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OtherANALGESIA AND DRUGS OF ABUSE

Ibuprofen Inhibits Rat Brain Deamidation of Anandamide at Pharmacologically Relevant Concentrations. Mode of Inhibition and Structure-Activity Relationship

Christopher J. Fowler, Gunnar Tiger and Anders Stenström
Journal of Pharmacology and Experimental Therapeutics November 1997, 283 (2) 729-734;
Christopher J. Fowler
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Gunnar Tiger
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Anders Stenström
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Abstract

The ability of rat brain (minus cerebellum) homogenates to deamidate arachidonyl ethanolamide (anandamide) was determined with a custom-synthesized substrate, arachidonyl ethanolamide-[1-3H] ([3H]anandamide). Conditions whereby initial velocities were measured were established. The homogenates deamidated anandamide with a Km value of 0.8 μM and a Vmax value of 1.73 nmol · (mg protein)−1 · min−1. The deamidation of 2 μM [3H]anandamide was inhibited by phenylmethylsulfonyl fluoride and arachidonyl trifluoromethyl ketone with IC50 values of 3.7 and 0.23 μM, respectively. Ibuprofen inhibited anandamide deamidation in a mixed fashion, withKi and K′i values of 82 and 1420 μM. At an anandamide concentration of 2 μM, the IC50 values (in μM) of a series of compounds related in structure to ibuprofen were as follows: suprofen, 170; ibuprofen, 270; fenoprofen, 480; naproxen, 550; ketoprofen, 650; diclofenac, ∼1000. Sulindac produced 27% inhibition at a concentration of 1000 μM, whereas isobutyric acid, hydrocinnamic acid, acetylsalicylic acid and acetaminophen were essentially inactive at concentrations ≤ 1 mM. We conclude that ibuprofen inhibits anandamide deamidation at pharmacologically relevant concentrations and that there is some specificity to the inhibition produced by ibuprofen and suprofen.

Footnotes

  • Send reprint requests to: Dr. Christopher J. Fowler, Department of Pharmacology, Umeå University, S-901 87 Umeå, Sweden.

  • ↵1 This work received financial support from the Research Fund of the Medical Faculty, University of Umeå, and the Joint Committee, North Health Region, Sweden.

  • Abbreviations:
    Anandamide
    arachidonyl ethanolamide
    PMSF
    phenylmethylsulfonyl fluoride
    NSAID
    nonsteroidal anti-inflammatory drug
    COX
    cyclooxygenase
    • Received November 25, 1996.
    • Accepted July 2, 1997.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics
Vol. 283, Issue 2
1 Nov 1997
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OtherANALGESIA AND DRUGS OF ABUSE

Ibuprofen Inhibits Rat Brain Deamidation of Anandamide at Pharmacologically Relevant Concentrations. Mode of Inhibition and Structure-Activity Relationship

Christopher J. Fowler, Gunnar Tiger and Anders Stenström
Journal of Pharmacology and Experimental Therapeutics November 1, 1997, 283 (2) 729-734;

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OtherANALGESIA AND DRUGS OF ABUSE

Ibuprofen Inhibits Rat Brain Deamidation of Anandamide at Pharmacologically Relevant Concentrations. Mode of Inhibition and Structure-Activity Relationship

Christopher J. Fowler, Gunnar Tiger and Anders Stenström
Journal of Pharmacology and Experimental Therapeutics November 1, 1997, 283 (2) 729-734;
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