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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 3. Pharmacological evaluation analogues 12a-20 tested at 10 μM against an ACh-mediated concentration-response curve.

graphic file with name EMS197014-i025.jpg
Compound # A Δbaselinea ΔpEC50 ΔEmaxb
1e graphic file with name EMS197014-i026.jpg 103.2 ± 2.85 1.48 ± 0.20 44.7 ± 2.74
12a graphic file with name EMS197014-i027.jpg 13.0 ± 2.18* 0.88 ± 0.07* 41.6 ± 2.67
12b graphic file with name EMS197014-i028.jpg 6.49 ± 1.85* 0.63 ± 0.07* 25.6 ± 2.78*
12c graphic file with name EMS197014-i029.jpg 47.2 ± 2.93* 0.17 ± 0.13* 56.8 ± 4.81
12d graphic file with name EMS197014-i030.jpg 90.6 ± 7.00* 1.49 ± 0.28 66.6 ± 5.99*
12e graphic file with name EMS197014-i031.jpg 48.5 ± 2.91* −0.34 ± 0.16* 35.1 ± 5.31
16 20.0 ± 4.81* 1.07 ± 0.20 11.8 ± 6.21*
20 24.5 ± 2.44* 1.06 ± 0.10 13.9 ± 2.95*

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 10 μM PAMs shown in Supp. Fig. 4. 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 baseline ACh response in the absence of PAM.

b

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