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

Table 5. Affinity of FPPQ for Receptors, Transporters, and Ion Channels Selected from Selectivity Profiling Panel, Compared with Its Affinities at 5-HT₃R and 5-HT₆R Main Targets, Suggest Decent Selectivity of FPPQ Compound.

assay^a	K_i [μM]
5-HT₃	0.00093^b
5-HT₆	0.003^b
α_2A	0.11
5-HT_2B	0.17
β₁	0.17
D₃	0.21
H₁	0.22
Ca⁺² channel L-type, dihydropyridine	0.50
Na⁺ channel, site 2	0.71
5-HT_2C	0.83
5-HT_1B	0.89
hERG	0.94
Ca⁺² channel L-type, benzothiazepine	1.08
DAT	1.09
NET	1.24
Ca⁺² channel L-Type, phenylalkylamine	1.32
M₁	1.94
5-HT_5A	2.87
μ (OP3, MOP)	2.88
κ (OP2, KOP)	3.27
σ₁	3.50
α_2B	4.61

Items meeting criteria of significance (≥50% stimulation or inhibition at 10 μM). For the results of all enzyme and radioligand binding assays, see Supporting Information Table S2.

See Table 4.

Table 5. Affinity of FPPQ for Receptors, Transporters, and Ion Channels Selected from Selectivity Profiling Panel, Compared with Its Affinities at 5-HT3R and 5-HT6R Main Targets, Suggest Decent Selectivity of FPPQ Compound.

Table 5. Affinity of FPPQ for Receptors, Transporters, and Ion Channels Selected from Selectivity Profiling Panel, Compared with Its Affinities at 5-HT₃R and 5-HT₆R Main Targets, Suggest Decent Selectivity of FPPQ Compound.