Investigation on the influx transport mechanism of pentazocine at the blood-brain barrier in rats using the carotid injection technique - PubMed (original) (raw)
. 2002 Oct;25(10):1351-5.
doi: 10.1248/bpb.25.1351.
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- PMID: 12392093
- DOI: 10.1248/bpb.25.1351
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Investigation on the influx transport mechanism of pentazocine at the blood-brain barrier in rats using the carotid injection technique
Toyofumi Suzuki et al. Biol Pharm Bull. 2002 Oct.
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Abstract
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 (Jmax), 3.6 +/- 1.2 micromol/min/g brain and the apparent Michaelis constant (K1), 3.7 +/- 1.7 mM for the saturable component of PTZ into the brain, and the nonsaturable uptake rate constant (Kd), 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 H1-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.
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