Role of P Glycoprotein in Absorption of Novel Antimalarial Drugs | Zendy

Andrew Crowe | Zendy; Kenneth F. Ilett | Zendy; Harin Karunajeewa | Zendy; Kevin T. Batty | Zendy; Timothy M. E. Davis | Zendy

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Role of P Glycoprotein in Absorption of Novel Antimalarial Drugs

Author(s) -

Andrew Crowe,

Kenneth F. Ilett,

Harin Karunajeewa,

Kevin T. Batty,

Timothy M. E. Davis

Publication year - 2006

Publication title -

antimicrobial agents and chemotherapy

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.07

H-Index - 259

eISSN - 1070-6283

pISSN - 0066-4804

DOI - 10.1128/aac.00708-06

Subject(s) - p glycoprotein , efflux , piperaquine , transporter , dihydroartemisinin , pharmacology , chemistry , mefloquine , artemisinin , absorption (acoustics) , biology , biochemistry , plasmodium falciparum , malaria , multiple drug resistance , immunology , antibiotics , gene , physics , acoustics

Bidirectional transport of four novel antimalarial compounds was determined using Caco-2 cell monolayers. P glycoprotein-mediated efflux was greatest for pyronaridine (5 to 20 μM) and low for naphthoquine (5 μM). With 20 μM naphthoquine, net efflux was blocked, suggesting saturation of the transporter. Piperaquine and dihydroartemisinin were not transported by the system.

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