Triggle D J
School of Pharmacy, State University of New York, Buffalo 14260.
Chirality. 1994;6(2):58-62. doi: 10.1002/chir.530060204.
Ion channels are pharmacological receptors with specific drug binding sites. These binding sites define specific structure-function relationships for the actions of drug classes. Interpretation of these structure-function relationships may be complex because of state-dependent drug-channel interactions. These state-dependent interactions determine affinity and access of drug to binding sites and may result in both quantitative and qualitative changes in structure-function relationships including stereoselectivity. A channel-active drug may exhibit antagonist or activator properties according to membrane potential and the stereoselectivity of interaction may also change with channel state.
离子通道是具有特定药物结合位点的药理学受体。这些结合位点定义了药物类别作用的特定结构-功能关系。由于状态依赖性药物-通道相互作用,对这些结构-功能关系的解释可能很复杂。这些状态依赖性相互作用决定了药物与结合位点的亲和力和可及性,并可能导致结构-功能关系的定量和定性变化,包括立体选择性。一种通道活性药物可能根据膜电位表现出拮抗剂或激活剂特性,并且相互作用的立体选择性也可能随通道状态而变化。