1. Kristensen AS, Andersen J, Jørgensen TN, Sørensen L, Eriksen J, Loland CJ, et al. SLC6 neurotransmitter transporters: structure, function, and regulation. Pharmacol Rev. 2011 Sep 1;63(3):585–640. 10.1124/pr.108.000869
2. Kilty JE, Lorang D, Amara SG. Cloning and expression of a cocaine-sensitive rat dopamine transporter. Science (80- ). 1991;254(5031):578–9. 10.1126/science.1948035
3. Shimada S, Kitayama S, Lin CL, Patel A, Nanthakumar E, Gregor P, et al. Cloning and expression of a cocaine-sensitive dopamine transporter complementary DNA. Science (80- ). 1991;254(5031):576–8. 10.1126/science.1948034
4. Giros B, Jaber M, Jones SR, Wightman RM, Caron MG. Hyperlocomotion and indifference to cocaine and amphetamine in mice lacking the dopamine transporter. Nature. 1996;379(6566):606–12. 10.1038/379606a0
5. Penmatsa A, Wang KH, Gouaux E. X-ray structure of dopamine transporter elucidates antidepressant mechanism. Nature. 2013 Nov 15;503(7474):85–90. 10.1038/nature12533
6. Leo D, Sukhanov I, Zoratto F, Illiano P, Caffino L, Sanna F, et al. Pronounced hyperactivity, cognitive dysfunctions, and BDNF dysregulation in dopamine transporter knock-out rats. J Neurosci. 2018 Feb 21;38(8):1959–72. 10.1523/JNEUROSCI.1931-17.2018
7. Mazei-Robison MS, Bowton E, Holy M, Schmudermaier M, Freissmuth M, Sitte HH, et al. Anomalous dopamine release associated with a human dopamine transporter coding variant. J Neurosci. 2008 Jul 9;28(28):7040–6. 10.1523/JNEUROSCI.0473-08.2008
8. Hansen FH, Skjørringe T, Yasmeen S, Arends N V., Sahai MA, Erreger K, et al. Missense dopamine transporter mutations associate with adult parkinsonism and ADHD. J Clin Invest. 2014 Jul 1;124(7):3107–20. 10.1172/JCI73778
9. Bhat S, El-Kasaby A, Freissmuth M, Sucic S. Functional and Biochemical Consequences of Disease Variants in Neurotransmitter Transporters: A Special Emphasis on Folding and Trafficking Deficits. Pharmacol Ther. 2021 Jun 1;222. 10.1016/j.pharmthera.2020.107785
10. Sitte HH, Freissmuth M. Amphetamines, new psychoactive drugs and the monoamine transporter cycle. Trends Pharmacol Sci. 2015;36(1):41–50. 10.1016/j.tips.2014.11.006
11. Ritz MC, Lamb RJ, Goldberg SR, Kuhar MJ. Cocaine receptors on dopamine transporters are related to self-administration of cocaine. Science (80- ). 1987 Sep 4;237(4819):1219–23. 10.1126/science.2820058
12. Bauer C, Banks M, Blough B, Negus S. Use of intracranial self-stimulation to evaluate abuse-related and abuse-limiting effects of monoamine releasers in rats. Br J Pharmacol. 2013 Feb;168(4):850–62. 10.1111/j.1476-5381.2012.02214.x
13. Rothman RB, Partilla JS, Baumann MH, Lightfoot-Siordia C, Blough BE. Studies of the Biogenic Amine Transporters. 14. Identification of Low-Efficacy “Partial” Substrates for the Biogenic Amine Transporters. J Pharmacol Exp Ther. 2012;341(1):251–62. 10.1124/jpet.111.188946
14. Niello M, Gradisch R, Loland CJ, Stockner T, Sitte HH. Allosteric Modulation of Neurotransmitter Transporters as a Therapeutic Strategy. Trends Pharmacol Sci. 2020 May;41(7):446–63. 10.1016/j.tips.2020.04.006
