General Information of Drug (ID: DMSZQAK)

Drug Name
Amphetamine Drug Info
Synonyms Amphetamine (tamper and abuse-resistant, Bio-MD/MPAR, ADHD); Amphetamine (tamper and abuse-resistant, Bio-MD/MPAR, ADHD), PharmacoFore; PF-08 (Bio-MD/MPAR/prodrug/oral, ADHD), PharmacoFore
Indication
Disease Entry ICD 11 Status REF
Attention deficit hyperactivity disorder 6A05.Z Approved [1]
Cross-matching ID
PubChem CID
3007
ChEBI ID
CHEBI:2679
CAS Number
CAS 300-62-9
TTD Drug ID
DMSZQAK
VARIDT Drug ID
DR00084
INTEDE Drug ID
DR0106
ACDINA Drug ID
D00036

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Discontinued Drug(s)
Investigative Drug(s)
Clinical Trial Drug(s)
Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Solid tumour/cancer 2A00-2F9Z Approved [11]
Progesterone DMUY35B Premature labour JB00 Approved [12]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [13]
Acetaminophen DMUIE76 Pain MG30-MG3Z Approved [14]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [15]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [16]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [17]
Dopamine DMPGUCF Parkinson disease 8A00.0 Approved [18]
Nicotine DMWX5CO Nicotine dependence 6C4A.2 Approved [19]
Propranolol DM79NTF Migraine 8A80 Approved [20]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Propranolol DM79NTF Migraine 8A80 Approved [21]
Ergotidine DM78IME Respiratory allergy 4A80 Approved [22]
Metformin DM89QE1 Type-2 diabetes 5A11 Approved [23]
Clonidine DM6RZ9Q Hypertension BA00-BA04 Approved [21]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [24]
Epinephrine DM3KJBC Allergy 4A80-4A85 Approved [22]
Norepinephrine DMOUC09 Sepsis 1G40-1G41 Approved [22]
Acetylcholine DMDF79Z Cataract 9B10 Approved [25]
Sodium chloride DMM3950 Skin burns ME65.0 Approved [26]
Etilefrine DM67PWD Cardiovascular disease BA00-BE2Z Withdrawn from market [27]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Verapamil DMA7PEW Hypertension BA00-BA04 Approved [28]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [29]
Entecavir DM7VTQO Hepatitis B virus infection 1E51.0 Approved [24]
Levacecarnine HCL DMJBOCR Cognitive impairment 6D71 Approved [30]
Potassium chloride DMMTAJC Hypokalemia 5C77 Approved [31]
Tiotropium DMFDC0Q Chronic obstructive pulmonary disease CA22 Approved [32]
Ipratropium DMFQ320 Obstructive lung disease CA22.Z Approved [32]
Mepyramine DMB4SFH Allergy 4A80-4A85 Approved [33]
Acetylcarnitine DM4UE3K Migraine 8A80 Phase 4 [34]
Acetyl-L-carnitine DM74HGJ Discovery agent N.A. Investigative [29]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Norepinephrine DMOUC09 Sepsis 1G40-1G41 Approved [35]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dopamine DMPGUCF Parkinson disease 8A00.0 Approved [36]
OPC-34712 DMHG57U Major depressive disorder 6A70.3 Approved [37]
Bretylium DM1FX74 Ventricular fibrillation BC71.1 Approved [38]
Benztropine DMGZOVN Parkinson disease 8A00.0 Approved [39]
Drug Name Drug ID Indication ICD 11 Highest Status REF
Lisdexamfetamine DM6W8V5 Attention deficit hyperactivity disorder 6A05.Z Approved [40]
Dextroamphetamine DMMIHVP Attention deficit hyperactivity disorder 6A05.Z Approved [2]
Hydroxyamphetamine Hydrobromide DMQSGM0 Horner syndrome 8D8A.1 Approved [41]
SEP-363856 DMG2QP4 Schizophrenia 6A20 Phase 3 [42]
NT0202 DMCMIJ1 Attention deficit hyperactivity disorder 6A05.Z Phase 3 [2]
SPD-465 DM7NV1I Attention deficit hyperactivity disorder 6A05.Z Phase 3 [2]
RG-7351 DMFGR98 Major depressive disorder 6A70.3 Phase 1 [43]
Tyramine DM4UXT1 Discovery agent N.A. Investigative [44]
EPPTB DMK3VID Discovery agent N.A. Investigative [45]
R(-)amphetamine DM72ES1 Discovery agent N.A. Investigative [46]
⏷ 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
Trace amine-associated receptor-1 (TAAR1) TTIU98M TAAR1_HUMAN Modulator [2] , [3] , [4] , [5] , [1]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Sodium-dependent dopamine transporter (SLC6A3) DT3BA8L SC6A3_HUMAN Substrate [6]
Sodium-dependent noradrenaline transporter (SLC6A2) DT9JBVI SC6A2_HUMAN Substrate [6]
Organic cation/carnitine transporter 2 (SLC22A5) DT3HUVD S22A5_HUMAN Substrate [7]
Organic cation transporter 3 (SLC22A3) DT6201N S22A3_HUMAN Substrate [8]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2D6 (CYP2D6) Main DME DECB0K3 CP2D6_HUMAN Substrate [9]
Tyramine oxidase (tynA) DEB3TNR AMO_ECOLI Substrate [10]

