デブリソキン
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2020/02/25 05:25:53」(JST)
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Debrisoquine[1]
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| Names
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| IUPAC name
1,2,3,4-tetrahydroisoquinoline-2-carboximidamide
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| Identifiers
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CAS Number
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3D model (JSmol)
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| ChEBI
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| DrugBank
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| ECHA InfoCard
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100.013.155
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| KEGG
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| MeSH
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Debrisoquine
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| UNII
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InChI
InChI=1S/C10H13N3/c11-10(12)13-6-5-8-3-1-2-4-9(8)7-13/h1-4H,5-7H2,(H3,11,12) Y Key: JWPGJSVJDAJRLW-UHFFFAOYSA-N Y InChI=1/C10H13N3/c11-10(12)13-6-5-8-3-1-2-4-9(8)7-13/h1-4H,5-7H2,(H3,11,12) Key: JWPGJSVJDAJRLW-UHFFFAOYAE
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SMILES
[N@H]=C(N)N2Cc1c(cccc1)CC2
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| Properties
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Chemical formula
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C10H13N3
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| Molar mass
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175.23032
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| Pharmacology
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ATC code
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C02CC04 (WHO)
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Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). |
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| Infobox references
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Debrisoquine is a derivative of guanidine. It is an antihypertensive drug similar to guanethidine. Debrisoquine is frequently used for phenotyping the CYP2D6 enzyme, a drug-metabolizing enzyme.[2]
See also
- Isoquinoline#Applications of derivatives
The guanidine part of the molecule also appears in guanoxan and guanadrel.
- The 7-bromo analog of Debrisoquine is called Guanisoquin.
References
- ^ Debrisoquine – Compound Summary, PubChem.
- ^ Fuhr, U.; Jetter, A.; Kirchheiner, J. (2007). "Appropriate Phenotyping Procedures for Drug Metabolizing Enzymes and Transporters in Humans and Their Simultaneous Use in the "Cocktail" Approach". Clinical Pharmacology & Therapeutics. 81 (2): 270–283. doi:10.1038/sj.clpt.6100050.
Sympatholytic (and closely related) antihypertensives (C02) |
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Sympatholytics
(antagonize α-adrenergic
vasoconstriction) | | Central | | α2 agonist |
- Clonidine
- Guanabenz
- Guanfacine
- Methyldopa#
- Tiamenidine‡
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| Adrenergic release inhibitors |
- Bethanidine
- Bretylium
- Debrisoquine
- Guanadrel
- Guanazodine
- Guanethidine
- Guanoclor
- Guanoxabenz
- Guanoxan
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| Imidazoline receptor agonist |
- Moxonidine
- Rilmenidine
- Tolonidine
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| Ganglion-blocking/nicotinic antagonist |
- Hexamethonium‡
- Mecamylamine
- Pentolinium
- Trimethaphan
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| Peripheral | | Indirect | | MAOI | |
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| Adrenergic uptake inhibitor |
- Bietaserpine
- Deserpidine
- Methoserpidine
- Rescinnamine
- Reserpine
- Syrosingopine
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| Tyrosine hydroxylase inhibitor | |
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| Direct | | α1 blockers |
- Prazosin
- Indoramin
- Trimazosin
- Doxazosin
- Urapidil
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| Non-selective α blocker | |
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| Other antagonists | | Serotonin antagonist | |
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| Endothelin antagonist (for PH) |
- dual (Bosentan, Macitentan)
- selective (Ambrisentan, Sitaxentan)
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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English Journal
- Cytochrome b5 is a major determinant of human cytochrome P450 CYP2D6 and CYP3A4 activity in vivo.
- Henderson CJ1, McLaughlin LA1, Scheer N1, Stanley LA1, Wolf CR2.
- Molecular pharmacology.Mol Pharmacol.2015 Apr;87(4):733-9. doi: 10.1124/mol.114.097394. Epub 2015 Feb 5.
- The cytochrome P450-dependent mono-oxygenase system is responsible for the metabolism and disposition of chemopreventive agents, chemical toxins and carcinogens, and >80% of therapeutic drugs. Cytochrome P450 (P450) activity is regulated transcriptionally and by the rate of electron transfer from
- PMID 25657337
- CYP2D6 -1584C>G promoter polymorphism and debrisoquine ultrarapid hydroxylation in healthy volunteers.
- Llerena A1, Dorado P, Ramírez R, Calzadilla LR, Peñas-Lledó E, Álvarez M, Naranjo ME, González I, Pérez B; CEIBA Consortium of Ibero–American Network of Pharmacogenetics & Pharmacogenomics RIBEF.
- Pharmacogenomics.Pharmacogenomics.2013 Dec;14(16):1973-7. doi: 10.2217/pgs.13.181.
- BACKGROUND & AIM: The CYP2D6 -1584C>G polymorphism (rs1080985) has been identified as a major factor for CYP2D6 expression and function, with the mutant -1584G promoter type being consistently associated with significantly greater expression than -1584C. It may therefore be associated with ul
- PMID 24279852
- Molecular insight into affinities of drugs and their metabolites to lipid bilayers.
- Paloncýová M1, Berka K, Otyepka M.
- The journal of physical chemistry. B.J Phys Chem B.2013 Feb 28;117(8):2403-10. doi: 10.1021/jp311802x. Epub 2013 Feb 19.
- The penetration properties of drug-like molecules on human cell membranes are crucial for understanding the metabolism of xenobiotics and overall drug distribution in the human body. Here, we analyze partitioning of substrates of cytochrome P450s (caffeine, chlorzoxazone, coumarin, ibuprofen, and de
- PMID 23387302
Japanese Journal
- Ethnic Differences in Genetic Polymorphisms of CYP2D6, CYP2C19, CYP3As and MDR1/ABCB1
- Evaluation of approach to predict the contribution of multiple cytochrome P450s in drug metabolism using relative activity factor: Effects of the differences in expression levels of NADPH-cytochrome P450 reductase and cytochrome b5 in the expression system and the differences in the marker activities
- Analysis of the CYP2D6 gene in relation to debrisoquin and desipramine hydroxylation in a Swedish population
Related Links
- Debrisoquin information including symptoms, causes, diseases, symptoms, treatments, and other medical and health issues. ... Introduction: Debrisoquin Description of Debrisoquin Debrisoquin: 3,4-dihydro-2(H ...
- Buy Debrisoquin sulfate (CAS 581-88-4), an antihypertensive that is an useful indicator for cytochrome P-450 polymorphism, from Santa Cruz. MW: 448.54 ... 同義語 Isocaramidine sulfate; Ro 5-3307 アプリケーション： An ...
★リンクテーブル★
[★]
- 英
- debrisoquine、debrisoquin
- 化
- 硫酸デブリソキン debrisoquine sulphate
- 降圧薬、グアニジン誘導体、末梢性交感神経遮断。現在は使われていない。