15. Reith MEA, Blough BE, Hong WC, Jones KT, Schmitt KC, Baumann MH, et al. Behavioral, biological, and chemical perspectives on atypical agents targeting the dopamine transporter. Drug Alcohol Depend. 2015;147:1–19. 10.1016/j.drugalcdep.2014.12.005
16. Luethi D, Liechti ME. Designer drugs: mechanism of action and adverse effects. Arch Toxicol. 2020 Apr 6;94(4):1085–133. 10.1007/s00204-020-02693-7
17. Baumann MH, Walters HM, Niello M, Sitte HH. Neuropharmacology of synthetic cathinones. In: Handbook of Experimental Pharmacology. Springer New York LLC; 2018. p. 113–42. 10.1007/164_2018_178
18. Schindler CW, Thorndike EB, Walters HM, Walther D, Rice KC, Baumann MH. Stereoselective neurochemical, behavioral, and cardiovascular effects of α-pyrrolidinovalerophenone enantiomers in male rats. Addict Biol. 2020 Nov 13;25(6). 10.1111/adb.12842
19. Maier J, Rauter L, Rudin D, Niello M, Holy M, Schmid D, et al. α-PPP and its derivatives are selective partial releasers at the human norepinephrine transporter. Neuropharmacology. 2021 Jun;190:108570. 10.1016/j.neuropharm.2021.108570
20. Patocka J, Zhao B, Wu W, Klimova B, Valis M, Nepovimova E, et al. Flakka: New Dangerous Synthetic Cathinone on the Drug Scene. Int J Mol Sci. 2020 Oct 31;21(21). 10.3390/ijms21218185
21. Karila L, Lafaye G, Scocard A, Cottencin O, Benyamina A. MDPV and α-PVP use in humans: The twisted sisters. Neuropharmacology. 2018 May 15;134(Pt A):65–72. 10.1016/j.neuropharm.2017.10.007
22. Umebachi R, Aoki H, Sugita M, Taira T, Wakai S, Saito T, et al. Clinical characteristics of α-pyrrolidinovalerophenone (α-PVP) poisoning. Clin Toxicol. 2016 Aug 8;54(7):563–7. 10.3109/15563650.2016.1166508
23. Crespi C. Flakka-Induced Prolonged Psychosis. Case Rep Psychiatry. 2016;2016:1–2. 10.1155/2016/3460849
24. Volkow ND, Ding YS, Fowler JS, Wang GJ, Logan J, Gatley JS, et al. Is Methylphenidate Like Cocaine?: Studies on Their Pharmacokinetics and Distribution in the Human Brain. Arch Gen Psychiatry. 1995;52(6):456–63. 10.1001/archpsyc.1995.03950180042006
25. Inaba T. Cocaine: Pharmacokinetics and biotransformation in man. Can J Physiol Pharmacol. 1989;67(9):1154–7. 10.1139/y89-184
26. Gannon BM, Baumann MH, Walther D, Jimenez-Morigosa C, Sulima A, Rice KC, et al. The abuse-related effects of pyrrolidine-containing cathinones are related to their potency and selectivity to inhibit the dopamine transporter. Neuropsychopharmacology. 2018 Nov 1;43(12):2399–407. 10.1038/s41386-018-0209-3
27. Gannon BM, Galindo KI, Mesmin MP, Sulima A, Rice KC, Collins GT. Relative reinforcing effects of second-generation synthetic cathinones: Acquisition of self-administration and fixed ratio dose-response curves in rats. Neuropharmacology. 2018 May 15;134(Pt A):28–35. 10.1016/j.neuropharm.2017.08.018
28. Duart-Castells L, Nadal-Gratacós N, Muralter M, Puster B, Berzosa X, Estrada-Tejedor R, et al. Role of amino terminal substitutions in the pharmacological, rewarding and psychostimulant profiles of novel synthetic cathinones. Neuropharmacology. 2021 Mar;186:108475. 10.1016/j.neuropharm.2021.108475
29. Gatch MB, Dolan SB, Forster MJ. Comparative behavioral pharmacology of three pyrrolidine-containing synthetic cathinone derivatives. J Pharmacol Exp Ther. 2015 Aug 1;354(2):103–10. 10.1124/jpet.115.223586
