Table 1.

(h)AChE inhibitory Activity (% inhibition or IC₅₀) and (h)5-HT₄R affinity (% inhibition or Ki).

Compound	X	R	(h)AChE IC50 (nM) or % Inhibition at 10−6 M	(h)5-HT4R Ki (nM) or % Inhibition at 10−8 M
Donepezil	-	-	7.0 ± 1.5	-
Rivastigmine	-	-	4.150 ± 160 1	-
RS67333	-	-	-	5.1 ± 0.5 2
4	CH2	OH	148.6 ± 34.9	5.1 ± 1.1
7	CH2	OCON(Me)Et	4151 ± 794	3%
5	O	OH	11%	0.6 ± 0.4
8	O	OCON(Me)Et	16,290 ± 240	23%
6	NH	OH	4%	5.8 ± 1.2
9	NH	OCON(Me)Et	10,077 ± 2,988	13%
19	CH2	OH, fumaric salt	72.0 ± 1.4	6.9 ± 1.2
20	CH2	OCON(Me)Et, fumaric salt	6070 ± 404	16%

IC₅₀ values are expressed as mean ± standard error of the mean (SEM) of at least two experiments; Ki values are expressed as mean ± standard error of the mean (SEM) of at least three experiments; ¹ Data from ref. [16]; ² Data from ref. [17].