INHIBITION OF ANANDAMIDE AMIDASE ACTIVITY IN MOUSE BRAIN MICROSOMES BY CANNABINOIDS

Kazuhito WATANABE; Yuichiro KAYANO; Tamihide MATSUNAGA; Ikuo YAMAMOTO; Hidetoshi YOSHIMURA

doi:10.1248/bpb.19.1109

Kazuhito WATANABE, Yuichiro KAYANO, Tamihide MATSUNAGA, Ikuo YAMAMOTO, Hidetoshi YOSHIMURA

著者情報

キーワード: cannabinoid, anandamide amidase, brain microsome, inhibitory effect

ジャーナルフリー

1996 年 19 巻 8 号 p. 1109-1111

DOI https://doi.org/10.1248/bpb.19.1109

詳細

抄録

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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