30. H. Brooks W, C. Guida W, G. Daniel K. The Significance of Chirality in Drug Design and Development. Curr Top Med Chem. 2011 Mar 28;11(7):760–70. 10.2174/156802611795165098
31. Gregg RA, Baumann MH, Partilla JS, Bonano JS, Vouga A, Tallarida CS, et al. Stereochemistry of mephedrone neuropharmacology: Enantiomer-specific behavioural and neurochemical effects in rats. Br J Pharmacol. 2015 Feb 1;172(3):883–94. 10.1111/bph.12951
32. Mayer FP, Cintulova D, Pittrich DA, Wimmer L, Luethi D, Holy M, et al. Stereochemistry of phase-1 metabolites of mephedrone determines their effectiveness as releasers at the serotonin transporter. Neuropharmacology. 2019 Apr 1;148:199–209. 10.1016/j.neuropharm.2018.12.032
33. Niello M, Cintulová D, Raithmayr P, Holy M, Jäntsch K, Colas C, et al. Effects of Hydroxylated Mephedrone Metabolites on Monoamine Transporter Activity in vitro. Front Pharmacol. 2021 Apr 9;12. 10.3389/fphar.2021.654061
34. Philogene-Khalid HL, Hicks C, Reitz AB, Liu-Chen L-Y, Rawls SM. Synthetic cathinones and stereochemistry: S enantiomer of mephedrone reduces anxiety- and depressant-like effects in cocaine- or MDPV-abstinent rats. Drug Alcohol Depend. 2017;178:119–25. 10.1016/j.drugalcdep.2017.04.024
35. Mayer FP, Luf A, Nagy C, Holy M, Schmid R, Freissmuth M, et al. Application of a combined approach to identify new psychoactive street drugs and decipher their mechanisms at monoamine transporters. In: Current Topics in Behavioral Neurosciences. 2016. p. 333–50. 10.1007/7854_2016_63
36. Niello M, Cintulova D, Hellsberg E, Jäntsch K, Holy M, Ayatollahi LH, et al. para-Trifluoromethyl-methcathinone is an allosteric modulator of the serotonin transporter. Neuropharmacology. 2019 Apr 24;161:107615. 10.1016/j.neuropharm.2019.04.021
37. Sitte HH, Huck S, Reither H, Boehm S, Singer EA, Pifl C. Carrier-mediated release, transport rates, and charge transfer induced by amphetamine, tyramine, and dopamine in mammalian cells transfected with the human dopamine transporter. J Neurochem. 1998 Nov 13;71(3):1289–97. 10.1046/j.1471-4159.1998.71031289.x
38. Bulling S, Schicker K, Zhang YW, Steinkellner T, Stockner T, Gruber CW, et al. The mechanistic basis for noncompetitive ibogaine inhibition of serotonin and dopamine transporters. J Biol Chem. 2012;287(22):18524–34. 10.1074/jbc.M112.343681
39. Hasenhuetl PS, Bhat S, Mayer FP, Sitte HH, Freissmuth M, Sandtner W. A kinetic account for amphetamine-induced monoamine release. J Gen Physiol. 2018 Feb 9;150(3):431–51. 10.1085/jgp.201711915
40. Hoffman AF, Spivak CE, Lupica CR. Enhanced dopamine release by dopamine transport inhibitors described by a restricted diffusion model and fast-scan cyclic voltammetry. ACS Chem Neurosci. 2016;7(6):700–9. 10.1021/acschemneuro.5b00277
41. Steinkellner T, Mus L, Eisenrauch B, Constantinescu A, Leo D, Konrad L, et al. In Vivo Amphetamine Action is Contingent on αCaMKII. Neuropsychopharmacology. 2014 Oct 29;39(11):2681–93. 10.1038/npp.2014.124
42. Gabriel MO, Nikou M, Akinola OB, Pollak DD, Sideromenos S. Western diet-induced fear memory impairment is attenuated by 6-shogaol in C57BL/6N mice. Behav Brain Res. 2020 Feb 17;380. 10.1016/j.bbr.2019.112419
