General Information of Drug (ID: DMC50ME)

Drug Name
Debrisoquin Drug Info
Synonyms
Debrisochinum; Debrisoquina; Debrisoquine; Debrisoquinum; Declinax; Equitonil; Isocaramidine; Tendor; DEBRISOQUIN SULFATE; Debrisoquin hemisulfate; Debrisoquine sulfate; Isocaramidine sulfate; Debrisoquina [INN-Spanish]; Debrisoquine [INN:BAN]; Debrisoquinum [INN-Latin]; Ro 5-3307/1; Sulfuric acid compound with 3,4-dihydro-2(1H)-isoquinolinecarboximidamide (1:1); 1,2,3, 4-Tetrahydro-isoquinoline-2-carboxamidine sulfate; 2(1H)-Isoquinolinecarboxamidine, 3,4-dihydro-(7CI,8CI); 2(1H)-Isoquinolinecarboxamidine, 3,4-dihydro-, sulfate (2:1); 2(1H)-Isoquinolinecarboximidamide, 3,4-dihydro-, sulfate (2:1); 2-Amidino-1,2,3,4-tetrahydroisoquinoline; 3,4-Dihydro-2(1H)-isoquinolinecarboxamidine; 3,4-Dihydro-2(1H)-isoquinolinecarboxamidine sulfate (2:1); 3,4-Dihydro-2(1H)-isoquinolinecarboximidamide; 3,4-Dihydro-2(1H;)-isoquinoline carboxamidine sulfate; 3,4-dihydro-1H-isoquinoline-2-carboximidamide; 3,4-dihydroisoquinoline-2(1H)-carboximidamide
Indication
Disease Entry ICD 11 Status REF
Hypertension BA00-BA04 Approved [1]
Therapeutic Class
Antihypertensive Agents
Cross-matching ID
PubChem CID
2966
ChEBI ID
CHEBI:34665
CAS Number
CAS 1131-64-2
TTD Drug ID
DMC50ME
VARIDT Drug ID
DR01479
INTEDE Drug ID
DR0427

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DTP
DME
Drug Status:
Approved Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Guanethidine DM9NSWT Moderate and severe hypertension BA00.Z Approved [7]
Drug(s) Transported By P-glycoprotein 1 (ABCB1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Amoxicillin DMUYNEI Acute otitis media AB00 Approved [8]
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [9]
Methotrexate DM2TEOL Anterior urethra cancer Approved [10]
Folic Acid DMEMBJC Colorectal carcinoma Approved [11]
Fluorouracil DMUM7HZ Adenocarcinoma 2D40 Approved [10]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [10]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [12]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [10]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [13]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [14]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dinoprostone DMTYOPD Medical abortion JA00.1Z Approved [15]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [16]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [17]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [18]
Zidovudine DM4KI7O Human immunodeficiency virus infection 1C62 Approved [8]
Verapamil DMA7PEW Angina pectoris BA40 Approved [19]
Sorafenib DMS8IFC Adenocarcinoma 2D40 Approved [20]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [21]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [22]
Propranolol DM79NTF Angina pectoris BA40 Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 1A1 (CYP1A1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Progesterone DMUY35B Amenorrhea GA20.0 Approved [24]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [25]
Estradiol DMUNTE3 Acne vulgaris ED80 Approved [26]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [27]
Oxaliplatin DMQNWRD Adenocarcinoma 2D40 Approved [28]
Diclofenac DMPIHLS Chronic renal failure GB61.Z Approved [29]
Estrone DM5T6US Acne vulgaris ED80 Approved [30]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [31]
Riboflavin DM8YMWE Acne vulgaris ED80 Approved [32]
Mercaptopurine DMTM2IK Acute lymphoblastic leukaemia 2A85 Approved [33]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Metabolized By Cytochrome P450 2D6 (CYP2D6)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Doxorubicin DMVP5YE Acute myelogenous leukaemia 2A41 Approved [34]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [35]
Tamoxifen DMLB0EZ Breast cancer 2C60-2C65 Approved [36]
Acetaminophen DMUIE76 Allergic rhinitis CA08.0 Approved [37]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [38]
Quinine DMSWYF5 Malaria 1F40-1F45 Approved [39]
Propofol DMB4OLE Anaesthesia 9A78.6 Approved [40]
Dopamine DMPGUCF Acromegaly 5A60.0 Approved [41]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [42]
Propranolol DM79NTF Angina pectoris BA40 Approved [43]
⏷ 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
Adrenergic neuron (AD neuro) TTT04VN NOUNIPROTAC Blocker [2]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Organic cation transporter 1 (SLC22A1) DTT79CX S22A1_HUMAN Substrate [3]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 2D6 (CYP2D6) DECB0K3 CP2D6_HUMAN Substrate [5]
Cytochrome P450 1A1 (CYP1A1) DE6OQ3W CP1A1_HUMAN Substrate [6]

