European Journal of Pharmacology: Molecular Pharmacology
Pharmacological study of dihydroetorphine in cloned μ-, δ- and κ-opioid receptors
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In vitro profiling of opioid ligands using the cAMP formation inhibition assay and the β-arrestin2 recruitment assay: No two ligands have the same profile
2020, European Journal of PharmacologyCitation Excerpt :This is not surprising, as the GTPγS binding assay reflects events close to the receptor and so is not subject to strong amplification compared with other downstream assays of GPCR signalling (Strange, 2010). At concentrations up to 10 μM, oxycodone and DPDPE were devoid of KOP-receptor agonist activity, mirroring findings by others using cAMP and potassium current functional assays as well as radioligand binding data (Katsumata et al., 1995; Lalovic et al., 2006; Narita et al., 2008; Toll et al., 1998). Fentanyl activated βArr2 recruitment with an EC50 of 0.2 μM at Rluc8-tagged HEK-MOP cells (Fig. 2A, Table 1B).
Prostaglandin EP3 receptor superactivates adenylyl cyclase via the G<inf>q</inf>/PLC/Ca<sup>2+</sup> pathway in a lipid raft-dependent manner
2009, Biochemical and Biophysical Research CommunicationsCitation Excerpt :Measurement of cAMP formation and intracellular Ca2+ mobilization. The cDNAs encoding mouse EP2, EP3β, and FP receptors and rat κ-opioid receptor were subcloned into pcDNA3 as described previously [13,14]. The cDNAs encoding HA-tagged EP2, FLAG-tagged EP3β, myc-tagged wild-type human caveolin-1 (Cav1/WT) and dominant negative caveolin-1 (Cav1/S80E) [15] were constructed.
Abolished thermal and mechanical antinociception but retained visceral chemical antinociception induced by butorphanol in μ-opioid receptor knockout mice
2008, NeuropharmacologyCitation Excerpt :Bmax estimates of receptor densities in these cell lines were 2300 ± 160, 3000 ± 270, and 5000 ± 450 fmol/mg protein, respectively. Binding assays were performed as previously described (Katsumata et al., 1995) with slight modifications. Expressing cells were harvested after 65 h in culture, homogenized in 50 mM Tris buffer (pH 7.4) containing 10 mM MgCl2 and 1 mM EDTA, pelleted by centrifugation for 20 min at 30 000g, and resuspended in the same buffer.
Affinity identification of δ-opioid receptors using latex nanoparticles
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2002, European Journal of PharmacologyTolerance to analgesia and dependence liability by topical application of dihydroetorphine to hairless rats
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