Abstract
For many drugs that target ion channels, drug affinity depends strongly on the precise gating state of the channel. A drug’s clinical utility is often due to its state dependence, and state-dependent inhibition is a key consideration for experimental use of a drug. This chapter describes theoretical models of state-dependent inhibition, including use-dependent block, modulated and guarded receptors, and drug-inactivation synergism, and shows how these models can explain the molecular mechanisms of block by several commonly used calcium channel antagonists.
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Timin, E.N., Berjukow, S., Hering, S. (2004). Concepts of State-Dependent Pharmacology of Calcium Channels. In: McDonough, S.I. (eds) Calcium Channel Pharmacology. Springer, Boston, MA. https://doi.org/10.1007/978-1-4419-9254-3_1
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DOI: https://doi.org/10.1007/978-1-4419-9254-3_1
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