Interindividual variability in the N‐sulphation of desipramine in human liver and platelets.

Romiti, P.; Giuliani, L.; Pacifici, Gian Maria

doi:10.1111/j.1365-2125.1992.tb03995.x

Cited by 19 publications

(8 citation statements)

References 34 publications

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“…Previously intense variation in the activity of desipramine N-sulfation in human liver was reported (Romiti et al, 1992). In the present study, we also observed a considerable variation in the activities of N-and O-sulfation among the HLCs used throughout the substrates tested.…”

Section: Discussionsupporting

confidence: 72%

“…Besides these quinolones, other amine drugs, desipramine and metoclopramide, have also been examined. These drugs were previously reported to be metabolized to N-sulfoconjugates in humans (Bateman et al, 1980;Romiti et al, 1992). Our present results clearly demonstrate that human SULT2A1 (hSULT2A1, ST2A3) is exclusively responsible for the N-sulfation of amine-containing quinolone drugs in the body.…”

supporting

confidence: 66%

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Selective Role of Sulfotransferase 2A1 (SULT2A1) in theN-Sulfoconjugation of Quinolone Drugs in Humans

Senggunprai¹,

Yoshinari²,

Yamazoe³

2009

Drug Metab Dispos

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ABSTRACT:N-Sulfoconjugation is a common metabolic pathway of amine compounds in vivo. In the present study, we investigated the N-sulfation of quinolones and other amine drugs (ciprofloxacin, moxifloxacin, garenoxacin, desipramine, and metoclopramide) to assess the contribution of specific human cytosolic sulfotransferases (SULTs) to the reactions using purified recombinant enzymes and human liver cytosols (HLCs). Among the enzymes examined, human (h) SULT2A1 exhibited N-sulfoconjugation activities toward all drugs tested, whereas the other five different forms (hSULT1A1, hSULT1A3, hSULT1B1, hSULT1C2, and hSULT1E1) showed no detectable activities except hSULT1A1 for garenoxacin sulfation. The N-sulfoconjugating activity of hSULT2A1 was highest toward moxifloxacin (

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Section: Discussionsupporting

confidence: 72%

supporting

confidence: 66%

Selective Role of Sulfotransferase 2A1 (SULT2A1) in theN-Sulfoconjugation of Quinolone Drugs in Humans

Senggunprai¹,

Yoshinari²,

Yamazoe³

2009

Drug Metab Dispos

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“…However, a study of N-sulphation of desipramine observed a 63-fold variation of levels of activity in platelets [188].…”

Section: Sulphotransferasesmentioning

confidence: 98%

Molecular basis of polymorphic drug metabolism

Daly

1995

J Mol Med

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Genetic polymorphisms with functional effects occur in many of the genes encoding drug metabolizing enzymes and are an important cause of adverse drug reaction. Recent advances in the understanding of the molecular genetics of drug-metabolizing enzymes, particularly the cytochromes P450, has enabled the molecular basis of several polymorphisms to be elucidated and genotyping assays using the polymerase chain reaction to be developed. Polymorphisms in this category include those in the cytochrome P450 genes CYP2D6, CYP2C19, CYP2A6, CYP2C9 and CYP2E1, the glutathione S-transferase genes GSTM1 and GSTT1 and the N-acetyltransferase gene NAT2. The molecular basis and importance to drug metabolism of the various polymorphisms as well as evidence for the existence of polymorphisms in other genes encoding drug-metabolizing enzymes such as the UDP-glucuronosyltransferases, the sulphotransferases and the methyltransferases are discussed.

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“…Blood samples (20 to 40 ml) were collected from the cord by opening the forceps and allowing blood to collect into heparinized tubes. The platelets were isolated as described elsewhere [19].…”

Section: Platelet Isolationmentioning

confidence: 99%

“…Considerable interindividual variability has been found in the hepatic rate of sulphation of ethinyloestradiol [18], desipramine [19] and minoxidil [20]. Phenol sulphotransferase seems to be under genetic control [21][22][23][24].…”

Section: Introductionmentioning

confidence: 99%

Interindividual variability of phenol‐ and catechol‐sulphotransferases in platelets from adults and newborns

Pacifici¹,

Marchi²

1993

Brit J Clinical Pharma

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(adult) and 4.80 ± 4.34 (newborn) pmol min-' mg-', respectively (P < 0.001). The coefficients of variation were 107% (adult) and 90% (newborn). The frequency distribution of sulphotransferase activity was positively skewed in both newborn and adult platelets. 4 Since sulphotransferase activity in platelets is well-expressed at birth and a prenatal development of sulphotransferase has been described in mid-gestational human foetal liver, the newborn should be able to sulphate drugs.

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Interindividual variability in the N‐sulphation of desipramine in human liver and platelets.

Cited by 19 publications

References 34 publications

Selective Role of Sulfotransferase 2A1 (SULT2A1) in theN-Sulfoconjugation of Quinolone Drugs in Humans

Selective Role of Sulfotransferase 2A1 (SULT2A1) in theN-Sulfoconjugation of Quinolone Drugs in Humans

Molecular basis of polymorphic drug metabolism

Interindividual variability of phenol‐ and catechol‐sulphotransferases in platelets from adults and newborns

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