Fig. 6.

Activation and potentiation of α4β2L15′M receptors by the novel TQS analog GAT927. (A) The averaged normalized raw data (n = 5) for cells expressing α4β2L15′M receptors to the application of 10 µM GAT927 (structure shown in the inset). Note the strong potentiation of subsequent ACh applications following the application of GAT927. (B) Responses of α4β2L15′M receptors to GAT927 applied alone. The data are averaged peak currents (±S.E.M, n = 4–7), normalized to 30 µM ACh control responses from the same cells. Note that following the application of concentrations of GAT927 ≥30 µM applied alone, subsequent applications of ACh produced responses too large to be voltage clamped. These data were unsuitable to be fit to the Hill equation since there was no detectable plateau in the response. (C) Responses of α4β2L15′M receptors to GAT927 coapplied with 30 µM ACh. The data are averaged peak currents (±S.E.M., n = 4–7), normalized to 30 µM ACh control responses from the same cells. Note that following the coapplication of concentrations of GAT927 >10 µM, responses were too large to be voltage clamped. These data were unsuitable to be fit to the Hill equation since there was no detectable plateau in the response.