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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/10/09 06:57:41」(JST)

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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]

References[edit]

^ 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. doi:10.1038/sj.clpt.6100050. edit

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1. 薬理ゲノム学の概要 overview of pharmacogenomics

English Journal

Inhibition of peripheral dopamine metabolism and the ventilatory response to hypoxia in the rat.

Bialkowska M1, Zajac D, Mazzatenta A, Di Giulio C, Pokorski M.
Advances in experimental medicine and biology.Adv Exp Med Biol.2015;837:9-17. doi: 10.1007/5584_2014_72.
Dopamine (DA) is a putative neurotransmitter in the carotid body engaged in the generation of the hypoxic ventilatory response (HVR). However, the action of endogenous DA is unsettled. This study seeks to determine the ventilatory effects of increased availability of endogenous DA caused by inhibiti
PMID 25310955

Time- and NADPH-dependent inhibition of cytochrome P450 3A4 by the cyclopentapeptide cilengitide: significance of the guanidine group and accompanying spectral changes.

Bojić M1, Barbero L1, Dolgos H1, Freisleben A1, Gallemann D1, Riva S1, Guengerich FP2.
Drug metabolism and disposition: the biological fate of chemicals.Drug Metab Dispos.2014 Sep;42(9):1438-46. doi: 10.1124/dmd.114.059295. Epub 2014 Jul 1.
Cilengitide is a stable cyclic pentapeptide containing an Arg-Gly-Asp motif responsible for selective binding to αVβ3 and αVβ5 integrins. The candidate drug showed unexpected inhibition of cytochrome P450 (P450) 3A4 at high concentrations, that is, a 15-mM concentration caused attenuation of P45
PMID 24985702

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

Japanese Journal

Effect of Cyclosporine and Tacrolimus on Cytochrome P450 Activities in Human Liver Microsomes

丹羽俊朗,山本幸子,斎藤美穂 [他],白神歳文,高木明
藥學雜誌 127(1), 209-216, 2007-01-01
… The effects of cyclosporine and tacrolimus on cytochrome P450 (CYP) 1A2-mediated 7-ethoxyresorufin O-deethylation, CYP2C9-mediated tolbutamide hydroxylation, CYP2C19-mediated S-mephenytoin 4'-hydroxylation, CYP2D6-mediated debrisoquine 4-hydroxylation, CYP2E1-mediated chlorzoxazone 6-hydroxylation, CYP3A4-mediated nifedipine oxidation, and CYP3A4-mediated testosterone 6β-hydroxylation activities in human liver microsomes were compared. …
NAID 110006155027

Effects of Serotonin-3 Receptor Antagonists on Cytochrome P450 Activities in Human Liver Microsomes(Biopharmacy)

Niwa Toshiro,Yamamoto Sachiko,Saito Miho [他],KOBAYASHI Naoto,IKEDA Kaoru,NODA Yasuo,TAKAGI Akira
Biological & pharmaceutical bulletin 29(9), 1931-1935, 2006-09-01
… The effects of three serotonin-3 (5-HT_3) receptor antagonists, azasetron, ondansetron, and ramosetron, on cytochrome P450 (CYP) 1A2-mediated 7-ethoxyresorufin O-deethylation, CYP2C9-mediated tolbutamide hydroxylation, CYP2C19-mediated S-mephenytoin 4'-hydroxylation, CYP2D6-mediated debrisoquine 4-hydroxylation, CYP2E1-mediated chlorzoxazone 6-hydroxylation, CYP3A4-mediated nifedipine oxidation, and CYP3A4-mediated testosterone 6β-hydroxylation activities in human liver microsomes were compared. …
NAID 110005602364

Effect of Antifungal Drugs on Cytochrome P450 (CYP) 1A2, CYP2D6, and CYP2E1 Activities in Human Liver Microsomes(Biopharmacy)

Niwa Toshiro,Inoue-Yamamoto Sachiko,Shiraga Toshifumi [他],TAKAGI Akira
Biological and Pharmaceutical Bulletin 28(9), 1813-1816, 2005-09-01
… The effects of five antifungal drugs, fluconazole, itraconazole, micafungin, miconazole, and voriconazole, on cytochrome P450 (CYP) 1A2-mediated 7-ethoxyresorufin O-deethylation, CYP2D6-mediated debrisoquine 4-hydroxylation, and CYP2E1-mediated chlorzoxazone 6-hydroxylation activities in human liver microsomes were compared. …
NAID 110003666521

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★リンクテーブル★

リンク元

「デブリソキン」

Debrisoquine
	IUPAC name 1,2,3,4-tetrahydroisoquinoline-2-carboximidamide
Identifiers
CAS number	1131-64-2
PubChem	2966
ChemSpider	2860
UNII	X31CDK040E
DrugBank	DB04840
KEGG	C13650
MeSH	Debrisoquine
ChEBI	CHEBI:34665
ChEMBL	CHEMBL169901
ATC code	C02CC04
Jmol-3D images	Image 1
	SMILES [N@H]=C(N)N2Cc1c(cccc1)CC2 ;
	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) ; Key: JWPGJSVJDAJRLW-UHFFFAOYSA-N 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 ;
Properties
Molecular formula	C10H13N3
Molar mass	175.23032
	(verify) (what is: /?); Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
	Infobox references

　　[★]

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。

[1] Debrisoquine - Compound Summary, PubChem.

[2] 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. doi:10.1038/sj.clpt.6100050. edit

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debrisoquine