Szolcsányi J, Jancsó-Gábor A
Arzneimittelforschung. 1975;25(12):1877-81.
A quantitative method for measuring the efficiency of pungent agents of capsaicin-type by the pain reaction elicited on the eye of rats is described. About 50 derivatives -- most of them amides or esters of homovanillic acid -- were tested by this method and the share of different chemical groups of the molecule in the pungent action was analyzed. It turned out that the presence of an acylamide linkage or alkyl chain is not essential for pungency, since acylamide linkage can be replaced by an esteric group and the alkyl chain by cycloalkyl rings. The importance of OH group on the aromatic ring is confirmed. On the basis of the findings a hypothetical pharmacological receptor for capsaicin on pain sensory nerve endings is presented.
描述了一种通过大鼠眼部引发的疼痛反应来测量辣椒素型辛辣剂效率的定量方法。用该方法测试了约50种衍生物——其中大多数是高香草酸的酰胺或酯——并分析了分子中不同化学基团在辛辣作用中的占比。结果表明，酰酰胺键或烷基链的存在对辛辣性并非必不可少，因为酰酰胺键可被酯基取代，烷基链可被环烷基环取代。证实了芳环上OH基团的重要性。基于这些发现，提出了一种关于辣椒素在疼痛感觉神经末梢上的假想药理受体。
