Different Types of Steroids Inhibit [3H]DIPRENORPHINE (cas 14357-78-9) Binding in Mouse Brain Membranes

Add time:08/09/2019    Source:sciencedirect.com

1.The binding of 60 drugs, mainly steroids, to opioid receptors was studied in crude membrane fractions from mouse brains.2.Competition assays with the different drugs (5×10−7–10−4M) were performed by labeling opiate receptors with [3H]diprenorphine (0.3–0.4 nM).3.Only 7 drugs (α,5β-tetrahydrodeoxycorticosterone, megestrol acetate, mifepristone, 17α-ethynylestradiol, diethylstilbestrol, clomiphene citrate and tamoxifen citrate) inhibited [3H]diprenorphine binding more than 50% at the highest concentration assayed (10−4 M). The IC50 values ranged between 6×10−5 M.4.Thus, the present results show that only a limited number of steroids, from diverse classes, bind to opiate receptors.

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