A Comprehensive In Vitro Screening of d-, l- , and dl-threo -Methylphenidate: An Exploratory Study
Abstract
dl-Methylphenidate (MPH) has been widely used to treat attention-deficit/hyperactivity disorder (ADHD) for the last half century. It had been exclusively available in the racemic form, i.e., a 50:50 mixture of d- and l-isomers. However, a single enantiomer formulation, d-MPH (dexmethylphenidate), became available for general clinical use in 2002. For this reason, the intrinsic pharmacological differences in the effects of d- and l-MPH have recently come under intense investigation. The primary therapeutic effects of MPH are generally recognized to reside in the d-isomer. The present investigation provides quantitative values for a broad range of receptor-level interactions of the individual MPH isomers to better characterize the distinction between dl-MPH versus d-MPH versus l-MPH as it relates to binding affinity at sites associated with relevant central nervous system (CNS) pharmacology, as well as peripheral physiology. Overall, there were few differences in binding affinities between d-MPH and the racemate whereas there were more apparent differences between d-MPH and l-MPH. d-MPH exhibited prominent affinity at the norepinephrine transporter (NET) site, even exceeding such affinity at the dopamine transporter (DAT). These results further demonstrate that affinity for catecholaminergic sites largely resides in the d-MPH isomer. Although binding affinity was not demonstrable at the serotonin (5-HT) transporter site (SERT), novel findings of the study included affinity for…
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MPH acts as an agonist for the 5-hydroxytryptamine (serotonin) receptor 1A (HTR1A).
“and as an agonist for the 5-hydroxytryptamine (serotonin) receptor 1A (HTR1A) [140, 141].”
From Molecular Characterisation of the Mechanism of Action of Stimulant Drugs Lisdexamfetamine and Methylphenidate on ADHD Neurobiology: A Review (2022) · cites this paper as [140]
MPH activates HTR1A, which induces a partial release of DA, thereby improving presynaptic signalling.
“MPH activates HTR1A [140, 141], which induces a partial release of DA, thereby improving the presynaptic signalling.”
From Molecular Characterisation of the Mechanism of Action of Stimulant Drugs Lisdexamfetamine and Methylphenidate on ADHD Neurobiology: A Review (2022) · cites this paper as [140]
Cites
Yung-Chi, C., & Prusoff, W. H. (1973) · Biochemical Pharmacology · doi:10.1016/0006-2952(73)90196-2 · Cited by 12,922 · see citing works
A review of central 5-HT receptors and their function
Barnes, N. M., & Sharp, T. (1999) · Neuropharmacology · doi:10.1016/s0028-3908(99)00010-6 · Cited by 3,150 · see citing works
Molecular genetics of attention-deficit/hyperactivity disorder
Faraone, S. V., Perlis, R. H., Doyle, A. E., Smoller, J. W., Goralnick, J. J., Holmgren, M. A., & Sklar, P. (2005) · Biological Psychiatry · doi:10.1016/j.biopsych.2004.11.024 · Cited by 2,357 · see citing works
Attention-Deficit/Hyperactivity Disorder: A Selective Overview
Biederman, J. (2004) · Biological Psychiatry · doi:10.1016/j.biopsych.2004.10.020 · Cited by 1,343 · see citing works
General hospital psychiatry: the Italian experience.
Faraone, S. V., Sergeant, J. A., Gillberg, C., & Biederman, J. (2003) · Europe PMC (PubMed Central) · Cited by 1,277 · see citing works
Barkley, R. A., Fischer, M., Smallish, L., & Fletcher, K. (2002) · Journal of Abnormal Psychology · doi:10.1037/0021-843x.111.2.279 · Cited by 1,199 · see citing works
Bymaster, F. (2002) · Neuropsychopharmacology · doi:10.1016/s0893-133x(02)00346-9 · Cited by 1,123 · see citing works
Committee on Quality Improvement, S. O. A.-D. D. (2000) · Pediatrics · doi:10.1542/peds.105.5.1158 · Cited by 1,076 · see citing works
Rothman, R. B., Baumann, M. H., Dersch, C. M., Romero, D. V., Rice, K. C., Carroll, F. I., & Partilla, J. S. (2000) · Synapse · doi:10.1002/1098-2396(20010101)39:1 · Cited by 934 · see citing works
Role of Serotonin in the Paradoxical Calming Effect of Psychostimulants on Hyperactivity
Gainetdinov, R. R., Wetsel, W. C., Jones, S. R., Levin, E. D., Jaber, M., & Caron, M. G. (1999) · Science · doi:10.1126/science.283.5400.397 · Cited by 885 · see citing works
Solanto, M. V. (1998) · Behavioural Brain Research · doi:10.1016/s0166-4328(97)00175-7 · Cited by 677 · see citing works
Kuczenski, R., & Segal, D. S. (1997) · Journal of Neurochemistry · doi:10.1046/j.1471-4159.1997.68052032.x · Cited by 623 · see citing works
Attention-deficit/hyperactivity disorder (adhd) as a noradrenergic disorder
Biederman, J., & Spencer, T. J. (1999) · Biological Psychiatry · doi:10.1016/s0006-3223(99)00192-4 · Cited by 513 · see citing works
The Dopamine Transporter and Attention-Deficit/Hyperactivity Disorder
Madras, B. K., Miller, G. M., & Fischman, A. J. (2005) · Biological Psychiatry · doi:10.1016/j.biopsych.2004.10.011 · Cited by 393 · see citing works
The neuropsychopharmacology of attention-deficit/hyperactivity disorder
Pliszka, S. R. (2005) · Biological Psychiatry · doi:10.1016/j.biopsych.2004.08.026 · Cited by 276 · see citing works
Kuczenski, R. T., & Segal, D. S. (2001) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)38829-9 · Cited by 267 · see citing works
A review of the role of serotonin receptors in psychiatric disorders
Naughton, M., Mulrooney, J. B., & Leonard, B. E. (2000) · Human Psychopharmacology Clinical and Experimental · doi:10.1002/1099-1077(200008)15:6 · Cited by 258 · see citing works
Evidence-based pharmacotherapy for attention-deficit hyperactivity disorder
Biederman, J., Spencer, T., & Wilens, T. (2004) · The International Journal of Neuropsychopharmacology · doi:10.1017/s1461145703003973 · Cited by 253 · see citing works
Leonard, B. E., McCartan, D., White, J., & King, D. J. (2004) · Human Psychopharmacology Clinical and Experimental · doi:10.1002/hup.579 · Cited by 242 · see citing works
Keating, G. M., & Figgitt, D. P. (2002) · Drugs · doi:10.2165/00003495-200262130-00009 · Cited by 201 · see citing works
Pharmacology of the enantiomers of threo-methylphenidate.
