Dextrorphan: an antagonist for phencyclidine receptors.
Radio-binding assay, bioassay and HPLC detection were used to observe the antagonistic effects of dextrorphan on PCP's actions. Dextrorphan displayed high affinity to PCP receptor in the rabbit mesenteric blood vessels. It had weak PCP-like bioactivity, but could antagonize PCP's action dose-dependently in vitro study with the rabbit ear artery preparation and shifted the dose-response curve of PCP to the right. After PCP administration, the content of norepinephrine in the vascular bath medium was increased, which was reversed by dextrorphan. Thus suggests that dextrorphan is an antagonist with very mild agonistic action for PCP receptors.
D000818:Animals; D001808:Blood Vessels / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D003917:Dextrorphan / Q000378:metabolism* / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D007700:Kinetics; D007981:Levorphanol / Q000378:metabolism; D009019:Morphinans / Q000378:metabolism*; D009638:Norepinephrine / Q000378:metabolism; D010622:Phencyclidine / Q000037:antagonists & inhibitors / Q000378:metabolism*; D011817:Rabbits; D011869:Radioligand Assay; D017981:Receptors, Neurotransmitter / Q000187:drug effects / Q000378:metabolism*; D017478:Receptors, Phencyclidine; D014661:Vasoconstriction / Q000187:drug effects
D009019:Morphinans; D017981:Receptors, Neurotransmitter; D017478:Receptors, Phencyclidine; D003917:Dextrorphan; D007981:Levorphanol; D010622:Phencyclidine; D009638:Norepinephrine