Biomaterial Database

In vitro metabolism of sparteine by human liver: competitive inhibition by debrisoquine. 1982

S V Otton, and T Inaba, and W A Mahon, and W Kalow

Population data indicate that the genetic control is the same for the oxidation of sparteine and debrisoquine, although whether the level of control is regulatory or enzymatic is not clear. Therefore, the influence of debrisoquine on the rates of in vitro formation of the two dehydrogenated metabolites of sparteine in the 9000 x g supernatant fractions of human liver was examined. The interaction of these two drugs was competitive, indicating that the same form of cytochrome P450 is responsible for their biotransformation. Antipyrine at concentrations as high as 4 mM had no effect on sparteine oxidation.

UI	MeSH Term	Description	Entries
D007546	Isoquinolines	A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
D008099	Liver	A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.	Livers
D003647	Debrisoquin	An adrenergic neuron-blocking drug similar in effects to GUANETHIDINE. It is also noteworthy in being a substrate for a polymorphic cytochrome P-450 enzyme. Persons with certain isoforms of this enzyme are unable to properly metabolize this and many other clinically important drugs. They are commonly referred to as having a debrisoquin 4-hydroxylase polymorphism.	Debrisoquine,Tendor
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000983	Antipyrine	An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29)	Phenazone,Anodynin,Pyramidone
D013034	Sparteine	A quinolizidine alkaloid isolated from several FABACEAE including LUPINUS; SPARTIUM; and CYTISUS. It has been used as an oxytocic and an anti-arrhythmia agent. It has also been of interest as an indicator of CYP2D6 genotype.	7,14-Methano-2H,6H-dipyrido(1,2-a:1',2'-e)(1,5)diazocine, dodecahydro-, (7S-(7alpha,7aalpha,14alpha,14abeta))-,Lupinidin,Lupinidine,Pachycarpine,D-sparteine,Depasan Retard,Genisteine Alkaloid,L-Sparteine,Pachycarpine Sulfate (1:1), Pentahydrate, (7S-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine Hydrochloride, (7R-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine Hydrochloride, (7S-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine Hydroiodide, (7R-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine Monohydrochloride, (7R-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine Monohydroiodide, (7R-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine Sulfate,Sparteine Sulfate (1:1), (7S-(7alpha,7aalpha,14alpha,14aalpha))-Isomer,Sparteine Sulfate (1:1), (7S-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine Sulfate Anhydrous,Sparteine, (+)-Isomer,Sparteine, (-)-Isomer,Sparteine, (7R-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine, (7R-(7alpha,7abeta,14alpha,14abeta))-Isomer,Sparteine, (7S-(7alpha,7aalpha,14alpha,14aalpha))-Isomer,Sparteine, (7S-(7alpha,7aalpha,14alpha,14abeta))-Isomer,Sparteine, (7S-(7alpha,7abeta,14alpha,14abeta))-Isomer,alpha-Isosparteine,beta-Isosparteine,Anhydrous, Sparteine Sulfate,Sulfate Anhydrous, Sparteine,alpha Isosparteine,beta Isosparteine
D066298	In Vitro Techniques	Methods to study reactions or processes taking place in an artificial environment outside the living organism.	In Vitro Test,In Vitro Testing,In Vitro Tests,In Vitro as Topic,In Vitro,In Vitro Technique,In Vitro Testings,Technique, In Vitro,Techniques, In Vitro,Test, In Vitro,Testing, In Vitro,Testings, In Vitro,Tests, In Vitro,Vitro Testing, In