By Guofeng You, Marilyn E. Morris, Binghe Wang
A accomplished advisor to drug transporters that impression the absorption, distribution, and removal of gear within the physique the advance of strong expression cloning and genome research thoughts has facilitated the molecular id and characterization of diverse transporters that play a very important position in drug disposition. Explaining the rules of drug delivery and the linked suggestions, Drug Transporters: Molecular Characterization and position in Drug Disposition: * presents a accomplished review of drug transporters * comprises particular descriptions of transporter households, together with substrate and inhibitor specificity, subcellular and tissue localization, mechanisms governing delivery, species transformations, the scientific implications of those transporters in human body structure and sickness, and their position in drug distribution, removing, and interactions in drug treatment * Describes transporter-mediated drug disposition, a newly rising box in drug treatment * supplies a accomplished precis of drug delivery throughout organic membranes * within the liver, mind, kidney, and gut * presents balanced insurance of mechanistic points and practical results * good points chapters contributed through unusual scientists of their uniqueness components * presents enough element to permit non-specialists to appreciate the foundations and strategies This authoritative advisor is a pragmatic hands-on table reference for researchers in academia and the pharmaceutical and scientists in govt enterprises. it's also a great textual content for graduate-level classes within the pharmaceutical and pharmacology fields.
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Extra resources for Drug Transporters: Molecular Characterization and Role in Drug Disposition
2000. Basolateral localization of organic cation transporter 2 in intact renal proximal tubules. Am J Physiol Renal Physiol 279(5):F826–F834. 47. Motohashi H, Sakurai Y, Saito H, Masuda S, Urakami Y, Goto M, Fukatsu A, Ogawa O, Inui K. 2002. Gene expression levels and immunolocalization of organic ion transporters in the human kidney. J Am Soc Nephrol 13(4):866–874. 48. Dudley AJ, Bleasby K, Brown CD. 2000. The organic cation transporter OCT2 mediates the uptake of beta-adrenoceptor antagonists across the apical membrane of renal LLC-PK(1) cell monolayers.
J Pharmacol Exp Ther 300(3):918–924. 39. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V. 1998. Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem 273(49):32776–32786. 40. Eisenhofer G. 2001. The role of neuronal and extraneuronal plasma membrane transporters in the inactivation of peripheral catecholamines. Pharmacol Ther 91(1):35–62. 41. Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H.
D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. D. Substrate 33 18 18,20 20,32 18,20 20,32 20,32 18 18 18 18,20 37 20,30 20,30 34 18,20 20 20,32 20,69 20,32 20 20 20,69 20,32 18,20 18,20 Refs. ” (not determined) for that isoform. a Includes compounds that have been tested as either substrates or inhibitors of any OCT isoform. 1. 2. 2 for details on tissue distribution of each OCT isoform. 15 The pharmacological signiﬁcance of OCT2 thus appears primarily to be its role in active secretion of organic cations in the kidney, facilitating the ﬁrst step (uptake of organic cations across the basolateral membrane) of active secretion.