[Ion channels and drugs: what can be learned from their interactions?].
The study of the interaction between drugs and the sodium channel is important to understand the functioning of the channel at the molecular level. The affinity of a drug to bind depends on the channel's state: rested, activated or inactivated state. Since the probability of these three states depends on the membrane potential and the drug itself may carry a charge, there are two reasons for a modulation of the effect by the membrane potential. Drugs like lidocaine and tertiary amines bind preferentially to the inactivated state. Others like disopyramide and penticainide block only the open or activated channel and do not bind to the channel in the rested or inactivated state. The same rule has to be applied for the unblocking. The consequences of these differences are discussed.
Carmeliet
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D000779:Anesthetics, Local / Q000494:pharmacology*; D004206:Disopyramide / Q000494:pharmacology; D004347:Drug Interactions; D006801:Humans; D008564:Membrane Potentials; D011437:Propylamines / Q000494:pharmacology; D011485:Protein Binding; D011725:Pyridines / Q000494:pharmacology; D015222:Sodium Channels / Q000187:drug effects* / Q000502:physiology*
D000779:Anesthetics, Local; D011437:Propylamines; D011725:Pyridines; D015222:Sodium Channels; C045930:propisomide; D004206:Disopyramide
Canaux ioniques et drogues: que peut-on apprendre de leur interaction?