43. Krueger BK. Kinetics and Block of Dopamine Uptake in Synaptosomes from Rat Caudate Nucleus. J Neurochem. 1990;55(1):260–7. 10.1111/j.1471-4159.1990.tb08847.x
44. Beuming T, Kniazeff J, Bergmann ML, Shi L, Gracia L, Raniszewska K, et al. The binding sites for cocaine and dopamine in the dopamine transporter overlap. Nat Neurosci. 2008 Jul 22;11(7):780–9. 10.1038/nn.2146
45. Wang KH, Penmatsa A, Gouaux E. Neurotransmitter and psychostimulant recognition by the dopamine transporter. Nature. 2015;521(7552):322–7. 10.1038/nature14431
46. Plenge P, Abramyan AM, Sørensen G, Mørk A, Weikop P, Gether U, et al. The mechanism of a high-affinity allosteric inhibitor of the serotonin transporter. Nat Commun. 2020 Dec 20;11(1):1491. 10.1038/s41467-020-15292-y
47. Rang HP. The kinetics of action of acetylcholine antagonists in smooth muscle. Proc R Soc Lond B Biol Sci. 1966;164(996):488–510. 10.1098/rspb.1966.0045
48. Kenakin T. Overview of receptor interactions of agonists and antagonists. In: Current Protocols in Pharmacology. Curr Protoc Pharmacol; 2008. 10.1002/0471141755.ph0401s42
49. Lew MJ, Ziogas J, Christopoulos A. Dynamic mechanisms of non-classical antagonism by competitive AT1 receptor antagonists. Trends Pharmacol Sci. 2000 Oct 1;21(10):376–81. 10.1016/S0165-6147(00)01523-6
50. Hasenhuetl PS, Schicker K, Koenig X, Li Y, Sarker S, Stockner T, et al. Ligand Selectivity among the Dopamine and Serotonin Transporters Specified by the Forward Binding Reaction. Mol Pharmacol. 2015 May 18;88(1):12–8. 10.1124/mol.115.099036
51. Erreger K, Grewer C, Javitch JA, Galli A. Currents in response to rapid concentration jumps of amphetamine uncover novel aspects of human dopamine transporter function. J Neurosci. 2008 Jan 23;28(4):976–89. 10.1523/JNEUROSCI.2796-07.2008
52. Li Y, Mayer FP, Hasenhuetl PS, Burtscher V, Schicker K, Sitte HH, et al. Occupancy of the zinc-binding site by transition metals decreases the substrate affinity of the human dopamine transporter by an allosteric mechanism. J Biol Chem. 2017 Apr 28;292(10):4235–43. 10.1074/jbc.M116.760140
53. Wee S, Anderson KG, Baumann MH, Rothman RB, Blough BE, Woolverton WL. Relationship between the serotonergic activity and reinforcing effects of a series of amphetamine analogs. J Pharmacol Exp Ther. 2005 May 17;313(2):848–54. 10.1124/jpet.104.080101
54. Newman AH, Kulkarni S. Probes for the dopamine transporter: New leads toward a cocaine-abuse therapeutic - A focus on analogues of benztropine and rimcazole. Med Res Rev. 2002 Sep;22(5):429–64. 10.1002/med.10014
55. Copeland RA. The drug-target residence time model: A 10-year retrospective. Nat Rev Drug Discov. 2016 Feb 3;15(2):87–95. 10.1038/nrd.2015.18
56. Copeland RA, Pompliano DL, Meek TD. Drug-target residence time and its implications for lead optimization. Nat Rev Drug Discov. 2006;5(9):730–9. 10.1038/nrd2082
57. IJzerman AP, Guo D. Drug–Target Association Kinetics in Drug Discovery. Vol. 44, Trends in Biochemical Sciences. Elsevier Ltd; 2019. p. 861–71. 10.1016/j.tibs.2019.04.004
58. Plenge P, Mellerup ET. An affinity-modulating site on neuronal monoamine transport proteins. Pharmacol Toxicol. 1997 Apr;80(4):197–201.
