Accelerated Communication

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Accelerated Communication HUMAN UGT2B7 CATALYZES MORPHINE GLUCURONIDATION

A human UDP-glucuronosyltransferase (UGT) catalyzing the glucuronidation of morphine has been identified. A full length cDNA was isolated from a human liver cDNA library and found to be identical to the UGT2B7 form having a tyrosine at position 268. This cDNA was transfected into HK 293 cells, and stable expression was achieved. Cell homogenates and membrane preparations from HK 293 cells expre...

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ACCELERATED COMMUNICATION Mdr1 Limits CYP3A Metabolism in Vivo

We determined whether the drug efflux protein P-glycoprotein (Pgp) could influence the extent of CYP3A-mediated metabolism of erythromycin, a widely used model substrate for CYP3A. We compared CYP3A metabolism of erythromycin (a Pgp substrate) using the erythromycin breath test in mice proficient and deficient of mdr1 drug transporters. We first injected mdr1(1/1) mice with [C]N-methyl erythrom...

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ACCELERATED COMMUNICATION Regulation of Smad-Mediated Gene Transcription by RGS3

Regulator of G protein signaling (RGS) proteins are united into a family by the presence of the homologous RGS domain that binds the subunits of heterotrimeric G proteins and accelerates their GTPase activity. A member of this family, RGS3 regulates the signaling mediated by Gq and Gi proteins by binding the corresponding G subunits. Here we show that RGS3 interacts with the novel partners Smad...

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ACCELERATED COMMUNICATION Iodo-Resiniferatoxin, a New Potent Vanilloid Receptor Antagonist

The highly potent vanilloid receptor (VR) agonist resiniferatoxin has been radiolabeled with I, and the pharmacology to the cloned rodent VR, VR1, and the endogenous VR in rat spinal cord membranes has been characterized. [I]RTX binding to human embryonic kidney 293 cells expressing VR1 was reversible and with high affinity (Kd 5 4.3 nM) in an apparent monophasic manner. In rat spinal cord memb...

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Accelerated Communication METABOLIC SCREENING USING ON-LINE ULTRAFILTRATION MASS SPECTROMETRY

An on-line mass spectrometric method has been developed to generate and identify drug metabolites formed by hepatic cytochromes P450. This method, pulsed ultrafiltration-mass spectrometry, may be used for rapid screening of drugs to determine their extent of metabolism by microsomal cytochromes P450 and to characterize the primary metabolites. Rat liver microsomes were trapped in a stirred ultr...

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ژورنال

عنوان ژورنال: Life Sciences

سال: 1997

ISSN: 0024-3205

DOI: 10.1016/s0024-3205(97)01106-5