KCC2a Inibidores

Os inibidores comuns do KCC2a incluem, entre outros, a furosemida CAS 54-31-9, o VU0240551 CAS 893990-34-6 e a tiazovivina CAS 1443246-62-5.

KCC2a inhibitors refer to a category of molecules that target the KCC2a subtype of the potassium-chloride cotransporter, commonly abbreviated as KCC2. This transporter is pivotal in neuronal physiology, specifically in determining the efficacy of inhibitory neurotransmission. KCC2 accomplishes this by actively extruding chloride ions (Cl-) from the neuron. The intracellular Cl- concentration plays a pivotal role in mediating the polarity and strength of GABAergic (gamma-aminobutyric acid) and glycinergic inhibitory postsynaptic. Thus, by regulating intracellular Cl- concentrations, KCC2 significantly impacts the overall excitability of the neuron.

The function of KCC2 has been a subject of extensive study, particularly in the context of neurodevelopment and neurological disorders. The efficacy of KCC2 can be modulated by various factors, including its phosphorylation status and interactions with other cellular proteins. KCC2a inhibitors, as the name suggests, act on the KCC2a subtype, and they work by altering the cotransporter's activity, usually by decreasing its function. Several compounds have been identified that inhibit KCC2a, with varying degrees of specificity and potency. The mechanism by which these inhibitors act can vary. Some bind directly to the transporter, competing with its natural substrates, while others might act allosterically, changing the conformation of the transporter to reduce its activity. A detailed understanding of these inhibitors and their precise mechanisms of action can offer insights into the intricate role KCC2a plays in the broader context of neuronal function and regulation.