Morphine-induced desensitization and down-regulation at mu-receptors in 7315c pituitary tumor cells
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Cited by (68)
Enhancing fentanyl antinociception and preventing tolerance with α-2 adrenoceptor agonists in rats
2024, Behavioural Brain ResearchKey differences in regulation of opioid receptors localized to presynaptic terminals compared to somas: Relevance for novel therapeutics
2023, NeuropharmacologyCitation Excerpt :Since all vlPAG neurons express NOP, NOP agonists directly inhibit vlPAG-RVM output neurons, thus negating actions of opioids on the circuit. Activation of NOP receptors with N/OFQ produces rapid desensitization (Pennock et al., 2012; Pu et al., 1999) and robust receptor internalization (Baiula et al., 2013; Corbani et al., 2004; Donica et al., 2013; Spampinato and Baiula, 2006; Spampinato et al., 2001, 2007). Phosphorylation of NOP by GRK3 results in desensitization, β-arrestin2-recruitment, internalization and arrestin-dependent JNK MAPK signaling (Hawes et al., 1998; Zhang et al., 2012).
Evaluating the expression pattern of the opioid receptor in pituitary neuroendocrine tumors (PitNET) and the role of morphine and naloxone in the regulation of pituitary cell line growth and apoptosis
2023, Biomedicine and PharmacotherapyCitation Excerpt :Notably, concentrations of 0.001–10 µM morphine had no significant effect on GH3 pituitary cell proliferation and survival (data not shown). Regarding the possible effect of morphine on MOR in pituitary tumor cells, a study has shown that concentrations greater than 10 µM morphine can decrease the number of opioid receptors and desensitization [44]. Based on our data, the opioid receptor appeared to be involved in morphine-induced GH3 cell death, however, the aim of this study was not to assess the number of MOR after morphine administration.
Role of receptor internalization in opioid tolerance and dependence
2008, Pharmacology and TherapeuticsChronic morphine treatment up-regulates mu opioid receptor binding in cells lacking filamin A
2007, Brain ResearchCitation Excerpt :Extensive studies in many different cell lines demonstrated MOP down-regulation by different agonists (Baumhaker et al., 1993; Chakrabarti et al., 1995; Kato et al., 1998; Yabaluri and Medzihradsky, 1997). Chronic morphine-induced MOP down-regulation has been well investigated and characterized in a various cell culture systems, such as SH-SY5Y (Zadina et al., 1993), HEK (Onoprishvili et al., 1999), CHO (Kato et al., 1998), C6 (Yabaluri and Medzihradsky, 1997), Neuro2a (Chakrabarti et al., 1995), 7315c (only 20%) (Puttfarcken and Cox, 1989) and SK-N-SH (Baumhaker et al., 1993). Opioid receptor up-regulation by antagonist treatment is a well-established phenomenon in animals and cell cultures.
Internalization and down-regulation of mu opioid receptors by endomorphins and morphine in SH-SY5Y human neuroblastoma cells
2004, Brain ResearchCitation Excerpt :By contrast, the mu opioid receptor has been shown in several systems to be resistant to internalization by morphine [1,8,29,45]. Nevertheless, morphine can induce down-regulation of the mu opioid receptor [4–6,28,42,57,59]. There are several studies that indicate a dissociation between GPCR internalization and down-regulation.
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Present address: Department of Psychiatry, Meyer 4–163, Johns Hopkins University, School of Medicine, 600 N. Wolfe Street, Baltimore, MD 21205.