Patrick, K. S., Caldwell, R. W., Ferris, R. M., & Breese, G. R. (1987) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-5347(25)00340-4 · Cited by 196 · see citing works
Self-citationWall, S. C., Gu, H., & Rudnick, G. (1995) · Molecular Pharmacology · doi:10.1016/s0026-895x(25)08574-8 · Cited by 183 · see citing works
Human 5-HT1A receptor C(−1019)G polymorphism and psychopathology
Huang, Y., Battistuzzi, C., Oquendo, M. A., Harkavy‐Friedman, J., Greenhill, L. L., Zalsman, G., Brodsky, B. S., Arango, V., Brent, D. A., & Mann, J. J. (2004) · The International Journal of Neuropsychopharmacology · doi:10.1017/s1461145704004663 · Cited by 182 · see citing works
The dopamine transporter and neuroimaging in attention deficit hyperactivity disorder
Krause, K.-H., Dresel, S. H. J., Krause, J., la Fougère, C. J., & Ackenheil, M. (2003) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2003.08.012 · Cited by 181 · see citing works
Markowitz, J. S., Straughn, A. B., & Patrick, K. S. (2003) · Pharmacotherapy The Journal of Human Pharmacology and Drug Therapy · doi:10.1592/phco.23.12.1281.32697 · Cited by 174 · see citing works
Self-citationComings, D., Gade-Andavolu, R., Gonzalez, N., Wu, S.-J., Muhleman, D., Blake, H., Dietz, G., Saucier, G., & MacMurray, J. P. (2000) · Clinical Genetics · doi:10.1034/j.1399-0004.2000.570304.x · Cited by 159 · see citing works
Influence of Ethanol and Gender on Methylphenidate Pharmacokinetics and Pharmacodynamics
Patrick, K. S., Straughn, A. B., Minhinnett, R., Yeatts, S. D., Herrin, A. E., DeVane, C. L., Malcolm, R. J., Janis, G. C., & Markowitz, J. S. (2007) · Clinical Pharmacology & Therapeutics · doi:10.1038/sj.clpt.6100082 · Cited by 137 · see citing works
Self-citationSrinivas, N. R., Hubbard, J. W., Quinn, D., & Midha, K. K. (1992) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.1992.185 · Cited by 120 · see citing works
Enantioselective Pharmacokinetics of dl-threo-Methylphenidate in Humans
Srinivas, N. R., Hubbard, J. W., Korchinski, E. D., & Midha, K. K. (1993) · Pharmaceutical Research · doi:10.1023/a:1018956526016 · Cited by 105 · see citing works
Association of Norepinephrine Transporter Gene With Methylphenidate Response
Yang, L., Wang, Y., Li, J., & Faraone, S. V. (2004) · Journal of the American Academy of Child & Adolescent Psychiatry · doi:10.1097/01.chi.0000131134.63368.46 · Cited by 97 · see citing works
Genetics of Childhood Disorders: XXIII. ADHD, Part 7: The Serotonin System
Quist, J. F., & Kennedy, J. L. (2001) · Journal of the American Academy of Child & Adolescent Psychiatry · doi:10.1097/00004583-200102000-00022 · Cited by 94 · see citing works
Davids, E., Zhang, K., Kula, N. S., Tarazi, F. I., & Baldessarini, R. J. (2002) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.301.3.1097 · Cited by 91 · see citing works
Davids, E., Zhang, K., Tarazi, F. I., & Baldessarini, R. J. (2002) · Psychopharmacology · doi:10.1007/s00213-001-0962-5 · Cited by 76 · see citing works
Synthesis and pharmacology of hydroxylated metabolites of methyl phenidate
Patrick, K. S., Kilts, C. D., & Breese, G. R. (1981) · Journal of Medicinal Chemistry · doi:10.1021/jm00142a021 · Cited by 72 · see citing works
Self-citationDiscriminative Stimulus Properties of Cocaine: Enhancement by Monoamine Reuptake Blockers
Kleven, M. S., & Koek, W. (1998) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(24)37310-0 · Cited by 67 · see citing works
New methylphenidate formulations for the treatment of attention-deficit/hyperactivity disorder
Patrick, K. S., Ángel-González, M., Straughn, A. B., & Markowitz, J. S. (2005) · Expert Opinion on Drug Delivery · doi:10.1517/17425247.2.1.121 · Cited by 58 · see citing works
Self-citationBinding of bromine-substituted analogs of methylphenidate to monoamine transporters
Pan, D., Gatley, S. J., Dewey, S. L., Chen, R., Alexoff, D., Ding, Y., & Fowler, J. S. (1994) · European Journal of Pharmacology · doi:10.1016/0014-2999(94)00460-9 · Cited by 56 · see citing works
Mester, Z., & Pawliszyn, J. B. (1999) · Rapid Communications in Mass Spectrometry · doi:10.1002/(sici)1097-0231(19991030)13:20 · Cited by 55 · see citing works
Attention-deficit hyperactivity disorder and the gene for the dopamine D5 receptor