References

1 Drug information of Debrisoquin, 2008. eduDrugs.
2 Guanethidine and related agents. 3. Antagonism by drugs which inhibit the norepinephrine pump in man. J Clin Invest. 1970 Aug;49(8):1596-604.
3 The prototypic pharmacogenetic drug debrisoquine is a substrate of the genetically polymorphic organic cation transporter OCT1. Biochem Pharmacol. 2012 May 15;83(10):1427-34.
4 Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein. Pharm Res. 1999 Mar;16(3):408-14.
5 Functional analysis of CYP2D6.31 variant: homology modeling suggests possible disruption of redox partner interaction by Arg440His substitution. Proteins. 2005 May 1;59(2):339-46.
6 4-Hydroxylation of debrisoquine by human CYP1A1 and its inhibition by quinidine and quinine. J Pharmacol Exp Ther. 2002 Jun;301(3):1025-32.
7 Characterization of bradykinin-induced endothelium-independent contraction in equine basilar artery. J Vet Pharmacol Ther. 2009 Jun;32(3):264-70.
8 Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
9 MDR1 (ABCB1) G1199A (Ser400Asn) polymorphism alters transepithelial permeability and sensitivity to anticancer agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):183-8.
10 Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
11 Folate transporter expression decreases in the human placenta throughout pregnancy and in pre-eclampsia. Pregnancy Hypertens. 2012 Apr;2(2):123-31.
12 Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res. 2001 Dec;18(12):1660-8.
13 Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92.
14 Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011 Apr;33(2):244-50.
15 Are organic cation transporters capable of transporting prostaglandins? Naunyn Schmiedebergs Arch Pharmacol. 2005 Aug;372(2):125-30.
16 Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). J Pharmacol Exp Ther. 2006 Nov;319(2):879-86.
17 Pharmacologic markers and predictors of responses to imatinib therapy in patients with chronic myeloid leukemia. Leuk Lymphoma. 2008 Apr;49(4):639-42.
18 Organic cation transporters are determinants of oxaliplatin cytotoxicity. Cancer Res. 2006 Sep 1;66(17):8847-57.
19 Implications of genetic polymorphisms in drug transporters for pharmacotherapy. Cancer Lett. 2006 Mar 8;234(1):4-33.
20 Upregulation of histone acetylation reverses organic anion transporter 2 repression and enhances 5-fluorouracil sensitivity in hepatocellular carcinoma
21 Comparison of type I and type II organic cation transport by organic cation transporters and organic anion-transporting polypeptides. J Pharmacol Exp Ther. 2001 Jul;298(1):110-5.
22 Organic cation transporters and their pharmacokinetic and pharmacodynamic consequences. Drug Metab Pharmacokinet. 2008;23(4):243-53.
23 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.
24 Allelic variants of human cytochrome P450 1A1 (CYP1A1): effect of T461N and I462V substitutions on steroid hydroxylase specificity. Pharmacogenetics. 2000 Aug;10(6):519-30.
25 Metabolism of tamoxifen by recombinant human cytochrome P450 enzymes: formation of the 4-hydroxy, 4'-hydroxy and N-desmethyl metabolites and isomerization of trans-4-hydroxytamoxifen. Drug Metab Dispos. 2002 Aug;30(8):869-74.
26 Cytochrome P450 isoforms catalyze formation of catechol estrogen quinones that react with DNA. Metabolism. 2007 Jul;56(7):887-94.
27 Preferred orientations in the binding of 4'-hydroxyacetanilide (acetaminophen) to cytochrome P450 1A1 and 2B1 isoforms as determined by 13C- and 15N-NMR relaxation studies. J Med Chem. 1994 Mar 18;37(6):860-7.
28 The influence of metabolic gene polymorphisms on urinary 1-hydroxypyrene concentrations in Chinese coke oven workers. Sci Total Environ. 2007 Aug 1;381(1-3):38-46.
29 Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: particular efficiency and regioselectivity of P450 2Cs. Biochemistry. 1999 Oct 26;38(43):14264-70.
30 A common CYP1B1 polymorphism is associated with 2-OHE1/16-OHE1 urinary estrone ratio. Clin Chem Lab Med. 2005;43(7):702-6.
31 Cytochromes P450 in crustacea. Comp Biochem Physiol C Pharmacol Toxicol Endocrinol. 1998 Nov;121(1-3):157-72.
32 Disruption of endogenous regulator homeostasis underlies the mechanism of rat CYP1A1 mRNA induction by metyrapone. Biochem J. 1998 Apr 1;331 ( Pt 1):273-81.
33 Pharmacogenomics in drug-metabolizing enzymes catalyzing anticancer drugs for personalized cancer chemotherapy. Curr Drug Metab. 2007 Aug;8(6):554-62.
34 Inhibitory effects of anticancer drugs on dextromethorphan-O-demethylase activity in human liver microsomes. Cancer Chemother Pharmacol. 1993;32(6):491-5.
35 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.
36 CYP2D6 polymorphisms and tamoxifen metabolism: clinical relevance. Curr Oncol Rep. 2010 Jan;12(1):7-15.
37 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.
38 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.
39 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.
40 Effects of propofol on human hepatic microsomal cytochrome P450 activities. Xenobiotica. 1998 Sep;28(9):845-53.
41 Pharmacogenetics of schizophrenia. Am J Med Genet. 2000 Spring;97(1):98-106.
42 Roles of CYP2A6 and CYP2B6 in nicotine C-oxidation by human liver microsomes. Arch Toxicol. 1999 Mar;73(2):65-70.
43 Structure-activity relationship for human cytochrome P450 substrates and inhibitors. Drug Metab Rev. 2002 Feb-May;34(1-2):69-82.