Diurnal Rhythmicity in the Transcription of Jejunal Drug Transporters†

Intestinal drug efflux proteins play a major role in the pharmacokinetics of many drugs. We assessed diurnal rhythmicity in the expression of ten major drug transporters. We acquired male Sprague-Dawley rats and harvested jejunal mucosa at 3-h intervals across a 24-h period. qPCR was performed for t...

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Main Authors: Adam T. Stearns (Author), Anita Balakrishnan (Author), David B. Rhoads (Author), Stanley W. Ashley (Author), Ali Tavakkolizadeh (Author)
Format: Book
Published: Elsevier, 2008-01-01T00:00:00Z.
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100 1 0 |a Adam T. Stearns  |e author 
700 1 0 |a Anita Balakrishnan  |e author 
700 1 0 |a David B. Rhoads  |e author 
700 1 0 |a Stanley W. Ashley  |e author 
700 1 0 |a Ali Tavakkolizadeh  |e author 
245 0 0 |a Diurnal Rhythmicity in the Transcription of Jejunal Drug Transporters† 
260 |b Elsevier,   |c 2008-01-01T00:00:00Z. 
500 |a 1347-8613 
500 |a 10.1254/jphs.08100SC 
520 |a Intestinal drug efflux proteins play a major role in the pharmacokinetics of many drugs. We assessed diurnal rhythmicity in the expression of ten major drug transporters. We acquired male Sprague-Dawley rats and harvested jejunal mucosa at 3-h intervals across a 24-h period. qPCR was performed for ten transporters: Mdr1, Mdr3, Mrp1 - 3, Mct1, Brcp, Pept1, Octn2, and Oatp-b. Rhythmicity was assessed with the cosinor procedure. Diurnal rhythmicity was observed for Mdr1, Mct1, Mrp2, Pept1, and Bcrp (1.6 - 5.4-fold-changes). Acrophases occurred during fasting hours. We conclude that many drug transporters display profound diurnal rhythms in transcription, which may underlie diurnal rhythms in drug pharmacokinetics. Keywords:: diurnal rhythm, intestinal, drug efflux transporter 
546 |a EN 
690 |a Therapeutics. Pharmacology 
690 |a RM1-950 
655 7 |a article  |2 local 
786 0 |n Journal of Pharmacological Sciences, Vol 108, Iss 1, Pp 144-148 (2008) 
787 0 |n http://www.sciencedirect.com/science/article/pii/S1347861319313866 
787 0 |n https://doaj.org/toc/1347-8613 
856 4 1 |u https://doaj.org/article/ae85e3d68e51418caf34b9c736d25b4f  |z Connect to this object online.