DMAB-anabaseine dihydrochloride. Antagonist or Partial Agonist of nAChR.
nAChRs are members of the Cys-Loop ligand-gated ion channel superfamily, located both in the peripheral and central nervous systems (PNS and CNS, respectively). These receptors, existing as both homopentameric and heteropentameric transmembrane ion channels, are validated therapeutic targets for various CNS pathologies.
DMAB-anabaseine (DMAB), an anabaseine analog, is a selectively partial agonist at alpha7 receptors which are predominantly found in the central nervous system. In contrast, DMAB is an antagonist at alpha3beta4, alpha4beta2 and other nicotinic receptors and blocks the alpha4beta2 current with an IC50 of about 5 μM.
Ion Channel Modulators; Nicotinic Acetylcholine Receptor Activators.
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