Receptor reserve and affinity of mu opioid agonists in mouse antinociception: correlation with receptor binding
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2012, Pharmacology Biochemistry and BehaviorContinuous morphine produces more tolerance than intermittent or acute treatment
2009, Pharmacology Biochemistry and BehaviorReceptor reserve reflects differential intrinsic efficacy associated with opioid diastereomers
2009, Pharmacology Biochemistry and BehaviorIncorporating receptor theory in mechanism-based pharmacokinetic-pharmacodynamic (PK-PD) modeling
2009, Drug Metabolism and PharmacokineticsHydromorphone efficacy and treatment protocol impact on tolerance and μ-opioid receptor regulation
2008, European Journal of PharmacologyCitation Excerpt :Regulation of μ-opioid receptor density is also related to analgesic efficacy, since higher efficacy agonists, but not lower efficacy agonists, are associated with μ-opioid receptor internalization and downregulation both in vivo and in vitro (Keith et al., 1996, 1998; Patel et al., 2002; Stafford et al., 2001; Yoburn et al., 2004; however see Haberstock-Debic et al., 2005). To date, quantitative estimates of analgesic efficacy (i.e., τ) have been confined to a relatively limited group of opioid agonists (e.g., Pawar et al., 2007; Pitts et al., 1998; Walker et al., 1998; Zernig et al., 1995). Furthermore, there are few studies directly examining the relationship between analgesic τ values, in vivo tolerance and μ-opioid receptor regulation (Pawar et al., 2007).