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Methods for anti-addictive narcotic analgesic activity screening

  • US 6,007,986 A
  • Filed: 08/27/1996
  • Issued: 12/28/1999
  • Est. Priority Date: 06/23/1993
  • Status: Expired due to Fees
First Claim
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1. An in vitro assay useful in screening test compounds for effects on opioid μ

  • receptors comprising;

    providing intact cells having opioid μ

    receptors, the receptors being coupled to a cAMP production system under cell growth conditions and including an adenylyl cyclase stimulating agent;

    (1) incubating a first portion of the receptors for about 12 hours or longer with a narcotic analgesic that functions as an agonist therein and forming a constitutively active receptor state;

    (2) removing substantially all of the agonist from the receptor and determining a cAMP value while in the constitutively active state, but being substantially free of agonist molecules;

    (3) determining another cAMP value by measuring cAMP production of a second portion of the receptors while being in the constitutively active state, being substantially free of any agonist molecules, but while being in the presence of naloxone as an inverse agonist to associate naloxone molecules with substantially all the receptors; and

    ,adding a test compound to a third portion of receptors when in a constitutively active receptor state during incubation with narcotic analgesic or after removal thereof to screen for effects of the test compound on opioid μ

    receptor activity and measuring any cAMP changes resulting therefrom.

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