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Quantitative evaluation of brain distribution and blood-brain barrier efflux transport of probenecid in rats by microdialysis: possible involvement of the monocarboxylic acid transport system.
TLDR
The data suggest that the restricted distribution of probenecid in the brain may be ascribed to efficient efflux from the brain ISF, which may be regulated by the monocarboxylic acid transport system at a relatively high ISF concentration.
Hydroxylation and methylthiolation of mono-ortho-substituted polychlorinated biphenyls in rats: identification of metabolites with tissue affinity.
TLDR
Another metabolism of mono-ortho-PCBs PCBs involved methylthiolation in the vicinal ortho and meta unsubstituted positions to give methylthio metabolites, which were detected as methylsulfonyl metabolites in liver and adipose tissue.
Mechanism of nasal absorption of drugs I: Physicochemical parameters influencing the rate of in situ nasal absorption of drugs in rats.
TLDR
The in situ technique can be used to predict in vivo absorption rate constants for propranolol and L-tyrosine when volumes of 0.1 mL were administered, and the calculated values were found to be close to those determined in in vivo experiments.
IDENTIFICATION OF SULFUR-CONTAINING METABOLITES OF p-DICHLOROBENZENE AND THEIR DISPOSITION IN RATS
The structure of two sulfur-containing metabolites of p-dichlorobenzene (p-DCB), the distribution of p-DCB and the metabolites in the blood and some tissues, and the excretion of the metabolites in
Relationship between brain serotonin transporter binding, plasma concentration and behavioural effect of selective serotonin reuptake inhibitors
TLDR
The present study has provided the first in vivo evidences to support that fluvoxamine, fluoxetine, parxetine and sertraline orally administered bind to the pharmacologically relevant brain SERT in mice and that their SERT‐binding characteristics is closely associated with the pharmacokinetics and inhibition of marble‐burying behaviour.
Blood-Brain Barrier Transport of 125I-Labeled Basic Fibroblast Growth Factor
TLDR
The results suggest that 125I-bFGF is transported acrossthe BBB, possibly by an adsorptive-mediated transcytosis mechanism that is triggered by binding to negatively charged species on the luminalmembrane surface of the brain microvasculature, such as heparansulfate proteoglycans.
Muscarinic receptor binding characteristics in rat tissues after oral administration of oxybutynin and propiverine.
TLDR
It is shown that oxybutynin and propiverine, after oral administration, bind significantly to muscarinic receptors in tissues such as the bladder, which is the target organ for the treatment of urinary incontinence, and that oxy butynin appears to exhibit long-term binding to musCarinic receptor in the salivary gland.
In vivo measurement by [3H]Tamsulosin of alpha1 adrenoceptors in rat tissues in relation to the pharmacokinetics.
TLDR
It is suggested that [3H]tamsulosin is a useful radioligand for in vivo measurement of alpha1 adrenoceptors in rat tissues and binds to alpha1A subtype with higher affinity than alpha1B subtype in vivo.
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