of melanocortins
2009, Pharmacological ResearchCitation Excerpt :α-MSH is 600 times more potent than desacetyl-α-MSH in inducing grooming [290,291]. In contrast, non-acetylated α-MSH and structurally related ACTH analogs are more potent than acetylated melanocortins in antagonizing opioid binding to their receptors and in attenuating opiate-mediated analgesia [292,293]. Differences in melanocortin receptor affinity for α-MSH and desacetyl-α-MSH are slight or absent [294,295].
Roles of acetylation and other post-translational modifications in melanocortin function and interactions with endorphins
2006, PeptidesCitation Excerpt :α-MSH was far more potent than desacetyl-α-MSH in inducing grooming, and the threshold dose for the latter was 600 times higher than for α-MSH. In contrast, non-acetylated α-MSH and structurally related ACTH analogs are more potent than acetylated melanocortins in attenuating opiate-mediated analgesia and antagonizing opioid receptor binding [3,120]. Also, i.c.v. injection of desacetyl α-MSH selectively increased slow-wave sleep in rats, whereas α-MSH had no effect on any sleep state [17].
No evidence for G-protein-coupled epsilon receptor in the brain of triple opioid receptor knockout mouse
2004, European Journal of PharmacologyCitation Excerpt :Interestingly the existence of epsilon sites was suggested in the rat brain also, on the basis of binding studies. [ 3H]β-Endorphin labeling showed a unique regional distribution (Akil et al., 1980; Goodman et al., 1983; Johnson et al., 1982) and distinct sensitivity to bivalent cations (Law et al., 1979) as compared to other tritiated opioid ligands. Later, studies aiming at characterizing the so-called “benzomorphan sites” in rat brain revealed strong similarities with properties of the epsilon receptor described in the rat vas deferens.
α-Melanotropin hormone inhibits the binding of [<sup>3</sup>H]SCH 23390 to the dopamine D<inf>1</inf> receptor in vitro
1998, European Journal of PharmacologyEvidence for the existence of the β-endorphin-sensitive 'ε-opioid receptor' in the brain: The mechanisms of ε-mediated antinociception
1998, Japanese Journal of Pharmacology