Fig. 3: The effect of oral (PO) naltrexone dose on opioid receptor blockade within 8 h of administration. | Neuropsychopharmacology

Fig. 3: The effect of oral (PO) naltrexone dose on opioid receptor blockade within 8 h of administration.

From: Opioid antagonism in humans: a primer on optimal dose and timing for central mu-opioid receptor blockade

Fig. 3

The bottom x-axis displays untransformed doses while the top x-axis shows the corresponding log10-transformed doses. The dashed horizontal line indicates full (90%) receptor blockade. MOR blockade (solid black curve) is based on data (black dots) from Rabiner et al. [23] (Table 1). DOR (dot-dashed red curve) and KOR blockade (long-dashed blue curve) were approximated from MOR blockade using the relative receptor affinities of naltrexone (Table S1). Semitransparent bands indicate 95% confidence band (black band), or range based on highest and lowest reported affinity ratio (blue and red bands; Table S1). The estimated ED50 for MOR, DOR and KOR blockade was 5.59 (SE = 0.80); see also [23], 441.83 and 11.19 mg, respectively.

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