Kristiansen U, Hansen L, Nielsen G D, Holst E
Acta Pharmacol Toxicol (Copenh). 1986 Jul;59(1):60-72. doi: 10.1111/j.1600-0773.1986.tb00135.x.
Cumene and n-propanol, model substances for alcohols and alkylbenzenes, were investigated for sensory irritation in mice. The concentrations within the first 2 min. depressing the respiratory rate by 50% due to the effect in the upper respiratory tract were 2,058 p.p.m. and 22,080 p.p.m., respectively. Activation of the sensory irritant receptor followed the dynamics of reversible bimolecular reactions. The extrapolated maximum response and the apparent dissociation constant were 114.3% and 2,723 p.p.m. for cumene and 68.4% and 8,178 p.p.m. for propanol, respectively. Later on desensitization was observed. The effect was weak for cumene but conspicuous for propanol. For cumene desensitization had the origin in the rise of a threshold. No change in the dissociation constant or the maximum response was found. For propanol a decrease in the maximum response, which may be explained by an allosteric effect, was observed. The pulmonary irritation response was weak for cumene but was for propanol more important than sensory irritation at high concentrations. The following hypotheses are put forward: the effect of pulmonary irritation on the tidal volume is mediated via the stretch receptors while the effect on the respiratory frequency is mediated via the J-receptors.
以异丙苯和正丙醇作为醇类和烷基苯的模型物质，对小鼠进行了感官刺激研究。在前2分钟内，由于对上呼吸道的作用使呼吸频率降低50%时的浓度，异丙苯为2058 ppm，正丙醇为22080 ppm。感觉刺激受体的激活遵循可逆双分子反应的动力学。异丙苯的外推最大反应和表观解离常数分别为114.3%和2723 ppm，丙醇分别为68.4%和8178 ppm。随后观察到脱敏现象。异丙苯的这种效应较弱，而正丙醇的则很明显。异丙苯脱敏的起因是阈值升高。未发现解离常数或最大反应有变化。对于正丙醇，观察到最大反应降低，这可能由变构效应来解释。异丙苯的肺部刺激反应较弱，但对于正丙醇来说，在高浓度时肺部刺激比感官刺激更重要。提出了以下假设：肺部刺激对潮气量的影响是通过牵张感受器介导的，而对呼吸频率的影响是通过J感受器介导的。