Barr, C. L., Wigg, K., Feng, Y., Zai, G. C., MALONE, M. A., Roberts, W., Schachar, R. J., Tannock, R., & Kennedy, J. L. (2000) · Molecular Psychiatry · doi:10.1038/sj.mp.4000777 · Cited by 55 · see citing works
Brain kinetics of methylphenidate (Ritalin) enantiomers after oral administration
Ding, Y., Gatley, S. J., Thanos, P. K., Shea, C. E., Garza, V., Xu, Y., Carter, P., King, P. T., Warner, D., Taintor, N. B., et al. (2004) · Synapse · doi:10.1002/syn.20046 · Cited by 53 · see citing works
Modi, N. B., Wang, B., Noveck, R. J., & Gupta, S. (2000) · The Journal of Clinical Pharmacology · doi:10.1177/009127000004001008 · Cited by 50 · see citing works
D ‐methylphenidate and D , L ‐methylphenidate are not developmental toxicants in rats and rabbits
Teo, S. K., Stirling, D., Hoberman, A. M., Christian, M. S., Thomas, S. D., & Khetani, V. D. (2003) · Birth Defects Research Part B Developmental and Reproductive Toxicology · doi:10.1002/bdrb.10018 · Cited by 32 · see citing works
Srinivas, N. R., Hubbard, J. W., McKay, G., Hawes, E. M., & Midha, K. K. (1991) · Chirality · doi:10.1002/chir.530030204 · Cited by 26 · see citing works
Kleven, M. S., Prinssen, E. P. M., & Koek, W. (1996) · European Journal of Pharmacology · doi:10.1016/0014-2999(96)00498-0 · Cited by 26 · see citing works
High throughput drug profiling
Entzeroth, M., Chapelain, B., Guilbert, J., & Hamon, V. (2000) · Journal of Analytical Methods in Chemistry · doi:10.1155/s1463924600000304 · Cited by 7 · see citing works
Flagged first, then by citations
2 of the 47 references couldn’t be matched to a known paper.
Cited by
Sorted by citations
Faraone, S. V. (2018) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2018.02.001 · Cited by 631 · see citing works
The solute carrier 6 family of transporters
Bröer, S., & Gether, U. (2012) · British Journal of Pharmacology · doi:10.1111/j.1476-5381.2012.01975.x · Cited by 274 · see citing works
Checa-Ros, A., Jeréz-Calero, A., Molina-Carballo, A., Campoy, C., & Muñoz-Hoyos, A. (2021) · Nutrients · doi:10.3390/nu13010249 · Cited by 164 · see citing works
Mechanisms of Action and Persistent Neuroplasticity by Drugs of Abuse
Korpi, E. R., den Hollander, B., Farooq, U., Vashchinkina, E., Rajkumar, R., Nutt, D. J., Hyytiä, P., & Dawe, G. S. (2015) · Pharmacological Reviews · doi:10.1124/pr.115.010967 · Cited by 148 · see citing works
Hodgkins, P., Shaw, M., Coghill, D., & Hechtman, L. (2012) · European Child & Adolescent Psychiatry · doi:10.1007/s00787-012-0286-5 · Cited by 147 · see citing works
Brown, J. A., Emnett, R. J., White, C. R., Yuede, C. M., Conyers, S. B., O’Malley, K. L., Wozniak, D. F., & Gutmann, D. H. (2010) · Human Molecular Genetics · doi:10.1093/hmg/ddq382 · Cited by 140 · see citing works
Triple uptake inhibitors: therapeutic potential in depression and beyond
Chen, Z., & Skolnick, P. (2007) · Expert Opinion on Investigational Drugs · doi:10.1517/13543784.16.9.1365 · Cited by 108 · see citing works
Pharmacology of Drugs Used as Stimulants
Docherty, J. R., & Alsufyani, H. A. (2021) · The Journal of Clinical Pharmacology · doi:10.1002/jcph.1918 · Cited by 97 · see citing works
Methylphenidate facilitates learning-induced amygdala plasticity
Tye, K. M., Tye, L. D., Cone, J. J., Hekkelman, E. F., Janak, P. H., & Bonci, A. (2010) · Nature Neuroscience · doi:10.1038/nn.2506 · Cited by 89 · see citing works
Methylphenidate for attention-deficit/hyperactivity disorder in adults: a narrative review
Jaeschke, R. R., Sujkowska, E., & Sowa-Kućma, M. (2021) · Psychopharmacology · doi:10.1007/s00213-021-05946-0 · Cited by 90 · see citing works
Differential Pharmacokinetics and Pharmacodynamics of Methylphenidate Enantiomers
Markowitz, J. S., & Patrick, K. S. (2008) · Journal of Clinical Psychopharmacology · doi:10.1097/jcp.0b013e3181733560 · Cited by 74 · see citing works
Self-citationQuintero, J., Gutiérrez-Casares, J. R., & Álamo, C. (2022) · Neurology and Therapy · doi:10.1007/s40120-022-00392-2 · Cited by 70 · see citing works
“On the other hand, MPH activates HTR1A and DRD2 (and potentially other G-coupled receptors) that might have a reinforcing feedback role on MPH modulation of the NT imbalance through further regulation of DAT1 [174].”
