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Tissue‐ and subcellular‐distribution of the binding site of [3H]9‐methyl‐7‐bromoeudistomin D, a potent caffeine‐like Ca2+ releaser, in rabbits

Abstract— Tissue and subcellular distribution of the binding site of 3H‐labelled 9‐methyl‐7‐bromoeudistomin D ([3H]MBED), a powerful caffeine‐like Ca2+ releaser, were investigated in rabbits. The order of specific activities of total homogenates was liver > brain > other tissues. All binding was completely suppressed by 10 Mm caffeine, indicating that all [3H]MBED binding sites are modulated by caffeine. [3H]MBED binding sites distributed mainly in membrane fractions rather than soluble fractions in most tissues. In lung and liver, [3H]MBED binding was enriched in microsomes. [3H]MBED may be useful as a probe to investigate the actions of caffeine at the molecular level not only in muscles but also in a variety of tissues including liver, kidney and lung.