Maggi C A, Astolfi M, Donnerer J, Amann R
Pharmacology Department, A. Menarini Pharmaceuticals, Florence, Italy.
Neurosci Lett. 1990 Mar 14;110(3):267-72. doi: 10.1016/0304-3940(90)90858-7.
In the rat isolated bladder, capsaicin produced a concentration-dependent contraction, shown previously to depend upon transmitter release from peripheral endings of primary afferents. When using low concentrations (30-300 nM) of capsaicin, exposure to a second and third dose of capsaicin produced smaller responses than the first application, although a subsequent challenge with 10 microM capsaicin still elicited a contraction which was not reduced as compared to the response produced by the first exposure to a low dose of capsaicin. Capsaicin also evoked a prompt outflow of calcitonin gene-related peptide-like immunoreactivity (CGRP-LI), taken as a marker for sensory nerve activation. A second or third application of a submaximal concentration of the drug was ineffective, although a subsequent challenge with 1 microM capsaicin was effective. These findings indicate that neuropeptide depletion does not necessarily account for the early stage of capsaicin 'desensitization' of primary afferents.
在大鼠离体膀胱中,辣椒素可产生浓度依赖性收缩,此前已证明这种收缩依赖于初级传入神经外周末梢释放递质。当使用低浓度(30 - 300 nM)辣椒素时,第二次和第三次给予辣椒素所产生的反应比第一次应用时小,尽管随后用10 μM辣椒素刺激仍能引发收缩,与第一次低剂量辣椒素刺激所产生的反应相比并未减弱。辣椒素还能迅速引起降钙素基因相关肽样免疫反应性物质(CGRP-LI)外流,将其作为感觉神经激活的标志物。第二次或第三次给予次最大浓度的该药物无效,尽管随后用1 μM辣椒素刺激有效。这些发现表明,神经肽耗竭不一定是初级传入神经对辣椒素“脱敏”早期阶段的原因。