Balfour J K
Toxicology. 1978 Feb;9(1-2):11-20. doi: 10.1016/0300-483x(78)90027-6.
The uptake and metabolic fate of the sensory irritant dibenz(b,f)-1,4-oxazepine (CR) have been investigated in intact cornea and corneal homogenates using 3H-labelled CR. The cornea metabolises CR to its lactam derivative (10,11-dihydro-10-oxo-dibenz(b,f)-1,4-oxazepine) by a process which appears to be located in the cell cytoplasm and which is easily saturated. Uptake studies with higher concentrations of [3H]CR (1 X10(-5) M) which saturate lactam biosynthesis, suggest that CR may bind, with low affinity, to sites within the corneal cells. The possible roles of CR metabolism and CR binding in chemical sensory irritation are discussed.
利用3H标记的CR,在完整角膜和角膜匀浆中研究了感觉刺激剂二苯并(b,f)-1,4-恶唑嗪(CR)的摄取和代谢命运。角膜通过一个似乎位于细胞质且容易饱和的过程将CR代谢为其内酰胺衍生物(10,11-二氢-10-氧代-二苯并(b,f)-1,4-恶唑嗪)。用更高浓度的[3H]CR(1×10(-5)M)进行的摄取研究使内酰胺生物合成饱和,表明CR可能以低亲和力与角膜细胞内的位点结合。讨论了CR代谢和CR结合在化学感觉刺激中的可能作用。