Carbonic anhydrase inhibition and the management of neuropathic pain.
DOI: 10.1080/14737175.2016.1193009
关键词: Analgesic 、 Neuralgia 、 Carbonic anhydrase 、 GABAA receptor 、 Allodynia 、 Population 、 Acetazolamide 、 Pharmacology 、 Neuropathic pain 、 Medicine
摘要: ABSTRACTIntroduction: Neuropathic pain affects up to 8% of the population with few therapeutic options for its management. No specific drugs are approved treatment.Areas covered: Recent advances in understanding pathological mechanisms this syndrome and biochemical/pharmacological characterization novel drug targets, evidenced carbonic anhydrase (CA, EC 4.2.1.1) inhibition as a new approach designing antineuropathic agents.Expert commentary: Peripheral nerve injury negatively influences spinal γ-aminobutyric (GABA)-ergic networks via reduction neuron-specific potassium-chloride (K+-Cl−) cotransporter (KCC2), which leads neuropathic allodynia. CA inhibitors (CAIs) reduce bicarbonate-dependent depolarization GABAA receptors, showing analgesic effects. Novel classes selective sulfonamide II/VII showed highly improved efficacy animal models pain, compared acetazolamide, offering basis development th...
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