Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
INHIBITION OF ANANDAMIDE AMIDASE ACTIVITY IN MOUSE BRAIN MICROSOMES BY CANNABINOIDS
Kazuhito WATANABEYuichiro KAYANOTamihide MATSUNAGAIkuo YAMAMOTOHidetoshi YOSHIMURA
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1996 Volume 19 Issue 8 Pages 1109-1111

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Abstract

Mouse brain microsomes contain an amidase that catalyzes the hydrolysis of N-arachidonylethanolamide to arachidonic acid and ethanolamine. The enzymatic activity is dependent on the protein concentration of the microsomes and observed over a wide range of pH, 7.4 to 9.5. Kinetic analysis indicated that Km (μM) and Vmax (nmol/min/mg protein) were 17.7 ± 4.1 and 1.81 ± 0.32, respectively. Cannabidiol (CBD), cannabinol (CBN) and Δ9-tetrahydrocannabinol (Δ9-THC) significantly inhibited the hydrolysis of the amide by mouse brain microsomes. At a concentration of 160 μM, the inhibitory potency decreased in the following order, CBD(66%)>CBN(46%)>Δ9-THC(31%).

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© The Pharmaceutical Society of Japan
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