The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein
العنوان: | The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein |
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المؤلفون: | Robin M. Taylor, Jennifer L. Donovan, Jun-Sheng Wang, John S. Markowitz, C. Lindsay DeVane, Ying Ruan |
المصدر: | The International Journal of Neuropsychopharmacology. 7:415-419 |
بيانات النشر: | Oxford University Press (OUP), 2004. |
سنة النشر: | 2004 |
مصطلحات موضوعية: | Male, medicine.medical_treatment, ATPase, Intraperitoneal injection, Mice, Transgenic, Pharmacology, Blood–brain barrier, Mice, Paliperidone Palmitate, medicine, Animals, Tissue Distribution, Pharmacology (medical), ATP Binding Cassette Transporter, Subfamily B, Member 1, Chromatography, High Pressure Liquid, Active metabolite, P-glycoprotein, Risperidone, biology, Chemistry, Brain, Isoxazoles, Endothelial stem cell, Psychiatry and Mental health, Pyrimidines, medicine.anatomical_structure, Knockout mouse, biology.protein, Serotonin Antagonists, Injections, Intraperitoneal, medicine.drug |
الوصف: | P-glycoprotein (P-gp) in the brain capillary endothelial cell limits the entry of many drugs into the brain. Our previous in-vitro study using ATPase as a marker of P-gp activity suggested that risperidone might be effectively transported by P-gp. In the present study, we compared the concentrations of risperidone and its major pharmacologically active metabolite 9-hydroxyrisperidone (9-OH-risperidone), in plasma, brain and various other tissues between abcb1ab-/- knockout mice which are functionally devoid of P-gp in their blood-brain barrier vs. FVB wild-type mice. One hour after intraperitoneal injection of 4 microg/g risperidone, the brain concentrations and ratios of brain:plasma concentrations of risperidone (13.1-fold and 12-fold respectively, p |
تدمد: | 1469-5111 1461-1457 |
URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c44283df69844af55a238ecd86ea9a24 https://doi.org/10.1017/s1461145704004390 |
حقوق: | OPEN |
رقم الأكسشن: | edsair.doi.dedup.....c44283df69844af55a238ecd86ea9a24 |
قاعدة البيانات: | OpenAIRE |
تدمد: | 14695111 14611457 |
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