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Related Experiment Videos

P-glycoprotein does not actively transport nicotine and cotinine.

Jun-Sheng Wang1, John S Markowitz, Jennifer L Donovan

  • 1Laboratory of Drug Disposition and Pharmacogenetics, Department of Psychiatry and Behavioral Sciences, Medical University of South Carolina 49425, USA.

Addiction Biology
|September 30, 2005
PubMed
Summary
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P-glycoprotein (P-gp) does not actively transport nicotine or cotinine. These substances may utilize other transporters, influencing drug delivery across the blood-brain barrier and placenta.

Area of Science:

  • Pharmacology
  • Biochemistry
  • Genetics

Background:

  • P-glycoprotein (P-gp), encoded by ABCB1, is crucial at the blood-brain barrier (BBB) and placenta, regulating drug passage.
  • Conflicting research exists on P-gp's involvement in nicotine disposition.

Purpose of the Study:

  • To investigate the interaction between nicotine, its metabolite cotinine, and P-gp.
  • To clarify whether P-gp mediates the transport of nicotine and cotinine.

Main Methods:

  • Assessed P-gp ATPase activity using P-gp-rich membranes.
  • Measured inorganic phosphate (Pi) release as an indicator of nicotine and cotinine binding affinity to P-gp.
  • Utilized verapamil as a positive control.

Main Results:

Related Experiment Videos

  • Nicotine and cotinine showed modest stimulation of P-gp ATPase activity across a range of concentrations (5-1000 microm).
  • Calculated Clint values for nicotine and cotinine were low (0.01 and 0.007 min⁻¹ x 10⁻³).
  • Verapamil demonstrated significant P-gp ATPase stimulation (Clint 1.7 min⁻¹ x 10⁻³), validating the assay.

Conclusions:

  • Nicotine and cotinine are unlikely to be substrates for active efflux by P-gp.
  • Carrier-mediated transport of nicotine observed in cell lines may involve transporters other than P-gp.