General Information of Drug (ID: DM7SJD6)

Drug Name
Methylphenidate Drug Info
Synonyms
Calocain; Centedein; Centedrin; Centredin; Concerta; Daytrana; Meridil; Metadate; Methylfenidan; Methylin; Methylofenidan; Methylphen; Methylphenidan; Methylphenidatum; Metilfenidato; Phenidylate; Plimasine; Riphenidate; Ritalin; Ritaline; Tsentedrin; Metadate CD; Metadate ER; Methyl phenidate; Methyl phenidyl acetate; Methyl phenidylacetate; Methylin ER; Metilfenidato [Italian]; Ritalin LA; Ritalin SR; Ritcher works; C 4311; Attenta (TN); Biphentin (TN); Concerta (TN); D-methylphenidate HCl; Daytrana (TN); Equasym (TN); Metadate ER (TN); Methylin (TN); Methylphenidate [INN:BAN]; Methylphenidatum [INN-Latin]; Metilfenidato [INN-Spanish]; Motiron (TN); PMS-Methylphenidate; Ritalin (TN); Ritalin LA (TN); Ritalin-SR; Rubifen (TN); Methylphenidate (USAN/INN); Alpha-Phenyl-2-piperidineacetic acid methyl ester; Methyl phenyl(piperidin-2-yl)acetate; Methyl alpha-phenyl-alpha-2-piperidinylacetate; Alpha-Phenyl-alpha-(2-piperidyl)acetic acid methyl ester; Methyl 2-phenyl-2-piperidin-2-ylacetate; Methyl alpha-phenyl-alpha-(2-piperidyl)acetate; Methyl (2-phenyl-2-(2-piperidyl)acetate); METHYLPHENIDATE (SEE ALSO: METHYLPHENIDATE HYDROCHLORIDE, CAS 298-59-9, NTPNO 10266-R); 2-Piperidineacetic acid, .alpha.-phenyl-, methyl ester; 2-Piperidineacetic acid, alpha-phenyl-, methyl ester
Indication
Disease Entry ICD 11 Status REF
Attention deficit hyperactivity disorder 6A05.Z Approved [1]
Depression 6A70-6A7Z Approved [2]
Myasthenia gravis 8C6Y Approved [2]
Narcolepsy 7A20 Approved [2]
Traumatic brain injury NA07.Z Phase 4 [1]
Therapeutic Class
Central Nervous System Stimulants
Cross-matching ID
PubChem CID
4158
ChEBI ID
CHEBI:84276
CAS Number
CAS 113-45-1
TTD Drug ID
DM7SJD6
VARIDT Drug ID
DR00389
INTEDE Drug ID
DR1054
ACDINA Drug ID
D00419

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting Dopamine transporter (DAT)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cocaine DMSOX7I Anaesthesia 9A78.6 Approved [7]
Dasotraline DMLDQFV Attention deficit hyperactivity disorder 6A05.Z Approved [8]
Modafinil DMYILBE Malignant glioma 2A00.0 Approved [9]
Phenmetrazine DMXYTN9 Obesity 5B81 Approved [10]
Ioflupane i-123 DMNARJT Parkinson disease 8A00.0 Approved [11]
DEXMETHYLPHENIDATE HYDROCHLORIDE DM8WBAH Attention deficit hyperactivity disorder 6A05.Z Approved [12]
Altropane DMO9WDS Attention deficit hyperactivity disorder 6A05.Z Approved [13]
Amitifadine DMS1X67 Obesity 5B81 Phase 3 [14]
NAV5001 DMRSI1M Dementia 6D80-6D86 Phase 3 [13]
MIN-117 DMSLIW6 Major depressive disorder 6A70.3 Phase 2 [15]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Glycine DMIOZ29 Allergic rhinitis CA08.0 Approved [16]
Norepinephrine DMOUC09 Alopecia ED70 Approved [17]
Drug(s) Metabolized By Carboxylesterase 1 (CES1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Irinotecan DMP6SC2 Adenocarcinoma 2D40 Approved [18]
Enalapril DMNFUZR Congestive heart failure BD10 Approved [19]
Candesartan DMRK8OT Chronic heart failure BD1Z Approved [20]
Salbutamol DMN9CWF Acute asthma CA23 Approved [21]
PSI-7977 DMLSUWZ HCV 1-6 infection 1E51 Approved [22]
Rufinamide DMWE60C Epilepsy 8A60-8A68 Approved [23]
Dexmethylphenidate DMUQE2A Attention deficit hyperactivity disorder 6A05.Z Approved [24]
MK-4827 DMLYGH4 Ovarian cancer 2C73 Phase 3 [25]
Dabigatran etexilate DMRDZ4X Venous thromboembolism BD72 Phase 3 [26]
Pradaxa DM2ZYX9 Stroke 8B20 Phase 3 [27]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Salmeterol DMIEU69 Allergic asthma CA23.0 Approved [28]
Bambuterol DMKLSHF Asthma CA23 Approved [29]
Terbutaline DMD4381 Asthma CA23 Approved [30]
Salbutamol DMN9CWF Acute asthma CA23 Approved [31]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [32]
Methotrexate DM2TEOL Anterior urethra cancer Approved [33]
Epinephrine DM3KJBC Acute asthma CA23 Approved [34]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [35]
Liothyronine DM6IR3P Congenital hypothyroidism Approved [36]
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [37]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Dopamine transporter (DAT) TTVBI8W SC6A3_HUMAN Blocker [3]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Sodium- and chloride-dependent glycine transporter 2 (SLC6A5) DTE8R17 SC6A5_HUMAN Substrate [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Carboxylesterase 1 (CES1) Main DME DEB30C5 EST1_HUMAN Substrate [5]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Beta-2 adrenergic receptor (ADRB2) OTSDOX4Q ADRB2_HUMAN Drug Response [6]

