蛋白激酶C激活剂，佛波醇12 - 肉豆蔻酸酯13 - 乙酸酯和佛波醇12,13 - 二丁酸酯，在小鼠体内皮克 - 纳摩尔范围内具有惊厥作用。

The protein kinase C activators, phorbol 12-myristate,13-acetate and phorbol 12,13-dibutyrate, are convulsant in the pico-nanomolar range in mice.

作者信息

Smith S E, Meldrum B S

机构信息

Department of Neurology, Institute of Psychiatry, Denmark Hill, London, U.K.

出版信息

Eur J Pharmacol. 1992 Mar 17;213(1):133-5. doi: 10.1016/0014-2999(92)90242-v.

DOI:10.1016/0014-2999(92)90242-v

PMID:1499648

Abstract

Administration of phorbol 12-myristate,13-acetate (PMA, 10 fmol-10 nmol) or phorbol 12,13-dibutyrate (PDB, 0.2-495 nmol) (i.c.v.) to mice induced: hindlimb scratching, tremor, myoclonic jerks, hyperlocomotion, clonic seizure, followed by death or recovery. CD50 values for clonic seizures for PMA and PDB were 1.0 pmol and 1.2 nmol. 4-alpha-Phorbol (68-686 nmol) was inactive. The effects of PDB (24-247 nmol) were reduced by pretreatment with staurosporine (30 nmol, i.c.v.). Protein kinase C activators are potent convulsants in vivo.

摘要

向小鼠脑室内注射佛波醇12 -肉豆蔻酸酯13 -乙酸酯（PMA，10飞摩尔 - 10纳摩尔）或佛波醇12,13 -二丁酸酯（PDB，0.2 - 495纳摩尔）会引发：后肢抓挠、震颤、肌阵挛性抽搐、运动亢进、阵挛性惊厥，随后导致死亡或恢复。PMA和PDB引发阵挛性惊厥的半数惊厥剂量（CD50）值分别为1.0皮摩尔和1.2纳摩尔。4-α-佛波醇（68 - 686纳摩尔）无活性。用星形孢菌素（30纳摩尔，脑室内注射）预处理可降低PDB（24 - 247纳摩尔）的作用。蛋白激酶C激活剂在体内是强效惊厥剂。