59. Desai RI, Kopajtic TA, Koffarnus M, Newman AH, Katz JL. Identification of a dopamine transporter ligand that blocks the stimulant effects of cocaine. J Neurosci. 2005 Feb 23;25(8):1889–93. 10.1523/JNEUROSCI.4778-04.2005
60. Nóbrega L, Dinis-Oliveira RJ. The synthetic cathinone α-pyrrolidinovalerophenone (α-PVP): pharmacokinetic and pharmacodynamic clinical and forensic aspects. Drug Metab Rev. 2018 Apr 3;50(2):125–39. 10.1080/03602532.2018.1448867
61. Coleman JA, Green EM, Gouaux E. X-ray structures and mechanism of the human serotonin transporter. Nature. 2016;532(7599):334–9. 10.1038/nature17629
62. Larsen MB, Sonders MS, Mortensen O V., Larson GA, Zahniser NR, Amara SG. Dopamine Transport by the Serotonin Transporter: A Mechanistically Distinct Mode of Substrate Translocation. J Neurosci. 2011;31(17):6605–15. 10.1523/JNEUROSCI.0576-11.2011
63. Grouleff J, Ladefoged LK, Koldsø H, Schiøtt B. Monoamine transporters: Insights from molecular dynamics simulations. Front Pharmacol. 2015;6(OCT). 10.3389/fphar.2015.00235
64. Cheng MH, Bahar I. Monoamine transporters: structure, intrinsic dynamics and allosteric regulation. Nat Struct Mol Biol. 2019 Jul 3;26(7):545–56. 10.1038/s41594-019-0253-7
65. Penmatsa A, Wang KH, Gouaux E. X-ray structures of Drosophila dopamine transporter in complex with nisoxetine and reboxetine. Nat Struct Mol Biol. 2015 Jun 3;22(6):506–8. 10.1038/nsmb.3029
66. Jacobs MT, Zhang YW, Campbell SD, Rudnick G. Ibogaine, a noncompetitive inhibitor of serotonin transport, acts by stabilizing the cytoplasm-facing state of the transporter. J Biol Chem. 2007 Oct 5;282(40):29441–7. 10.1074/jbc.M704456200
67. Coleman JA, Yang D, Zhao Z, Wen PC, Yoshioka C, Tajkhorshid E, et al. Serotonin transporter–ibogaine complexes illuminate mechanisms of inhibition and transport. Nature. 2019 May 24;569(7754):141–5. 10.1038/s41586-019-1135-1
68. Wacker D, Wang S, McCorvy JD, Betz RM, Venkatakrishnan AJ, Levit A, et al. Crystal Structure of an LSD-Bound Human Serotonin Receptor. Cell. 2017 Jan 26;168(3):377-389.e12. 10.1016/j.cell.2016.12.033
69. Tonge PJ. Drug-Target Kinetics in Drug Discovery. ACS Chem Neurosci. 2018 Jan 17;9(1):29–39. 10.1021/acschemneuro.7b00185
70. Collins GT, Sulima A, Rice KC, France CP. Self-administration of the synthetic cathinones 3,4-methylenedioxypyrovalerone (MDPV) and α-pyrrolidinopentiophenone (α-PVP) in rhesus monkeys. Psychopharmacology (Berl). 2019 Dec 1;236(12):3677–85. 10.1007/s00213-019-05339-4
71. Schroeder C, Jordan J. Norepinephrine transporter function and human cardiovascular disease. Am J Physiol - Hear Circ Physiol. 2012 Dec 1;303(11). 10.1152/ajpheart.00492.2012
72. Mackie P, Lebowitz J, Saadatpour L, Nickoloff E, Gaskill P, Khoshbouei H. The dopamine transporter: An unrecognized nexus for dysfunctional peripheral immunity and signaling in Parkinson’s Disease. Brain Behav Immun. 2018 May 1;70:21–35. 10.1016/j.bbi.2018.03.020
73. Harris RC, Zhang MZ. Dopamine, the kidney, and hypertension. Curr Hypertens Rep. 2012 Apr;14(2):138–43. 10.1007/s11906-012-0253-z
74. Bull DR, Palij P, Sheehan MJ, Millar J, Stamford JA, Kruk ZL, et al. Application of fast cyclic voltammetry to measurement of electrically evoked dopamine overflow from brain slices in vitro. J Neurosci Methods. 1990;32(1):37–44. 10.1016/0165-0270(90)90069-R
75. Baumann MH, Partilla JS, Lehner KR, Thorndike EB, Hoffman AF, Holy M, et al. Powerful cocaine-like actions of 3,4-methylenedioxypyrovalerone (MDPV), a principal constituent of psychoactive “bath salts” products. Neuropsychopharmacology. 2013;38(4):552–62. 10.1038/npp.2012.204