Feldman R D, Dixon S J
Department of Medicine, University of Western Ontario, London, Canada.
Mol Pharmacol. 1993 Aug;44(2):393-8.
Analogues of amiloride are widely used as pharmacological probes for inhibition of sodium-hydrogen counter-transport. In Jurkat cells, a leukemic T lymphocyte cell line, analogues of amiloride are also potent inhibitors of Na-K-Cl cotransport. The effects of these agents are not additive with those of beta-adrenoceptor agonists (which inhibit Na-K-Cl cotransport presumably by stimulation of adenylyl cyclase). Further, analogues of amiloride potently stimulate cAMP-dependent protein kinase activity. The present studies indicate that beta-adrenoceptor agonists and analogues of amiloride both act to inhibit Na-K-Cl cotransport and both stimulate cAMP-dependent protein kinase activity. Furthermore, these studies demonstrate a novel mechanism by which amiloride analogues may mediate effects separately from inhibition of sodium-hydrogen exchange.
氨氯地平类似物被广泛用作抑制钠氢逆向转运的药理学探针。在白血病T淋巴细胞系Jurkat细胞中，氨氯地平类似物也是钠-钾-氯协同转运的有效抑制剂。这些药物的作用与β-肾上腺素能受体激动剂（可能通过刺激腺苷酸环化酶抑制钠-钾-氯协同转运）的作用不是相加的。此外，氨氯地平类似物能有效刺激cAMP依赖性蛋白激酶活性。目前的研究表明，β-肾上腺素能受体激动剂和氨氯地平类似物都能抑制钠-钾-氯协同转运，且都能刺激cAMP依赖性蛋白激酶活性。此外，这些研究还证明了一种新机制，通过该机制氨氯地平类似物可能独立于抑制钠氢交换介导其效应。
