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Amitriptyline

In Vitro Substrates

No substrate information.

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter

Transporter	Synonyms	Inhibitor	IC50 (μM)	Ki (μM)	Substrate used	Cell System	Reference
SLC22A2	OCT2	Amitriptyline	11.3		1-methyl-4-phenylpyridinium (MPP+)	CHO-OCT2	Sandoval, 2018
SLC22A1	OCT1	Amitriptyline	16.9		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	HEK293-OCT1	Ahlin, 2008
SLC22A2	OCT2	Amitriptyline	1.8		4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+)	CHO-OCT2	Sandoval, 2018
ABCC2	MRP2, cMOAT	Amitriptyline	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC3	MRP3	Amitriptyline	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
ABCC4	MRP4	Amitriptyline	>133		Estradiol-17beta-glucuronide	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A1	OCT1	Amitriptyline	6.99		Metformin	HEK293-OCT1	Ahlin, 2010
SLC22A2	OCT2	Amitriptyline	0.51		Metformin	HEK293-OCT2	Hacker, 2015
SLC22A2	OCT2	Amitriptyline	2.4		Metformin	CHO-OCT2	Sandoval, 2018
SLC22A1	OCT1	Amitriptyline	4.4		Morphine	HEK293-OCT1	Tzvetkov, 2013
SLC22A1	OCT1	Amitriptyline	1.89		Morphine	HEK293-OCT1	Zhu, 2018
SLC22A2	OCT2	Amitriptyline	14		N-methylpyridinium	HEK293-OCT2	Zolk, 2009
SLC22A2	OCT2	Amitriptyline	2.5		NBD-MTMA	CHO-OCT2	Belzer, 2013
SLC22A2	OCT2	Amitriptyline	4		NBD-MTMA	CHO-OCT2	Sandoval, 2018
SLC22A1	OCT1	Amitriptyline	58.1		Rhodamine 123	HEK293-OCT1	Jouan, 2014
SLC22A1	OCT1	Amitriptyline	3.47		Sumatriptan	HEK293-OCT1	Matthaei, 2016
ABCB11	BSEP	Amitriptyline	>133		Taurocholate	Sf9 cell membrane vesicles	Morgan, 2013
SLC22A2	OCT2	Amitriptyline	2.4	2.5	Tetraethylammonium	S2-OCT2	Chiba, 2013
SLC22A2	OCT2	Amitriptyline	5		Tetraethylammonium	CHO-OCT2	Sandoval, 2018

No drug-drug interaction information.