Potent positive allosteric modulator of alpha4beta2 nAChRs (EC50 values are 20 and 18 nM for rat and human, respectively). Selective for halpha4beta2 over halpha3beta2, halpha3beta4 and halpha7. Inhibits (alpha4)2(beta2)3, muscle-type and Torpedo nAChRs (IC50 values are 0.5, 0.7 and 0.2 µM, respectively), but not (alpha4)3(beta2)2 receptors. Exhibits ability to photoincorporate into aliphatic and nucleophilic amino acid side chains.
Target-Kategorie:
Others
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