卡巴胆碱诱导的豚鼠盲肠带短期脱敏发生在细胞内钙储存部位，而组胺诱导的短期脱敏发生在H1受体部位。
Short-term desensitization of guinea-pig taenia caecum induced by carbachol occurs at intracellular Ca stores and that by histamine at H1-receptors.
作者信息
Hishinuma S, Uchida M K
机构信息
Department of Molecular Pharmacology, Meiji College of Pharmacy, Toyoko, Japan.
出版信息
Br J Pharmacol. 1988 Jul;94(3):882-9. doi: 10.1111/j.1476-5381.1988.tb11600.x.
Abstract
- In Ca-free solution, the contractile response of guinea-pig taenia caecum to 10(-4) M carbachol was mediated through muscarinic receptors and was reduced time-dependently by desensitization with 10(-4) M carbachol, but not 10(-4) M histamine. On the other hand, the response to 10(-4) M histamine was shown to be mediated through H1-receptors and to be reduced time-dependently by desensitization with either 10(-4) M histamine or 10(-4) M carbachol. 2. The maximal K+ contraction was not changed by desensitization with carbachol or histamine. Thus, contractile proteins and voltage-dependent Ca channels maintain their normal functions. 3. To study the coupling of Ca channel activity in cell surface membrane to receptor activation, the contractile responses elicited by carbachol and histamine added simultaneously with Ca to Ca-free solution were measured. The response elicited by carbachol plus Ca was not changed by desensitization with carbachol, while that elicited by histamine plus Ca was reduced by desensitization with histamine. These results show that desensitization by carbachol occurs at a post-receptor site, whereas that induced by histamine occurs at H1-receptors. 4. After desensitization with carbachol, but not histamine, the contractile response to 5 x 10(-2) M caffeine in Ca-free solution was significantly reduced. 5. These results show that short-term desensitization of guinea-pig taenia caecum by carbachol is heterologous and occurs at intracellular Ca stores, while that induced by histamine is homologous and occurs at histamine H1-receptors.
摘要
- 在无钙溶液中，豚鼠盲肠带对10⁻⁴ M卡巴胆碱的收缩反应是通过毒蕈碱受体介导的，并且用10⁻⁴ M卡巴胆碱脱敏会使其随时间依赖性降低，但用10⁻⁴ M组胺则不会。另一方面，对10⁻⁴ M组胺的反应显示是通过H1受体介导的，并且用10⁻⁴ M组胺或10⁻⁴ M卡巴胆碱脱敏都会使其随时间依赖性降低。2. 用卡巴胆碱或组胺脱敏不会改变最大钾离子收缩。因此，收缩蛋白和电压依赖性钙通道保持其正常功能。3. 为了研究细胞表面膜中钙通道活性与受体激活的偶联，测量了在无钙溶液中同时添加钙和卡巴胆碱或组胺所引发的收缩反应。用卡巴胆碱脱敏不会改变卡巴胆碱加钙所引发的反应，而用组胺脱敏会降低组胺加钙所引发的反应。这些结果表明，卡巴胆碱引起的脱敏发生在受体后位点，而组胺引起的脱敏发生在H1受体处。4. 用卡巴胆碱而非组胺脱敏后，无钙溶液中对5×10⁻² M咖啡因的收缩反应显著降低。5. 这些结果表明，卡巴胆碱对豚鼠盲肠带的短期脱敏是异源的，发生在细胞内钙储存处，而组胺引起的脱敏是同源的，发生在组胺H1受体处。
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