BackgroundInfluentialThe psychostimulant d-threo-(R,R)-methylphenidate binds as an agonist to the 5HT1A receptor
Markowitz, J. S., Markowitz, J. S., DeVane, C. L., Ramamoorthy, S., Zhu, H.-J., & Zhu, H.-J. (2009) · Die Pharmazie · doi:10.31083/ph.2009.8691 · Cited by 68 · see citing works
Self-citationSex Differences in the Response of Children With ADHD to Once-Daily Formulations of Methylphenidate
Sonuga-Barke, E. J. S., Coghill, D., Markowitz, J. S., Swanson, J. M., Vandenberghe, M., & HATCH, S. J. (2007) · Journal of the American Academy of Child & Adolescent Psychiatry · doi:10.1097/chi.0b013e31804659f1 · Cited by 66 · see citing works
Self-citationEconomidou, D., Dalley, J. W., & Everitt, B. J. (2010) · Biological Psychiatry · doi:10.1016/j.biopsych.2010.09.040 · Cited by 63 · see citing works
Frati, P., Kyriakou, C., RIO, A. D., Marinelli, E., Vergallo, G. M., Zaami, S., & Busardò, F. P. (2014) · Current Neuropharmacology · doi:10.2174/1570159x13666141210221750 · Cited by 60 · see citing works
Bisagno, V., González, B., & Urbano, F. J. (2016) · Pharmacological Research · doi:10.1016/j.phrs.2016.01.013 · Cited by 59 · see citing works
Secondary pharmacology: screening and interpretation of off-target activities – focus on translation
Whitebread, S., Dumotier, B. M., Armstrong, D., Fekete, A., Chen, S., Hartmann, A., Muller, P. Y., & Urbán, L. (2016) · Drug Discovery Today · doi:10.1016/j.drudis.2016.04.021 · Cited by 59 · see citing works
From Clinical Application to Cognitive Enhancement: The Example of Methylphenidate
Busardò, F., Kyriakou, C., Cipolloni, L., Zaami, S., & Frati, P. (2016) · Current Neuropharmacology · doi:10.2174/1570159x13666150407225902 · Cited by 52 · see citing works
New Formulations of Stimulants: An Update for Clinicians
Steingard, R. J., Taskiran, S. A., Connor, D. F., Markowitz, J. S., & Stein, M. A. (2019) · Journal of Child and Adolescent Psychopharmacology · doi:10.1089/cap.2019.0043 · Cited by 52 · see citing works
Self-citationEstrogens of multiple classes and their role in mental health disease mechanisms
Watson, C. S. (2010) · International Journal of Women s Health · doi:10.2147/ijwh.s6907 · Cited by 52 · see citing works
Luppi, A. I., Singleton, S. P., Hansen, J. Y., Jamison, K. W., Bzdok, D., Kuceyeski, A. F., Betzel, R. F., & Mišić, B. (2024) · Nature Biomedical Engineering · doi:10.1038/s41551-024-01242-2 · Cited by 56 · see citing works
Unravelling the effects of methylphenidate on the dopaminergic and noradrenergic functional circuits
Dipasquale, O., Martins, D., Sethi, A., Veronese, M., Hesse, S., Rullmann, M., Sabri, O., Turkheimer, F., Harrison, N. A., Mehta, M. A., et al. (2020) · Neuropsychopharmacology · doi:10.1038/s41386-020-0724-x · Cited by 45 · see citing works
Neuropharmacological Mechanisms Underlying the Neuroprotective Effects of Methylphenidate
Volz, T. (2008) · Current Neuropharmacology · doi:10.2174/157015908787386041 · Cited by 46 · see citing works
Muniz, R., Brams, M. N., Mao, A. R., McCague, K., Pestreich, L. K., & Silva, R. (2008) · Journal of Child and Adolescent Psychopharmacology · doi:10.1089/cap.2007.0015 · Cited by 43 · see citing works
Self-citationBrams, M. N., Muniz, R., Childress, A. C., Giblin, J. M., Mao, A. R., Turnbow, J. M., Borrello, M., McCague, K., López, F. A., & Silva, R. (2008) · CNS Drugs · doi:10.2165/00023210-200822080-00006 · Cited by 42 · see citing works
Self-citationEvolution of stimulants to treat ADHD: transdermal methylphenidate
Patrick, K. S., Straughn, A. B., Perkins, J. S., & Ángel-González, M. (2008) · Human Psychopharmacology Clinical and Experimental · doi:10.1002/hup.992 · Cited by 42 · see citing works
Self-citationMonoamine Reuptake Inhibitors in Parkinson’s Disease
Huot, P., Fox, S. H., & Brotchie, J. M. (2015) · Parkinson s Disease · doi:10.1155/2015/609428 · Cited by 39 · see citing works