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7236).
2 Methylphenidate FDA Label
3 Imaging the effects of methylphenidate on brain dopamine: new model on its therapeutic actions for attention-deficit/hyperactivity disorder. Biol Psychiatry. 2005 Jun 1;57(11):1410-5.
4 SLC6 transporters: structure, function, regulation, disease association and therapeutics. Mol Aspects Med. 2013 Apr-Jun;34(2-3):197-219.
5 Methylphenidate is stereoselectively hydrolyzed by human carboxylesterase CES1A1. J Pharmacol Exp Ther. 2004 Aug;310(2):469-76.
6 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
7 Differential involvement of the norepinephrine, serotonin and dopamine reuptake transporter proteins in cocaine-induced taste aversion. Pharmacol Biochem Behav. 2009 Jul;93(1):75-81.
8 Dasotraline for the Treatment of Attention-Deficit/Hyperactivity Disorder: A Randomized, Double-Blind, Placebo-Controlled, Proof-of-Concept Trial in Adults. Neuropsychopharmacology. 2015 Nov;40(12):2745-52.
9 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
10 Interaction of the anorectic medication, phendimetrazine, and its metabolites with monoamine transporters in rat brain. Eur J Pharmacol. 2002 Jun 28;447(1):51-7.
11 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
12 Synthesis and pharmacology of site-specific cocaine abuse treatment agents: restricted rotation analogues of methylphenidate. J Med Chem. 2007 May 31;50(11):2718-31.
13 Rapid detection of Parkinson's disease by SPECT with altropane: a selective ligand for dopamine transporters. Synapse. 1998 Jun;29(2):128-41.
14 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 927).
15 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
16 Mutations in the GlyT2 gene (SLC6A5) are a second major cause of startle disease. J Biol Chem. 2012 Aug 17;287(34):28975-85.
17 SLC6A2 Gene (Protein Coding).
18 Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 2010 Jan;24(1):104-23.
19 Absorption and cleavage of enalapril, a carboxyl ester prodrug, in the rat intestine: in vitro, in situ intestinal perfusion and portal vein cannulation models. Biopharm Drug Dispos. 2015 Sep;36(6):385-397.
20 Different hydrolases involved in bioactivation of prodrug-type angiotensin receptor blockers: carboxymethylenebutenolidase and carboxylesterase 1. Drug Metab Dispos. 2013 Nov;41(11):1888-95.
21 Effect of carboxylesterase 1 c.428G>A single nucleotide variation on the pharmacokinetics of quinapril and enalapril. Br J Clin Pharmacol. 2015 Nov;80(5):1131-8.
22 Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977. J Biol Chem. 2010 Nov 5;285(45):34337-47.
23 Investigation of the metabolism of rufinamide and its interaction with valproate. Drug Metab Lett. 2011 Dec;5(4):280-9.
24 Dexmethylphenidate hydrochloride in the treatment of attention deficit hyperactivity disorder. Neuropsychiatr Dis Treat. 2006 Dec;2(4):467-73.
25 Summary of FDA-approved anticancer cytotoxic drugs at May 2019.
26 Pharmacogenomics of novel direct oral anticoagulants: newly identified genes and genetic variants. J Pers Med. 2019 Jan 17;9(1). pii: E7.
27 Conventional liquid chromatography/triple quadrupole mass spectrometry based metabolite identification and semi-quantitative estimation approach in the investigation of in vitro dabigatran etexilate metabolism. Anal Bioanal Chem. 2013 Feb;405(5):1695-704.
28 Pleiotropic beta-agonist-promoted receptor conformations and signals independent of intrinsic activity. Am J Respir Cell Mol Biol. 2007 Feb;36(2):236-43. doi: 10.1165/rcmb.2006-0257OC. Epub 2006 Sep 15.
29 Development of 3D-QSAR models for predicting the activities of chemicals to stimulate muscle growth via (2)-adrenoceptor. Toxicol In Vitro. 2021 Dec;77:105251. doi: 10.1016/j.tiv.2021.105251. Epub 2021 Sep 30.
30 Beta2-adrenergic receptor polymorphisms in African American children with status asthmaticus. Pediatr Crit Care Med. 2006 Jan;7(1):15-8. doi: 10.1097/01.pcc.0000194010.63115.a2.
31 beta2-adrenergic receptor polymorphisms and salbutamol-stimulated energy expenditure. J Clin Endocrinol Metab. 2005 Apr;90(4):2301-7. doi: 10.1210/jc.2004-1356. Epub 2005 Feb 1.
32 Neutrophil beta(2)-adrenoceptor function in major depression: G(s) coupling, effects of imipramine and relationship to treatment outcome. Eur J Pharmacol. 1999 Dec 15;386(2-3):135-44. doi: 10.1016/s0014-2999(99)00749-9.
33 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
34 Myocardial ischaemia and ventricular arrhthymias precipitated by physiological concentrations of adrenaline in patients with coronary artery disease. Br Heart J. 1992 May;67(5):419-20. doi: 10.1136/hrt.67.5.419-b.
35 Phenotypic characterization of retinoic acid differentiated SH-SY5Y cells by transcriptional profiling. PLoS One. 2013 May 28;8(5):e63862.
36 Hormonal regulation of beta2-adrenergic receptor level in prostate cancer. Prostate. 2008 Jul 1;68(10):1133-42. doi: 10.1002/pros.20778.
37 Histamine augments beta2-adrenoceptor-induced cyclic AMP accumulation in human prostate cancer cells DU-145 independently of known histamine receptors. Biochem Pharmacol. 2007 Mar 15;73(6):814-23. doi: 10.1016/j.bcp.2006.11.022. Epub 2006 Dec 1.