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Related Experiment Videos

Chlorphentermine uptake by rabbit lung slices

L S Angevine, H M Mehendale

    Toxicology
    |January 1, 1980
    PubMed
    Summary

    Rabbit lung tissue actively uptakes chlorphentermine (CP) via a partially sodium-dependent process. This active transport mechanism influences pulmonary sequestration of CP, as demonstrated by uptake and binding studies.

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    Area of Science:

    • Pharmacology
    • Pulmonary Physiology
    • Cellular Transport Mechanisms

    Background:

    • Chlorphentermine (CP) is a lipophilic amine with known pulmonary accumulation.
    • Understanding the mechanisms of CP uptake is crucial for its pharmacokinetic and toxicological assessment.

    Purpose of the Study:

    • To investigate the mechanism of chlorphentermine (CP) uptake and sequestration in rabbit lung tissue.
    • To determine if CP uptake is an active, energy-dependent process and identify key factors influencing it.

    Main Methods:

    • Incubation of rabbit lung slices with radiolabeled [14C]chlorphentermine (CP).
    • Analysis of tissue (T) to medium (M) ratios for CP concentration and uptake kinetics.
    • Assessment of CP uptake and binding under varying ionic conditions, substrate concentrations, and in the presence of inhibitors.

    Main Results:

    • CP uptake reached a plateau with a significant tissue-to-medium ratio, indicating accumulation.
    • Uptake was concentration-dependent, saturable, and decreased with higher CP concentrations.
    • CP uptake was reduced by Na+-pump inhibitors (harmaline, iodoacetate), low temperature, and certain other amines, suggesting active transport.
    • Imipramine and amphetamine displaced accumulated CP, and inhibited CP binding to lung homogenates.

    Conclusions:

    • Pulmonary sequestration of CP involves a partially Na+-dependent, active uptake process.
    • These findings align with previous studies on intact lung preparations, reinforcing the understanding of CP's pulmonary disposition.

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