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. Author manuscript; available in PMC: 2024 Jul 10.
Published in final edited form as: Eur J Med Chem. 2023 Jul 1;258:115588. doi: 10.1016/j.ejmech.2023.115588

Table 2. Pharmacological evaluation analogues 1e and 6j-u, tested at 10 μM against an ACh-mediated concentration-response curve.

graphic file with name EMS197014-i011.jpg
Compound # R1 Δbaselinea ΔpEC50 ΔEmaxb
1e graphic file with name EMS197014-i012.jpg 103.2 ± 2.85 1.48 ± 0.20 44.7 ± 2.74
6j graphic file with name EMS197014-i013.jpg 32.1 ± 2.52* 1.15 ± 0.10 21.8 ± 2.97*
6k graphic file with name EMS197014-i014.jpg 51.4 ± 9.53* 0.76 ± 0.26* 128.8 ± 9.68
6l graphic file with name EMS197014-i015.jpg 8.48 ± 4.01* 1.27 ± 0.15 5.60 ± 4.45*
6m graphic file with name EMS197014-i016.jpg 88.1 ± 4.09 1.31 ± 0.17 80.6 ± 4.78*
6n graphic file with name EMS197014-i017.jpg 51.7 ± 4.21* 1.35 ± 0.17 53.5 ± 5.54
6o graphic file with name EMS197014-i018.jpg 33.2 ± 4.25* 0.25 ± 0.11* 97.7 ± 4.47*
6p graphic file with name EMS197014-i019.jpg 78.2 ± 5.58* 1.99 ± 0.19 61.3 ± 3.81
6q graphic file with name EMS197014-i020.jpg 77.3 ± 3.17* 1.33 ± 0.13 65.6 ± 3.48*
6r graphic file with name EMS197014-i021.jpg 52.2 ± 5.62* 1.63 ± 0.17 57.7 ± 4.85
6s graphic file with name EMS197014-i022.jpg 89.7 ± 6.11 2.57 ± 0.25* 73.3 ± 7.00*
6t graphic file with name EMS197014-i023.jpg 83.3 ± 4.16* 2.11 ± 0.18* 50.5 ± 3.60
6u graphic file with name EMS197014-i024.jpg 18.6 ± 3.70* 1.24 ± 0.11 39.0 ± 3.53

Data represent the mean ± SEM of 4 independent experiments performed in duplicate. Only the change in pEC50, baseline and Emax for the 10 μM concentrations of PAMs are reported, with the full ACh concentration-response curves in the presence of 1 μM and 10 μM PAMs shown in Supp. Fig. 3. Data were analysed by one-way ANOVA and compared to the control PAM, 1e, with a post-hoc Dunnett test

where *p < 0.05 was considered to be significantly different.

a

Δbaseline is expressed as a percentage of the maximum ACh response in the absence of PAM.

b

ΔEmax is expressed as a percentage of the maximum ACh response in the absence of PAM.