Al-Gadi M, Hill S J
Br J Pharmacol. 1987 May;91(1):213-22. doi: 10.1111/j.1476-5381.1987.tb09001.x.
The effect of calcium on the H1- and H2-receptor components of the cyclic AMP response to histamine in rabbit cerebral cortical slices has been investigated. Removal of calcium ions from the incubation medium during the preparation, preincubation and final incubation of brain slices significantly reduced the cyclic AMP responses to adenosine, histamine and the H2-selective agonist, impromidine. Removal of calcium ions from the incubation medium during only the final incubation with agonists did not influence the responses to adenosine, histamine, impromidine and the H1-selective agonist, 2-thiazolylethylamine. Final incubation of rabbit cerebral cortical slices in calcium-free buffer containing EGTA (1 mM) however, selectively reduced the cyclic AMP responses to the H1-agonists histamine and 2-thiazolylethylamine without affecting the response to impromidine or adenosine. These latter incubation conditions significantly reduced the maximal extent of the augmentation of impromidine- or adenosine-stimulated cyclic AMP accumulation produced by H1-receptor stimulation, without affecting the EC50 values of the H1-agonists. Calcium-free/EGTA conditions did not, however, alter the dose-response parameters for the response to the H2-agonist, impromidine. These data provide further evidence that the two histamine receptor systems affect cyclic AMP accumulation in rabbit cerebral cortical slices by different mechanisms.
研究了钙对兔大脑皮质切片中组胺引起的环磷酸腺苷(cAMP)反应的H1和H2受体成分的影响。在脑片制备、预孵育和最终孵育过程中,从孵育培养基中去除钙离子显著降低了对腺苷、组胺和H2选择性激动剂英普咪定的cAMP反应。仅在与激动剂的最终孵育过程中从孵育培养基中去除钙离子,并不影响对腺苷、组胺、英普咪定和H1选择性激动剂2-噻唑基乙胺的反应。然而,将兔大脑皮质切片在含有EGTA(1 mM)的无钙缓冲液中进行最终孵育,选择性地降低了对H1激动剂组胺和2-噻唑基乙胺的cAMP反应,而不影响对英普咪定或腺苷的反应。这些后一种孵育条件显著降低了H1受体刺激产生的英普咪定或腺苷刺激的cAMP积累增加的最大程度,而不影响H1激动剂的半数有效浓度(EC50)值。然而,无钙/EGTA条件并未改变对H2激动剂英普咪定反应的剂量反应参数。这些数据进一步证明,两种组胺受体系统通过不同机制影响兔大脑皮质切片中的cAMP积累。