Investigation on the Influx Transport Mechanism of Pentazocine at the Blood-Brain Barrier in Rats Using the Carotid Injection Technique(Biopharmacy)

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概要

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• The influx transport mechanism of pentazocine (PTZ) at the blood-brain barrier (BBB) was investigated in rats using the carotid injection technique. The uptake kinetics of PTZ into the rat brain exhibited saturability, which occurred by both nonsaturable and carrier-mediated transport processes. The in vivo kinetic parameters were estimated as follows : the maximal uptake rate (J_<max>), 3.6±1.2μmol/min/g brain and the apparent Michaelis constant (K_t), 3.7±1.7 m_M for the saturable component of PTZ into the brain, and the nonsaturable uptake rate constant (K_d), 0.06±0.04 ml/min/g brain. The uptake of PTZ by the brain was strongly inhibited by lidocaine, imipramine and propranolol, and also by H_1-antagonists such as mepyramine, diphenhydramine. In addition, narcotic-antagonist analgesic (buprenorphine, butorphanol or eptazocine) and an opioid antagonist (naloxone) significantly inhibited PTZ transport. These results suggest that PTZ permeates into the brain via a carrier-mediated transport system, which may widely recognize the cationic drugs.

• 公益社団法人日本薬学会の論文
• 2002-10-01

著者

• WATANABE Jun

  Department of Cardiovascular Medicine, Tohoku University Graduate School of Medicine

• Watanabe J

  School Of Pharmacy Aichi Gakuin University

• Suzuki T

  Department Of Biochemistry University Of Shizuoka School Of Pharmaceutical Sciences:core Research Fo

• Hanano Manabu

  Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Tokyo

• SUZUKI Toyofumi

  Department of Pharmaceutics, College of Pharmacy, Nihon University

• TOMONO Kazuo

  Department of Pharmaceutics, College of Pharmacy, Nihon University

• Tomono K

  Res. Unit Of Pharmaceutics Coll. Of Pharmacy Nihon Univ.

• Tomono K

  Nihon Univ. Chiba Jpn

• Tomono Kazuo

  Department Of Pharmaceutics College Of Pharmacy Nihon University

• Hanano Manabu

  Faculty Of Pharmaceutical Sciences University Of Tokyo

• Hanano M

  Department Of Pharmaceutics College Of Pharmacy Nihon University

• Hanano M

  Department Of Pharmaceutical Science College Of Pharmacy Nihon University

• GOTO HIROKO

  Department of Pharmaceutics, College of Pharmacy, Nihon University

• Goto H

  Department Of Pharmaceutics College Of Pharmacy Nihon University

• Hanano M

  Faculty Of Pharmaceutical Sciences University Of Tokyo

• Hanano Manabu

  Department Of Biopharmaceutics Faculty Of Pharmaceutical Sciences Nagoya City University:department

• Suganuma Taiyo

  (pressent Address)department Of Pharmacology Tokyo Women's Medical University

• Watanabe J

  Department Of Pharmaceutics College Of Pharmacy Nihon University

• MORIKI Yoshiaki

  Department of Pharmaceutics, College of Pharmacy, Nihon University

• Moriki Yoshiaki

  Department Of Pharmaceutics College Of Pharmacy Nihon University

• Suzuki Takashi

  Department Of Biochemistry University Of Shizuoka School Of Pharmaceutical Sciences:core Research Fo

• Watanabe Jun

  Department Of Anatomy & Cell Science Kansai Medical University

• Goto Hiroko

  Department of Pediatric Cardiology, Gifu Prefectural General Medical Center

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