. 2019 Apr 11;10:379. doi: 10.3389/fphar.2019.00379

Table 1.

TREK-1 blockers.

	Molecule	IC50	Cell type	Specificity	References
Peptides	Spadin (PE 12–28)	70 nM	COS, HEK, hTREK-1/HEK	Specific for TREK-1 channels, no effect on TREK-2, TRAAK, TASK or TRESK channels	Mazella et al., 2010
	PE 22–28	0.12 nM	hTREK-1/HEK		Djillani et al., 2017
	Biotin-PE 22–28	nd	hTREK-1/HEK		Djillani et al., 2017
	G/A-PE 22–28	0.1 nM	hTREK-1/HEK		Djillani et al., 2017
	Biotin-G/A-PE 22–28	1.2 nM	hTREK-1/HEK		Djillani et al., 2017
SSRIs	Fluoxetine	19 μM	tsA 201 cells	Antagonize TREK-2 (IC50 = 28.7 ± 7.6 μM), SERT (Ki = 0.07 μM), NAT (Ki = 8–10 μM) and Nav1.5 (IC50 = 39.4 ± 2 μM)	Kennard et al., 2005; Wong et al., 2005; Poulin et al., 2014
	Norfluoxetine	9 μM	tsA 201 cells	Blocks TREK-2 (IC50 = 4.9 ± 0.5 μM), Nav1.5 (IC50 = 29.5 ± 1 μM)	Kennard et al., 2005; Poulin et al., 2014; Mcclenaghan et al., 2016
	Paroxetine	20 μM tested	HEK293 cells	blocks TREK-2 (at 20 μM tested), SERT (Kd = 0.13 nM), GIRK and Kv3.1	Hirano et al., 2005; Kim et al., 2017
	Citalopram	100 μM tested	HEK293 cells	blocks TREK-2 (at 100 μM tested), SERT, Kv1.5 (IC50 = 2.8 ± 1.1 μM) and L-type Ca²⁺ channels (IC50 = 60.3 ± 8.5 μM)	Kim et al., 2017
	Escitalopram	81.94 μM	HEK293 cells	nd	Lin et al., 2015
Antipsychotics	Fluphenazine	4.7 μM	COS cells	Block TREK-2 (at 10 μM tested), no effect on TRAAK channels at 10 μM	Thummler et al., 2007
	Chlorpromazine	2.7 μM
	Haloperidol	5.5 μM
	Flupenthixol	2 μM
	Loxapine	19.7 μM
	Pimozide	1.8 μM
	Clozapine	10 μM tested
DHP Ca²⁺ channel antagonists	Amlodipine	0.43 μM	Bovine AZF	Block L-type Ca²⁺-channels	Liu et al., 2007
	Niguldipine	0.75 μM
Other TREK-1 blockers	SID1900	29.72 μM	HEK293 cells	nd	Ye et al., 2015
	l-NBP, d-NBP, ld-NBP	0.06 ± 0.03 μM	CHO cells	nd	Ji et al., 2011
	L-methionine	1 mM	Bladder smooth muscle	nd	Lei et al., 2014
	Lig4-4	2.06 μM	CHO cells	Blocks Kv2.1, Kv1.5, Kv3.1, hERG and neuronal Na⁺ and Ca²⁺channels (IC50 = 30 μM)	Wang et al., 2018