Zhu, H., Patrick, K. S., & Markowitz, J. S. (2011) · Journal of Chromatography B · doi:10.1016/j.jchromb.2011.02.033 · Cited by 38 · see citing works
Self-citationAndersen, S. L., & Navalta, C. P. (2011) · Journal of Child Psychology and Psychiatry · doi:10.1111/j.1469-7610.2011.02376.x · Cited by 38 · see citing works
Volz, T. J., Farnsworth, S. J., Rowley, S. D., Hanson, G. R., & Fleckenstein, A. E. (2008) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.139386 · Cited by 37 · see citing works
Methylphenidate off-label use and safety
Trenque, T. C., Herlem, E., Taam, M. A., & Dramé, M. (2014) · SpringerPlus · doi:10.1186/2193-1801-3-286 · Cited by 35 · see citing works
Stevens, T., Sangkuhl, K., Brown, J. T., Altman, R. B., & Klein, T. E. (2019) · Pharmacogenetics and Genomics · doi:10.1097/fpc.0000000000000376 · Cited by 34 · see citing works
Recent Advances and Challenges of the Drugs Acting on Monoamine Transporters
Xue, W., Fu, T., Zheng, G., Tu, G., Zhang, Y., Yang, F., Tao, L., Yao, L., & Zhu, F. (2018) · Current Medicinal Chemistry · doi:10.2174/0929867325666181009123218 · Cited by 32 · see citing works
Batalhão, I. G., Lima, D., Russi, A. P. M., Boscolo, C. N. P., da Silva, D. G. H., Pereira, T. S. B., Bainy, A. C. D., & de Almeida, E. A. (2019) · Fish Physiology and Biochemistry · doi:10.1007/s10695-019-00645-2 · Cited by 30 · see citing works
Neurobiology of Attention Deficit Hyperactivity Disorder
Faraone, S. V., & Radonjić, N. V. (2023) · Springer eBooks · doi:10.1007/978-3-030-42825-9_33-1 · Cited by 31 · see citing works
Park, S., Kim, B.-N., Cho, S.-C., Kim, J.-W., Kim, J. I., Shin, M., Yoo, H., Han, D. H., & Cheong, J. H. (2014) · Journal of Child and Adolescent Psychopharmacology · doi:10.1089/cap.2013.0079 · Cited by 28 · see citing works
Moen, M. D., & Keam, S. J. (2009) · CNS Drugs · doi:10.2165/11201140-000000000-00000 · Cited by 27 · see citing works
Role of echocardiography in toxic heart valvulopathy
Droogmans, S., Kerkhove, D., Cosyns, B., & Camp, G. V. (2009) · European Journal of Echocardiography · doi:10.1093/ejechocard/jep023 · Cited by 27 · see citing works
Cummins, T. D. R., Jacoby, O., Hawi, Z., Nandam, L. S., Byrne, M., Kim, B.-N., Wagner, J., Chambers, C., & Bellgrove, M. A. (2013) · Molecular Psychiatry · doi:10.1038/mp.2013.140 · Cited by 26 · see citing works
Fazelipour, S., Jahromy, M. H., Tootian, Z., Kiaei, S. B., Sheibani, M. T., & Talaee, N. (2012) · Europe PMC (PubMed Central) · Cited by 26 · see citing works
Angyal, N., Horvath, E. Z., Tarnok, Z., Richman, M. J., Bognar, E., Lakatos, K., Sasvari-Szekely, M., & Nemoda, Z. (2018) · Progress in Neuro-Psychopharmacology and Biological Psychiatry · doi:10.1016/j.pnpbp.2018.01.013 · Cited by 25 · see citing works
Huot, P., Fox, S. H., & Brotchie, J. M. (2016) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.116.232371 · Cited by 25 · see citing works
Gutiérrez-Casares, J. R., Quintero, J., Jorba, G., Junet, V., Martínez, V., Pozo-Rubio, T., Oliva, B., Daura, X., Mas, J. M., & Montoto, C. (2021) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2021.741170 · Cited by 22 · see citing works
Zhu, N. W., Weedon, J., & Dow-Edwards, D. L. (2010) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2009.12.004 · Cited by 22 · see citing works
Farnsworth, S. J., Volz, T. J., Hanson, G. R., & Fleckenstein, A. E. (2008) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.108.146159 · Cited by 22 · see citing works
Methylphenidate: Gender trends in adult and pediatric populations over a 7 year period
Ehrhardt, C., Boucherie, Q., Pauly, V., Braunstein, D., Ronfle, E., Thirion, X., Frauger, É., & Micallef, J. (2017) · Therapies · doi:10.1016/j.therap.2017.05.005 · Cited by 20 · see citing works
Salman, T., Afroz, R., Nawaz, S., Mahmood, K., Haleem, D. J., & Zarina, S. (2021) · Biochimie · doi:10.1016/j.biochi.2021.08.009 · Cited by 18 · see citing works
