The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein

التفاصيل البيبلوغرافية
العنوان: The brain entry of risperidone and 9-hydroxyrisperidone is greatly limited by P-glycoprotein
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