Short communication
Differential effects of cytochrome P-450 induction on ligand binding to σ receptors

https://doi.org/10.1016/0922-4106(92)90148-OGet rights and content

Abstract

The identity of the σ receptor as a form of cytochrome P-450 was investigated in rats treated with 3-methylcholanthrene or phenobarbital. The density of [3H]N,N′-di(o-toly)guanidine (DTG) binding to σ2 receptors in hepatic subcellular fractions increased following both treatments, while [3H](+)-pentazocine binding to σ1 receptors was unchanged. Furthermore, proadifen and piperonyl butoxide inhibited [3H](+)-pentazocine and [3H]DTG binding with low potency. The low affinity of cytochrome P-450 inhibitors for σ receptors, the similar degree of enhancement of [3H]DTG binding by agents with disparate cytochrome P-450 induction profiles and the lack of change in [3H](+)-pentazocine binding are inconsistent with the identity of the σ receptor as a cytochrome P-450.

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Cited by (13)

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