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Substance P receptor antagonist I: conversion of phosphoramidate prodrug after i.v. administration to rats and dogs

Autor: S E, Huskey, D, Luffer-Atlas, B J, Dean, E M, McGowan, W P, Feeney, S H, Chiu

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 27(11)

A water-soluble phosphoramidate prodrug (L-758,298, compound I) of the potent and selective human Substance P receptor antagonist L-754, 030 (compound II) is under development as an i.v. drug for treatment of emesis, migraine, and chronic pain. Compo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::aa7ccc9aaa3f7c9f29050315811ac2c6
https://pubmed.ncbi.nlm.nih.gov/10534323

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N-glucuronidation reactions. III. Regioselectivity of N-glucuronidation of methylbiphenyl tetrazole, methylbiphenyl triazole, and methylbiphenyl imidazole using human and rat recombinant UDP-glucuronosyltransferases stably expressed in V79 cells

Autor: S E, Huskey, J, Magdalou, M, Ouzzine, G, Siest, S H, Chiu

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 22(4)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::c9164aa3d0aa1fb6484cedd146394c81
https://pubmed.ncbi.nlm.nih.gov/7956744

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N-glucuronidation reactions. I. Tetrazole N-glucuronidation of selected angiotensin II receptor antagonists in hepatic microsomes from rats, dogs, monkeys, and humans

Autor: S E, Huskey, R R, Miller, S H, Chiu

Publikováno v: Drug metabolism and disposition: the biological fate of chemicals. 21(5)

In vitro conditions for the preparation of tetrazole N2-glucuronides using liver microsomes (enriched with UDP-glucuronic acid) from rats, dogs, monkeys, and humans have been developed and optimized. The structures of tetrazole N2-glucuronides of 3 b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::6e14ad88f8c9732a255d40a229f11b01
https://pubmed.ncbi.nlm.nih.gov/7902238

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Site-directed mutagenesis of glutathione S-transferase YaYa. Important roles of tyrosine 9 and aspartic acid 101 in catalysis

Autor: R W, Wang, D J, Newton, S E, Huskey, B M, McKeever, C B, Pickett, A Y, Lu

Publikováno v: The Journal of biological chemistry. 267(28)

The roles of tyrosine 9 and aspartic acid 101 in the catalytic mechanism of rat glutathione S-transferase YaYa were studied by site-directed mutagenesis. Replacement of tyrosine 9 with phenylalanine (Y9F), threonine (Y9T), histidine (Y9H), or valine

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::729181f6f8b522d46cba47ca5040b296
https://pubmed.ncbi.nlm.nih.gov/1400302

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