Fonnum F, Styr F
Acta Pharmacol Toxicol (Copenh). 1978 Oct;43(4):280-4. doi: 10.1111/j.1600-0773.1978.tb02266.x.
The effects of different compounds on the inhibition of choline acetyltransferase in guinea pig cornea have been studied. N-hydroxyethyl-4(naphthylvinyl)pyridinium bromide inhibited the enzyme in the cornea when a 0.5% solution was applied topically to the eye. The inhibition could not be explained by redistribution of the inhibitor after homogenization of the tissue. Inhibition of the enzyme was slowly reversed and nearly full enzyme activity was obtained when the eye was left intact for 48 hrs. N-methyl-4(naphthylvinyl)pyridinium bromide was a less efficient inhibitor in vivo and no inhibition was found with bromo acetonyl trimethylammonium bromide or acryloylcholine. Corneal ChAT was inhibited by the application of 3-methyl-5-methoxyphenyl pyridinium bromide, but the mechanism was obscured by the compound causing corneal oedema. The investigation shows that epithelium of the cornea can be used to test the in vivo effect of choline acetyltransferase inhibitors.
研究了不同化合物对豚鼠角膜中胆碱乙酰转移酶的抑制作用。当将0.5%的N-羟乙基-4(萘乙烯基)溴化吡啶溶液局部滴眼时,它能抑制角膜中的该酶。组织匀浆后抑制剂的重新分布无法解释这种抑制作用。酶的抑制作用缓慢逆转,当眼睛保持完整48小时后,几乎可获得完全的酶活性。N-甲基-4(萘乙烯基)溴化吡啶在体内是一种效率较低的抑制剂,而溴代丙酮基三甲基溴化铵或丙烯酰胆碱未发现有抑制作用。应用3-甲基-5-甲氧基苯基溴化吡啶可抑制角膜胆碱乙酰转移酶,但该化合物导致角膜水肿,使作用机制变得模糊。该研究表明,角膜上皮可用于测试胆碱乙酰转移酶抑制剂的体内作用。