TABLE 1.

List of some DAT substrates/inhibitors with their preferential binding site and DAT’s conformational state.

Ligand	Site Preference	Configuration preference
Allotropacocaine		Closed/inward-facing Schmitt et al. (2013)
Amphetamine	S1 Wang et al. (2015)	Closed Cheng et al. (2015)
Benztropinamines	S1 Zou et al. (2017)	Induce inward-open Zou et al. (2017)
Benztropines analogs	S1, S2 Bisgaard et al. (2011)	Occluded Loland et al. (2008)
Bupropion		Closed/inward -facing Schmitt et al. (2013)
Cocaine and cocaine analogs	S1, S2 Beuming et al. (2008)	Outward-open Beuming et al. (2008)
Dopamine	Orthosteric Cheng et al. (2015)	Occluded Cheng et al. (2015)
GBR12909		Closed/inward facing Schmitt et al. (2013)
Ibogaine	S2 (Bulling et al., (2012)	Inward-open Bulling et al. (2012)
JHW007	S1 Bisgaard et al. (2011)	Closed/inward -facing Schmitt et al. (2013)
KM822	Allosteric Aggarwal et al. (2019)	Outward-open Aggarwal et al. (2019)
MDPV	S1 Steele et al. (2021)	Outward-open Steele et al. (2021)
Methamphetamine	S1 Wang et al. (2015)	Outward-open Wang et al. (2015)
Methylphenidate	S1 Foroughi et al. (2020)	Outward-open Schmitt and Reith, (2011)
MFZ 2–24	S1 Krout et al. (2017)	Outward-open Krout et al. (2017)
(±)-modafinil	S1 Schmitt and Reith, (2011)	Occluded Nikiforuk et al. (2017)
MRS7292	Allosteric Navratna et al. (2018)	Outward-open Navratna et al. (2018)
Nisoxetine	S1 Penmatsa et al. (2015)	Outward-open Penmatsa et al. (2015)
Nortriptyline	S1 Penmatsa et al. (2013)	Outward-open Penmatsa et al. (2013)
Orphenadrine	S1 Cheng et al. (2015)	Outward-open Cheng et al. (2015)
Reboxetine	S1 Penmatsa et al. (2015)	Outward-open Penmatsa et al. (2015)
Rimcazole		Closed/inward-facing Schmitt et al. (2013)
Rimcazole analogs		Occluded Loland et al. (2008)
RTI 82	S1 Dahal et al. (2014)	Outward-open Dahal et al. (2014)
SRI-31142	Allosteric Moerke et al. (2018)	Inward-facing Moerke et al. (2018)
Sydnocarb	Allosteric near EC Aggarwal et al. (2021)	Outward-open Aggarwal et al. (2021)
Tamoxifen	S2 site Mikelman et al. (2018)	Outward open Mikelman et al. (2018)
WIN 35, 428	S1 Beuming et al. (2008)	Outward-open Schmitt and Reith, (2011)