Table 1.

Inhibition in vitro binding affinities (K_i, nM) of ASEM, para-ASEM and the Abbott lead toward α7-nAChR, heteromeric nAChR subtypes and 5-HT₃ [48].

Compound	α7-nAChR a	Heteromeric nAChR subtypes b						5-HT3c	Selectivity
		α2β2	α2β4	α3β2	α3β4	α4β2	α4β4		α7/α4β2	α7/5HT3
	0.3, 0.5	-	-	-	-	-	-	660d	-	-
	0.37, 0.45	>10000	4000	1000	709	562	1000	230	1370	561
	1.32, 1.35	1000	8000	2000	5000	885	3000	505	663	378

^aRat cortical membranes, radiotracer [¹²⁵I]α-bungarotoxin (0.1 nM), K_D = 0.7 nM

^bInhibition in vitro binding assay of all heteromeric nAChR subtypes was performed with stably transfected HEK293 cells and [³H]epibatidine (0.5 nM), K_D = 0.021 nM (α2β2-nAChR), K_D = 0.084 nM (α2β4-nAChR), K_D = 0.034 nM (α3β2-nAChR), K_D = 0.29 nM (α3β4-nAChR), K_D = 0.046 nM (α4β2-nAChR), K_D = 0.094 nM (α4β4-nAChR).[80]

^cHuman 5-HT₃ recombinant/HEK293 cells, radiotracer [³H]GR65630 (0.35 nM), K_D = 0.5 nM

^dthe K_i value is taken from[60]