Tricyclic compounds inhibit the OATP1A2 transporter
نویسندگان
چکیده
منابع مشابه
Effects of b-Blockers and Tricyclic Antidepressants on the Activity of Human Organic Anion Transporting Polypeptide 1A2 (OATP1A2) s
The organic anion transporting polypeptide 1A2 (OATP1A2), a membrane drug transporter expressed on important organs (such as the brain, kidney, and intestine) may be a key element in the disposition of drugs. Previous studies demonstrated that it could transport a broad spectrum of substrates, including endogenous molecules and clinically relevant drugs, such as several b-blockers and 3-hydroxy...
متن کاملEffects of β-blockers and tricyclic antidepressants on the activity of human organic anion transporting polypeptide 1A2 (OATP1A2).
The organic anion transporting polypeptide 1A2 (OATP1A2), a membrane drug transporter expressed on important organs (such as the brain, kidney, and intestine) may be a key element in the disposition of drugs. Previous studies demonstrated that it could transport a broad spectrum of substrates, including endogenous molecules and clinically relevant drugs, such as several β-blockers and 3-hydroxy...
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Prion diseases currently have no effective therapy. These illnesses affect both animal and human populations, and are characterized by the conformational change of a normal self protein PrP(C) (C for cellular) to a pathological and infectious conformer, PrP(Sc) (Sc for scrapie). We used a well characterized tissue culture model of prion infection, where mouse neuroblastoma cells (N2a) were infe...
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Neurotransmitter transporters are present in nerve terminal membranes and are responsible for the inactivation of released neurotransmitter by reuptake. One such transporter is the serotonin transporter which also represents the site of action of many clinically used tricyclic antidepressants, such as imipramine. Recently, most of the known Na+-dependent neurotransmitter transporters have been ...
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Based on the crystal structure of LeuTAa, a bacterial homologue to the Na+/Cl--dependent neurotransmitter transporters (SLC6 family) from Aquifex aeolicus, it was proposed that inhibitors of the serotonin and norepinephrine transporters (i.e., tricyclic antidepressants, TCAs) bind in the outer vestibule of the transporter and thus occlude access of the substrate to the substrate binding site. T...
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ژورنال
عنوان ژورنال: The FASEB Journal
سال: 2013
ISSN: 0892-6638,1530-6860
DOI: 10.1096/fasebj.27.1_supplement.674.2