Fazelipour, S., Tootian, Z., Saremi, Z., Shafii, M., Sheibani, M. T., Kiaei, S. B., KIUMARSI, M., & Asadi, F. (2014) · TURKISH JOURNAL OF MEDICAL SCIENCES · doi:10.3906/sag-1301-109 · Cited by 19 · see citing works
Mucci, F., Avella, M. T., & Marazziti, D. (2019) · Current Medicinal Chemistry · doi:10.2174/0929867326666190805153610 · Cited by 20 · see citing works
Gerlach, M., Grünblatt, E., & Lange, K. W. (2013) · ADHD Attention Deficit and Hyperactivity Disorders · doi:10.1007/s12402-013-0105-y · Cited by 18 · see citing works
Brookshire, B. R., & Jones, S. R. (2012) · Synapse · doi:10.1002/syn.21569 · Cited by 18 · see citing works
Huang, Y., Yeh, C., Chen, C.-H., Shang, C., & Gau, S. S. (2021) · Journal of Child and Adolescent Psychopharmacology · doi:10.1089/cap.2020.0104 · Cited by 18 · see citing works
Nikolaus, S., Mamlins, E., Giesel, F., Schmitt, D., & Müller, H. (2021) · Reviews in the Neurosciences · doi:10.1515/revneuro-2021-0083 · Cited by 17 · see citing works
Thompson, J. L., Yang, J., Lau, B. K., Liu, S., Baimel, C., Kerr, L. E., Liu, F., & Borgland, S. L. (2015) · Cerebral Cortex · doi:10.1093/cercor/bhv222 · Cited by 17 · see citing works
The Pharmacokinetics and Pharmacogenomics of Psychostimulants
Markowitz, J. S., & Melchert, P. W. (2022) · Child and Adolescent Psychiatric Clinics of North America · doi:10.1016/j.chc.2022.03.003 · Cited by 15 · see citing works
Self-citationLifetime evolution of ADHD treatment
Mucci, F., Carpita, B., Pagni, G., Vecchia, A. D., Bjedov, S., Pozza, A., & Marazziti, D. (2021) · Journal of Neural Transmission · doi:10.1007/s00702-021-02336-w · Cited by 14 · see citing works
Cardiovascular and temperature adverse actions of stimulants
Docherty, J. R., & Alsufyani, H. A. (2021) · British Journal of Pharmacology · doi:10.1111/bph.15465 · Cited by 13 · see citing works
Fuller, J., Burrell, M., Yee, A. G., Liyanagama, K., Lipski, J., Wickens, J. R., & Hyland, B. I. (2019) · Progress in Neurobiology · doi:10.1016/j.pneurobio.2019.101681 · Cited by 13 · see citing works
Brams, M. N., Turnbow, J. M., Pestreich, L. K., Giblin, J. M., Childress, A. C., McCague, K., & Muniz, R. (2012) · Journal of Clinical Psychopharmacology · doi:10.1097/jcp.0b013e3182677825 · Cited by 12 · see citing works
Self-citationPoddar, A., Gaddam, S., Sonnaila, S., Bhavaraju, V. S. M., & Agrawal, S. (2025) · NeuroSci · doi:10.3390/neurosci6020041 · Cited by 12 · see citing works
Antel, J., Albayrak, Ö., Heusch, G., Banaschewski, T., & Hebebrand, J. (2014) · European Archives of Psychiatry and Clinical Neuroscience · doi:10.1007/s00406-014-0522-8 · Cited by 11 · see citing works
Schneider, M. K. F., Retz, W., Gougleris, G., Verhoeven, W. M. A., Tulen, J. H. M., & Rösler, M. (2011) · Neuropsychobiology · doi:10.1159/000326693 · Cited by 11 · see citing works
The Ethics of Neuroenhancement
Wagner, N., Robinson, J., & Wiebking, C. (2015) · International Journal of Technoethics · doi:10.4018/ijt.2015010101 · Cited by 10 · see citing works
Serotonin Syndrome With Sertraline and Methylphenidate in an Adolescent
Türkoğlu, S. (2015) · Clinical Neuropharmacology · doi:10.1097/wnf.0000000000000075 · Cited by 10 · see citing works
Methylphenidate-induced spontaneous ejaculation
Öncü, B., Çolak, B., & Er, O. (2014) · Therapeutic Advances in Psychopharmacology · doi:10.1177/2045125314561993 · Cited by 10 · see citing works
Jeon, D. G., Kim, Y. W., Kim, N. Y., & Park, J. H. (2017) · Clinical Neuropharmacology · doi:10.1097/wnf.0000000000000220 · Cited by 10 · see citing works
Luppi, A. I., Singleton, S. P., Hansen, J. Y., Bzdok, D., Kuceyeski, A. F., Betzel, R. F., & Mišić, B. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.03.16.532981 · Cited by 10 · see citing works
Grünblatt, E., Bartl, J., Marinova, Z., & Walitza, S. (2012) · Journal of Neural Transmission · doi:10.1007/s00702-012-0869-9 · Cited by 9 · see citing works
