Pharmacological gating modulation of small- and intermediate-conductance Ca(2+)-activated K(+) channels (KCa2.x and KCa3.1).

摘要: This short review discusses pharmacological modulation of the opening/closing properties (gating) small- and intermediate-conductance Ca(2+)-activated K(+) channels (KCa2 KCa3.1) with special focus on mechanisms-of-action, selectivity, binding sites, therapeutic potentials. Despite KCa channel gating-modulation being a relatively novel field in drug discovery, efforts this area have already revealed surprising plethora sites-of-actions subtype selectivity exerted by different chemical classes. The currently published positive modulators show that such molecules are potentially useful for treatment various neurodegenerative disorders as ataxia, alcohol dependence, epilepsy well hypertension. negative KCa2 very effective agents atrial fibrillation. prediction is further unraveling molecular details gating pharmacology will allow design even more potent selective entering into development these indications.