Amino acids regulating allosteric and orthosteric nAChR activation

Abstract

GAT107, the (+)-enantiomer of racemic 4BPTQS, is a strong positive allosteric modulator (PAM) of α7 nAChR activation by orthosteric agonists with intrinsic allosteric agonist activity. The direct activation produced by GAT107 in electrophysiological studies is observed only as long as GAT107 is freely diffusible in solution, while the potentiating activity… (More)

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