Verite, F., & Micallef, J. (2016) · Therapies · doi:10.1016/j.therap.2016.10.002 · Cited by 7 · see citing works
The Societal Hazards of Neuroenhancement Technologies
Wagner, N., Robinson, J., & Wiebking, C. (2018) · Advances in information security, privacy, and ethics book series · doi:10.4018/978-1-5225-5094-5.ch010 · Cited by 6 · see citing works
Elmaghraby, R., Pines, A. R., Geske, J. R., Coombes, B. J., Leung, J. G., Croarkin, P. E., Markota, M., & Bobo, W. V. (2024) · JAACAP Open · doi:10.1016/j.jaacop.2024.01.003 · Cited by 6 · see citing works
Walitza, S., Romanos, M., Warnke, A., Greenhill, L. L., & Gerlach, M. (2014) · Springer eBooks · doi:10.1007/978-3-7091-1501-5_8 · Cited by 6 · see citing works
Extended-Release Dexmethylphenidate 30 mg/d Versus 20 mg/d
Silva, R. R., Brams, M. N., McCague, K., Pestreich, L. K., & Muniz, R. (2013) · Clinical Neuropharmacology · doi:10.1097/wnf.0b013e31829aa92c · Cited by 6 · see citing works
Self-citationPrescriptions hors AMM supervisées de méthylphénidate dans le TDAH de l’adulte
Carton, L., Dondaine, T., Deheul, S., Marquié, C., Brigadeau, F., Amad, A., Devos, D., Danel, T., Bordet, R., Cottencin, O., et al. (2018) · L Encéphale · doi:10.1016/j.encep.2018.05.008 · Cited by 6 · see citing works
Saiz, L. C., Gil, M., Alonso, Á., Erviti, J., Garjón, J., & Martinez, M. I. (2020) · Pharmacoepidemiology and Drug Safety · doi:10.1002/pds.4954 · Cited by 6 · see citing works
Faraone, S. V., Ward, C. L., Boucher, M., Elbekai, R. H., & Brunner, E. (2025) · Expert Opinion on Therapeutic Targets · doi:10.1080/14728222.2025.2552324 · Cited by 8 · see citing works
Tamilselvan, T., Siddique, S. A., Vishnupriya, M., Sindhu, G., & Balamurugan, E. (2017) · Beni-Suef University Journal of Basic and Applied Sciences · doi:10.1016/j.bjbas.2017.01.001 · Cited by 5 · see citing works
Walitza, S., Gerlach, M., Romanos, M., & Renner, T. (2016) · Springer eBooks · doi:10.1007/978-3-662-48624-5_8 · Cited by 5 · see citing works
Graney, P. L., Chen, M. Y., Wood, R. I., & Wagner, C. K. (2024) · Hormones and Behavior · doi:10.1016/j.yhbeh.2024.105550 · Cited by 4 · see citing works
Baweja, R. K., Mills, S., & Waxmonsky, J. G. (2018) · Journal of Child and Adolescent Psychopharmacology · doi:10.1089/cap.2018.0034 · Cited by 4 · see citing works
Gutiérrez-Casares, J. R., Quintero, J., Segú-Vergés, C., Monterde, P. R., Pozo-Rubio, T., Coma, M., & Montoto, C. (2023) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2023.939650 · Cited by 5 · see citing works
The discriminative stimulus properties of methylphenidate in C57BL/6J mice
McGovern, R. W., Middaugh, L. D., Patrick, K. S., & Griffin, W. C. (2010) · Behavioural Pharmacology · doi:10.1097/fbp.0b013e3283423d92 · Cited by 4 · see citing works
Self-citationPark, Y., & Jung, Y.-K. (2010) · Progress in Neuro-Psychopharmacology and Biological Psychiatry · doi:10.1016/j.pnpbp.2010.03.016 · Cited by 4 · see citing works
Luppi, A. I., Hansen, J. Y., Adapa, R., Carhart-Harris, R. L., Roseman, L., Timmermann, C., Golkowski, D., Ranft, A., Ilg, R., Jordan, D., et al. (2022) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2022.07.12.499688 · Cited by 4 · see citing works
Effects of Methylphenidate and Atomoxetine on Development of the Brain
Altunkaynak, B. Z., Önger, M. E., Türkmen, A. P., Yurt, K. K., Altun, G., Yuce, M., & Kaplan, S. (2016) · Springer eBooks · doi:10.1007/978-81-322-2803-5_48 · Cited by 3 · see citing works
The Treatment of Adult ADHD: Complexity at Hand
Pallanti, S., & Salerno, L. (2020) · Springer eBooks · doi:10.1007/978-3-030-39051-8_19 · Cited by 3 · see citing works
Danysz, W., Flik, G., McCreary, A. C., Tober, C., Dimpfel, W., Bizot, J. C., Kostrzewa, R. M., Brown, R. W., Jatzke, C., Greco, S., et al. (2015) · Journal of Neural Transmission · doi:10.1007/s00702-015-1392-6 · Cited by 3 · see citing works
CONTRIBUTION OF CATECHOLAMINES TO VISUAL WORKING MEMORY IN THE MACAQUE MONKEY