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
2 Methamphetamine and HIV-1-induced neurotoxicity: role of trace amine associated receptor 1 cAMP signaling in astrocytes. Neuropharmacology. 2014 Oct;85:499-507.
3 Alpha-1B adrenergic receptor knockout mice are protected against methamphetamine toxicity. J Neurochem. 2003 Jul;86(2):413-21.
4 Involvement of the alpha(1D)-adrenergic receptor in methamphetamine-induced hyperthermia and neurotoxicity in rats. Neurotox Res. 2013 Aug;24(2):130-8.
5 Methamphetamine increases the hippocampal alpha(2A)-adrenergic receptor and Galpha(o) in mice. Neurosci Lett. 2002 Dec 16;334(3):145-8.
6 Amphetamines, new psychoactive drugs and the monoamine transporter cycle. Trends Pharmacol Sci. 2015 Jan;36(1):41-50.
7 Novel organic cation transporter 2-mediated carnitine uptake in placental choriocarcinoma (BeWo) cells. J Pharmacol Exp Ther. 2005 Jan;312(1):192-8.
8 Interaction of organic cation transporter 3 (SLC22A3) and amphetamine. J Neurochem. 2010 Jul;114(1):142-9.
9 Involvement of CYP2D6 in the in vitro metabolism of amphetamine, two N-alkylamphetamines and their 4-methoxylated derivatives. Xenobiotica. 1999 Jul;29(7):719-32.
10 Mechanistic elucidation of amphetamine metabolism by tyramine oxidase from human gut microbiota using molecular dynamics simulations. J Cell Biochem. 2019 Jan 30.
11 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
12 Effect of genetic polymorphism on the metabolism of endogenous neuroactive substances, progesterone and p-tyramine, catalyzed by CYP2D6. Brain Res Mol Brain Res. 2004 Oct 22;129(1-2):117-23.
13 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
14 Metabolic interactions between acetaminophen (paracetamol) and two flavonoids, luteolin and quercetin, through in-vitro inhibition studies. J Pharm Pharmacol. 2017 Dec;69(12):1762-1772.
15 Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.
16 Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues. Chem Res Toxicol. 2003 Apr;16(4):450-9.
17 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
18 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
19 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
20 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.
21 Influx Transport of Cationic Drug at the Blood-Retinal Barrier: Impact on the Retinal Delivery of Neuroprotectants. Biol Pharm Bull. 2017;40(8):1139-1145.
22 Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. Neuropharmacology. 2006 Jun;50(8):941-52.
23 Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver. Hepatology. 2009 Oct;50(4):1227-40.
24 Multiple SLC and ABC Transporters Contribute to the Placental Transfer of Entecavir. Drug Metab Dispos. 2017 Mar;45(3):269-278.
25 Organic cation transporters: physiology, toxicology and special focus on ethidium as a novel substrate. Curr Drug Metab. 2009 Jul;10(6):617-31.
26 Organic cation transporter 3 (Slc22a3) is implicated in salt-intake regulation. J Neurosci. 2004 Mar 17;24(11):2846-51.
27 Drug specificity and intestinal membrane localization of human organic cation transporters (OCT). Biochem Pharmacol. 2005 Dec 5;70(12):1851-60.
28 Genetic variations of the SLC22A5 gene in the Chinese and Indian populations of Singapore. Drug Metab Pharmacokinet. 2010;25(1):112-9.
29 Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84.
30 Colistin is substrate of the carnitine/organic cation transporter 2 (OCTN2, SLC22A5). Drug Metab Dispos. 2017 Dec;45(12):1240-1244.
31 Mutations affecting GABAergic signaling in seizures and epilepsy. Pflugers Arch. 2010 Jul;460(2):505-23.
32 Transport of ipratropium, an anti-chronic obstructive pulmonary disease drug, is mediated by organic cation/carnitine transporters in human bronchial epithelial cells: implications for carrier-mediated pulmonary absorption. Mol Pharm. 2010 Feb 1;7(1):187-95.
33 Genetic deficiency of carnitine/organic cation transporter 2 (slc22a5) is associated with altered tissue distribution of its substrate pyrilamine in mice. Biopharm Drug Dispos. 2009 Dec;30(9):495-507.
34 Cloning and functional characterization of a novel up-regulator, cartregulin, of carnitine transporter, OCTN2. Arch Biochem Biophys. 2006 Aug 1;452(1):29-37.
35 Chronic depolarization stimulates norepinephrine transporter expression via catecholamines. J Neurochem. 2006 May;97(4):1044-51.
36 Characterization of VNTRs Within the Entire Region of SLC6A3 and Its Association with Hypertension. DNA Cell Biol. 2017 Mar;36(3):227-236.
37 Brexpiprazole reduces hyperactivity, impulsivity, and risk-preference behavior in mice with dopamine transporter knockdown-a model of mania. Psychopharmacology (Berl). 2017 Mar;234(6):1017-1028.
38 Which form of dopamine is the substrate for the human dopamine transporter: the cationic or the uncharged species? J Biol Chem. 1999 Feb 19;274(8):4876-82.
39 Pharmacological characterization of a dopamine transporter ligand that functions as a cocaine antagonist. J Pharmacol Exp Ther. 2014 Jan;348(1):106-15.
40 2007 FDA drug approvals: a year of flux. Nat Rev Drug Discov. 2008 Feb;7(2):107-9.
41 Diagnostic pharmacology of the pupil.Clin Neuropharmacol.1985;8(1):27-37.
42 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
43 Clinical pipeline report, company report or official report of Roche.
44 Differential modulation of Beta-adrenergic receptor signaling by trace amine-associated receptor 1 agonists. PLoS One. 2011;6(10):e27073.
45 The selective antagonist EPPTB reveals TAAR1-mediated regulatory mechanisms in dopaminergic neurons of the mesolimbic system. Proc Natl Acad Sci U S A. 2009 Nov 24;106(47):20081-6.
46 The Trace Amine 1 receptor knockout mouse: an animal model with relevance to schizophrenia. Genes Brain Behav. 2007 Oct;6(7):628-39.