(-)U50,488H [(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide] induces internalization and down-regulation of the human, but not the rat, kappa-opioid receptor: structural basis for the differential regulation.

Abstract excerpt

We showed previously that prolonged activation by (-)U50,488H [(trans)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide] led to internalization and down-regulation of the human kappa opioid receptor (hkor), but not the rat kappa opioid receptor (rkor). Herein, we investigated structural determinants in the receptors underlying these differences using chimeric and mutant receptor constructs...

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