PROSTAGLANDINS AND CANNABIS .16. ANTAGONISM OF DELTA-1-TETRAHYDROCANNABINOL ACTION BY ITS METABOLITES

PROSTAGLANDINS AND CANNABIS .16. ANTAGONISM OF DELTA-1-TETRAHYDROCANNABINOL ACTION BY ITS METABOLITES
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DOI:
10.1016/0006-2952(86)90053-5
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发表时间:
1986-08-01
影响因子:
5.8
通讯作者:
RENZULLI, L
RENZULLI, L
中科院分区:
医学2区
文献类型:
--
作者:
BURSTEIN, S;HUNTER, SA;RENZULLI, L

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细胞在体外预先暴露于DELTA1-四氢大麻酚-7-OIC酸(DELTA1-THC-7-OIC酸)可降低随后用DELTA1-THC处理引起的前列腺素合成的刺激程度。这种抑制作用的作用部位似乎是环氧合酶,而不是参与磷脂酶介导的花生四烯酸释放的早期步骤。DELTA1-THC-7-OIC酸是DELTA1-THC的主要代谢物,在人类体内没有精神活动。然而,我们的发现提出了这样一种可能性,即它可能通过拮抗其对细胞前列腺素合成的刺激作用来影响Delta1-THC的体内活性。
Prior exposure of cells in vitro to .DELTA.1-tetrahydrocannabinol-7-oic acid (.DELTA.1-THC-7-oic acid) reduced the degree of stimulation of prostaglandin synthesis incurred by subsequent treatment with .DELTA.1-THC. The site of action of this inhibitory effect seemed to be on cyclooxygenase and not at the earlier step involving the phospholipase-mediated release of arachidonic acid. .DELTA.1-THC-7-oic acid is a major metabolite of .DELTA.1-THC and has no psychoactivity in humans. Our findings raise the possibility, however, that it may influence the in vivo activities of .DELTA.1-THC by antagonizing its stimulatory action on cellular prostaglandin synthesis.