Pharmacokinetics of Pentazocine and Its Occupancy of Opioid Receptors in Rat Brain
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概要
- 論文の詳細を見る
In order to assess quantitatively the pharmacodynamic process of pentazocine (PTZ), time courses of its plasma concentration and of the occupation of specific opioid receptors in the brain were investigated after intravenous (i.v.) administration of PTZ to rats. The plasma concentration of PTZ was determined by HPLC and the pharmacokinetic parameters were analyzed using nonlinear least-squares analysis. Measurement of ex vivo receptor occupation was made by comparing the specific [^3H]naloxone (opioid receptor antagonist) binding in vitro to the crude P_2-synaptosomal fractions between vehicle-treated rats (control) and PTZ-treated rats. Following the i.v. administration of PTZ, the occupancy of specific opioid receptors decreased rapidly until 10 min, depending on the two pharmacological doses (2.5 and 10 mg/kg). The results strongly suggest the fast binding kinetics of PTZ in terms of its association with and dissociation from specific opioid receptor sites in the brain in addition to its fast rate of disappearance from the brain compartment. Furthermore, we demonstrated that the time profile of receptor occupancy correlated well (r=0.8650) with that of the unbound concentration in plasma until 120 min after the i.v. administration of PTZ to rats.
- 公益社団法人日本薬学会の論文
- 1997-11-15
著者
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Suzuki T
Department Of Biochemistry University Of Shizuoka School Of Pharmaceutical Sciences:core Research Fo
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Hanano Manabu
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Tokyo
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SUZUKI Toyofumi
Department of Pharmaceutics, College of Pharmacy, Nihon University
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Hanano Manabu
Faculty Of Pharmaceutical Sciences University Of Tokyo
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Hanano M
Department Of Pharmaceutics College Of Pharmacy Nihon University
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Hanano M
Department Of Pharmaceutical Science College Of Pharmacy Nihon University
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NISHINO Junichi
Department of Chemistry, Nagaoka University of Technology
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Hanano M
Faculty Of Pharmaceutical Sciences University Of Tokyo
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Hanano Manabu
Department Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Nagoya City University:department
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SUGANUMA Taiyo
Department of Medical Eudcation, Tokyo Women's Medical University School of Medicine
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Suganuma Taiyo
(pressent Address)department Of Pharmacology Tokyo Women's Medical University
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Suganuma Taiyo
Department Of Medical Eudcation Tokyo Women's Medical University School Of Medicine
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Suzuki Takashi
Department Of Biochemistry University Of Shizuoka School Of Pharmaceutical Sciences:core Research Fo
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Nishino Junichi
(pressent Address)drug Regulatory Affairs Department Navartis Pharma K.k.
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Nishino Junichi
Department Of Chemistry Nagaoka University Of Technolgy
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Suganuma Taiyo
Department Of Medical Education Tokyo Women's Medical University
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