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. 2023 Mar 3;28(5):2349. doi: 10.3390/molecules28052349

Table 1.

Histamine H3 receptor affinities, cholinesterases, and MAO B inhibitory activity of the tested compounds.

graphic file with name molecules-28-02349-i001.jpg
Comp Amine n R hH3R aKi (nM)
Mean
[CI 95%]		 eeAChE b
IC50 (µM)
Mean ± SEM
(% inh) e 		eqBuChE c
IC50 (µM)
Mean ± SEM
(% inh) e 		hMAO B d
(% inh) f
2 graphic file with name molecules-28-02349-i002.jpg 3 CH3 34 [24;47] (45%) (25%) (2%)
3 4 CH3 75 [34;169] (67%) (23%) (3%)
4 3 C2H5 24 [11;54] (49%) (32%) (16%)
5 4 C2H5 41 [27;64] 4.79 ± 0.19 1.35 ± 0.04 (22%)
6 graphic file with name molecules-28-02349-i003.jpg 3 CH3 26 [13;52] 3.06 ± 0.10 (14%) (10%)
7 4 CH3 72 [41;127] 1.75 ± 0.05 (18%) (0%)
8 3 C2H5 12 [6;22] 2.10 ± 0.06 1.75 ± 0.05 (19%)
9 4 C2H5 38 [20;72] (68%) (66%) (12%)
10 graphic file with name molecules-28-02349-i004.jpg 3 CH3 120 [82;177] (60%) (43%) (0%)
11 4 CH3 106 [76;149] 2.65 ± 0.11 (49%) (0%)
12 3 C2H5 57 [36;91] (58%) 1.29 ± 0.08 (0%)
13 4 C2H5 58 [35;96] 2.56 ± 0.08 (65%) (1%)
14 graphic file with name molecules-28-02349-i005.jpg 3 CH3 52 [38;71] (63%) (63%) (37%)
15 4 CH3 79 [41;150] (67%) (68%) (6%)
16 3 C2H5 30 [17;53] 3.60 ± 0.12 0.55 ± 0.02 (6%)
17 4 C2H5 42 [20;85] 1.06 ± 0.03 2.86 ± 0.03 (5%)
pitolisant 12 ± 3 g (3%) g 8.42 ± 0.18 g (2%) g
donepezil nt h 0.04 ± 0.01 g 1.83 ± 0.02 nt h
safinamide nt h nt h nt h (98%)
7.60 ± 1.0 i

a [3H]-Nα-Methylhistamine binding assay performed in HEK293 cells expressing the human H3 receptor; mean value with a confidence interval (CI95%) from at least three independent repetitions b AChE of electric eel; IC50, mean value of three independent experiments; c BuChE of equine serum; IC50, mean value of three independent experiments. d Fluorometric AmplexTM red MAO assay. e Percentage inhibition of eeAChE or eqBuChE at 10 μM. f Percentage inhibition of hMAO B at 1 μM; mean values of two independent experiments. g Data from Ref. [19]. h Not tested. i IC50 in nM; data from ref. [20].