Abstract
In functional studies, the term tissue selectivity is used for an agent showing varying degrees of potency among tissues with a preferential action in a given one. Such a selectivity is well known in the field of β-adrenoceptors, where β1 and β2 agonists and antagonists, differ by the ratio of activity at the level of a given tissue. Usually, this is related to their respective affinities for β1 and β2 adrenoceptors. Selectivity is not specificity which means that a given agent interacts with only one type of receptor. Such an interaction is largely documented in the field of histaminergic receptors where H1 antagonists do not interact with H2 receptors and vice versa. A question that has been raised several times (Godfraind et al., 1986), is the existence of a possible tissue selectivity of calcium antagonists. In other words, does any selectivity exist in the pharmacology of calcium channels ?
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References
Amédée, T., and Large, W. A., 1989, Microelectrode study on the ionic mechanisms which contribute to the noradrenaline-induced depolarization in isolated cells of the rabbit portal vein, Br. J. Pharmacol., 97:1331.
Bean, B. P., 1984, Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state, Proc. Natl. Acad. Sci., 81:6388.
Bean, B. P., Sturek, M., Puga, A. and Hermsmeyer, K., 1986, Calcium channels in muscle cells isolated from rat mesenteric arteries: modulation by dihydropyridine drugs, Circ. Res., 59:229.
Bristow, M. R., Ginsburg, R., Laser, J. A., McAuley, B. J. and Minoba, W., 1984, Tissue response selectivity of calcium antagonists is not due to heterogeneity of [3H]-nitrendipine binding sites, Br. J. Pharmacol. 82:309.
Cauvin, C., and Van Bremen, C., 1985, Different Ca2+ channels along the arterial tree, J. Cardiovasc. Pharmacol., 7:54.
Cauvin, C, and Van Bremen, C, 1985, 45Ca fluxes in isolated rabbit mesenteric resistance vessels as compared to rabbit aorta, Prog. Appl. Microvasc. 8:47.
Chen, G., and Suzuki, H., 1989, Some electrical properties of the endothelium-dependent hyperpolarization recorded from rat arterial smooth muscle cells, J. Physiol. (Lond.). 410:91.
Dunn, W. R., Daly, C. J., McGrath, J. C. and Wilson, V. G., 1991, A comparison of the effects of angiotensin II and Bay K 8644 on responses to noradrenaline mediated via postjunctionnal oci and \ga2-adrenoceptors in rabbit isolated blood vessels, Br. J. Pharmacol.. 103:1475.
Féron, O., Wibo, M., and Godfraind, T., 1991, Interaction of Pinaverium bromide with the dihydropyridine binding site in rat ileum smooth muscle, Arch. Int. Pharm.
Godfraind, T., 1983, Actions of nifedipine on calcium fluxes and contraction in isolated rat arteries, J. Pharmacol. Exp. Ther., 224:443.
Godfraind, T., Egleme, C., Finet, M. and Jaumin, P., 1987, The actions of nifedipine and nisoldipine on the contractile activity of human coronary arteries and human cardiac tissue in vitro, Pharmacol. Toxicol., 61:79.
Godfraind, T. and Kaba, A., 1969, Inhibition by cinnarizine and chlorpromazine of the contraction induced by calcium and adrenaline in vascular smooth muscle, Br. J. Pharmacol., 35:354P.
Godfraind, T., Miller, R. C., and Wibo, M., 1986, Calcium antagonism and calcium entry blockers, Pharmacol. Rev., 38:321.
Kokubun, S., Prod’Hom, B., Becker, C., Porzig, H., and Reuter, H., 1986, Studies on Ca channels in intact cardiac cells voltage -dependent effects and cooperative interactions of dihydropyridine enantiomers, Mol. Pharmacol., 30:571.
Marriott, J. F., 1988, Comparison of the effects of the calcium entry blockers, verapamil, diltiazem and flunarizine against contractions of the rat isolated aorta and portal vein, Br. J. Pharmacol., 95:145.
McKenna, E., Koch, W. J., Slish, D. F., and Schwartz, A., 1990, Toward an understanding of the dihydropyridine-sensitive calcium channel, Biochem. Pharmacol., 39:1145.
Morel, N., and Godfraind, T., 1987, Prolonged depolarization increases the pharmacological effect of dihydropyridines and their binding affinity for calcium channels of vascular smooth muscle, J. Pharmacol. Exp. Ther., 243:711.
Morel, N., and Godfraind, T., 1988, Selective modulation by membrane potential of the interaction of some calcium entry blockers with calcium channels in rat mesenteric artery, Br. J. PHarmacol., 95:252.
Morel, N., and Godfraind, T., 1989, Pharmacological properties of voltage-dependent calcium channles in functional microvessels isolated from rat brain, Naunyn-Schmiedeberg’s Arch. Pharmacol., 340:442.
Morel, N., and Godfraind, T., 1991, Characterization in rat aorta of the binding sites responsible for blockade of noradrenaline-evoked calcium entry and contraction by nisoldipine, Br. J. Pharmacol., 102:467.
Pacaud, P., Loirand, G., Mironneau, C., and Mironneau, J., 1989, Noradrenaline activates a calcium-activated chloride conductance and increases the voltage-dependent calcium current in cultured single cells of rat portal vein, Br. J. Pharmacol., 97:139.
Sanguinetti, M. C, and Kass, R. S., 1984, Voltage-dependent block of calcium channel current in the calf cardiac Purkinje fiber by dihydropyridine calcium channel antagonists, Circ. Res., 55:336.
Sumimoto, K, Hirata, M., and Kuriyama, H., 1988, Characterization of [3H]nifedipine binding to intact vascular smooth muscle cells, Am. J. Phvsiol., 254:C45.
Tsien, R.W., 1983, Calcium channels in excitable cell membranes, Annu. Rev. Phvsiol., 45:341.
White, D. G., and Martin, W., 1989, Differential control and calcium-dependence of production of endothelium-derived relaxing factor and prostacyclin by pig aortic endothelial cells, Br. J. Clin. Pharmacol., 97:683.
Wibo, M., De Roth, L., and Godfraind, T., 1988, Pharmacological relevance of dihydropyridine binding sites in membrane from rat aorta: kinetic and equilibrium studies, Circ. Res., 62:91.
Wibo, M., 1989, Mode of action of calcium antagonists: voltage-dependence and kinetics of drug-receptor interaction, Pharmacol. Toxicol., 65:1.
Yatani, A., Codina, J., Imoto, Y., Reeves, J. P., Birnbaumer, L., and Brown, A. M., 1987, A G protein directly regulates mammalian cardiac calcium channels, Science. 238:1288.
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Godfraind, T. (1992). Analysis of Factors Involved in the Tissue Selectivity of Calcium Antagonists. In: Frank, G.B., Bianchi, C.P., ter Keurs, H.E.D.J. (eds) Excitation-Contraction Coupling in Skeletal, Cardiac, and Smooth Muscle. Advances in Experimental Medicine and Biology, vol 311. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-3362-7_8
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DOI: https://doi.org/10.1007/978-1-4615-3362-7_8
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