Oemisch, M. (2012) · QSpace (Queen's University Library) · Cited by 3 · see citing works
Chronic Administration of Methylphenidate Induced Degeneration of Spermatogenesis in Adult Male Rats
Abdollahifar, M., Zangiabadian, M., Moradi, A., Rezaei, F., Fadai, S., Khatmi, A., Ezi, S., Norozian, M., Moghoddam, M. H., Razminia, Y., et al. (2020) · Pharmaceutical Chemistry Journal · doi:10.1007/s11094-020-02257-0 · Cited by 2 · see citing works
Psychopharmacology of Pediatric Attention-Deficit/Hyperactivity Disorder
Greydanus, D. E., Rowland, D. C., Patel, D. R., & Soares, N. S. (2021) · Psychiatric Annals · doi:10.3928/00485713-20210914-01 · Cited by 2 · see citing works
Lyseng-Williamson, K. A. (2017) · Drugs & Therapy Perspectives · doi:10.1007/s40267-017-0462-2 · Cited by 2 · see citing works
The rate of dasotraline brain entry is slow following intravenous administration
Lew, R., Constantinescu, C. C., Holden, D., Carson, R. E., Carroll, V. M., Galluppi, G. R., Koblan, K. S., & Hopkins, S. C. (2020) · Psychopharmacology · doi:10.1007/s00213-020-05623-8 · Cited by 2 · see citing works
Ayme‐Dietrich, E., Kaguelidou, F., Bertschy, G., & Chouchana, L. (2024) · Pharmacoepidemiology and Drug Safety · doi:10.1002/pds.5814 · Cited by 2 · see citing works
Synthetic approaches and bio-distribution studies of [11C]methyl-phenidate.
Patt, M., Solbach, C., Wüllner, U., Blocher, A., Stahlschmidt, A., Gündisch, D., Kovar, K. ‐., & Machulla, H. (2007) · PubMed · Cited by 1 · see citing works
Pouraman, M., Kianifard, D., & Akbari, G. (2019) · DOAJ (DOAJ: Directory of Open Access Journals) · Cited by 1 · see citing works
Paulus, M. P., Kuplicki, R., Victor, T. A., Yeh, H., & Khalsa, S. S. (2021) · BMC Psychiatry · doi:10.1186/s12888-021-03583-7 · Cited by 1 · see citing works
Disentangling Brain Networks in Adult ADHD: Studies with fMRI and TMS
Schneider, M. (2012) · RePub (Erasmus University Rotterdam) · Cited by 1 · see citing works
Fazelipour, S., Tootian, Z., Kazergah, F. M., Kiaie, B., Chegini, H., Mohammadzadeh Kazergah, A., & Soleimani, M. (2013) · DOAJ (DOAJ: Directory of Open Access Journals)
The role of Dopamine D1/5 receptors in fear and reward
Abraham, A. D. (2014) · doi:10.6083/m4513wxq
- Authors
- Markowitz, J. S., DeVane, C. L., Pestreich, L. K., Patrick, K. S., & Muniz, R.
- Affiliations
- Medical University of South Carolina (US)
- Norvartis Pharmaceuticals, East Hanover, New Jersey.
- Venue
- Journal of Child and Adolescent Psychopharmacology
- Publisher
- SAGE Publications
- Published
- 2006-12
- Volume
- 16
- Issue
- 6
- Pages
- 687-698
- ISSN
- 1044-5463 (ISSN-L)
- 1557-8992
- OpenAlex
- W2065636703
- Cited by
- 109
- References
- 47
- Citations by year
- 2025: 3 · 2024: 6 · 2023: 4 · 2022: 3 · 2021: 12 · 2020: 5 · 2019: 6 · 2018: 8 · 2017: 4 · 2016: 7 · 2015: 6 · 2014: 8 · 2013: 4 · 2012: 8
- FWCI
- 3.19
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Child and Adolescent Psychopharmacology (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Attention Deficit Hyperactivity Disorder
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuroscience and Neuropharmacology Research
- Keywords
- methylphenidate, enantiomers, racemic mixtures, attention deficit hyperactivity disorder, receptor binding affinity, norepinephrine transporter, dopamine transporter, 5-HT1A receptor, 5-HT2B receptor, serotonergic neurotransmission, CNS pharmacology
- MeSH terms
- Central Nervous System Stimulants, Animals, Carrier Proteins, Cells, Cultured, Drug Evaluation, Preclinical, Guinea Pigs, Humans, Ion Channels, Isomerism, Methylphenidate, Protein Binding, Receptors, Drug, Receptors, Muscarinic, Stereoisomerism, Receptor, Serotonin, 5-HT1A, Receptor, Serotonin, 5-HT2B, Dopamine Plasma Membrane Transport Proteins, Norepinephrine Plasma Membrane Transport Proteins, Rats, Dexmethylphenidate Hydrochloride
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