. 2021 Sep 1;64(18):13279–13298. doi: 10.1021/acs.jmedchem.1c00224

Table 1. Agonist/Antagonist Properties of Compounds 5d, 5e, 6, 7, II, and Ondansetron for 5-HT₃Rs, and Antagonist Properties and Binding Data of Compounds 5d, 5e, 6, 7, II, Ondansetron, Intepirdine, and SB399885 for 5-HT₆Rs.

			5-HT₃R			5-HT₆R
compound	core	R	agonist effect^b	antagonist effect^c	pD₂′^d	K_b [nM]^e	K_i [nM]^f
5d	A	CH₃	100 (100 nM)	NT	NT	>10 000	245
5e	A	H	9 (100 nM) 43 (300 nM)	NT	NT	>10 000	757
6	B	CH₃	NT	28 (100 nM) 48 (300 nM)	NT	4	2
7	B	H	NT	26 (100 nM) 60 (300 nM)	6.43	17	11
II^a			NT	7 (300 nM)	NT	1	6
ondansetron			NT	pA₂ = 7.11 ± 0.12	NT	>10 000	NT
intepirdine			NT	NT	NT	1.2	1.4
SB399885			NT	NT	NT	1.6	0.7

Compound reported in ref (37). For synthesis, see Supporting Information Scheme S1.

The effect induced by the tested compounds at the concentration of 100 or 300 nM expressed as a percent of maximal contraction of guinea pig ileum induced by control agonist (5-HT).

Percent inhibition of response to stimulation by 5-HT (contraction of guinea pig ileum) at the concentration of 3 μM induced by different concentrations of tested compounds shown in brackets (N = 6–8, SEM ≤ 12%).

Antagonist potency expressed as pD₂′ (N = 6–8, SEM ≤ 14%).

Mean K_b values based on two independent experiments in 1321N1 cells (SEM ≤ 22%).

Mean K_i values based on three independent binding experiments in HEK cells stably expressing h5-HT₆R (SEM ≤ 15%).

Table 1. Agonist/Antagonist Properties of Compounds 5d, 5e, 6, 7, II, and Ondansetron for 5-HT3Rs, and Antagonist Properties and Binding Data of Compounds 5d, 5e, 6, 7, II, Ondansetron, Intepirdine, and SB399885 for 5-HT6Rs.

Table 1. Agonist/Antagonist Properties of Compounds 5d, 5e, 6, 7, II, and Ondansetron for 5-HT₃Rs, and Antagonist Properties and Binding Data of Compounds 5d, 5e, 6, 7, II, Ondansetron, Intepirdine, and SB399885 for 5-HT₆Rs.