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Effect of N-hydroxyethylpromethazine (Aprobit®) on the distribution of 35S-chlorpromazine studied by autoradiography in cats and mice

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Summary

The effect of a quaternary phenothiazine compound, N-hydroxyethylpromethazine (Aprobit®, NHP), on the distribution of 35S-chlorpromazine (36S-CPZ) was studied in mice and cats using an autoradiographic technique. NHP did not change the sedative action of CPZ or ether but it caused a strong relaxation of the nictitating membrane, mydriasis and shivering in all cats.

A pronounced accumulation of 35S-CPZ was recorded in the inferior cervical ganglion of the cat during the entire 16 h period of observation. In addition to the lung parenchyma a strong activity was concentrated in the bronchial mucosa and excretions. The uptake was very high in the brain, eye, liver, kidney, pancreas, oesophagic excretion, in the gastro-intestinal contents, salivary glands and especially in the sublingual gland.

The NHP-pretreatment increased the radioactivity in the sympathetic ganglia, sublingual glands, lungs, liver and bone marrow. NHP delayed the penetration of 35S-CPZ into the brain. At 16 h after the i.v. injection a stronger retention of the radioactivity in the cerebral tissue was observed in the NHP-pretreated animals. In pregnant mice NHP decreased the accumulation of 35S-CPZ or its metabolites in the fetuses.

The possible mechanism whereby NHP increases the retention of 35S-CPZ or its metabolites in the brain is discussed.

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Authors and Affiliations

  1. Department of Pharmacology, University of Helsinki, Helsinki, Finland

    J. E. Idänpään-Heikkilä, H. I. Vapaatalo & P. J. Neuvonen

Authors
  1. J. E. Idänpään-Heikkilä
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  2. H. I. Vapaatalo
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  3. P. J. Neuvonen
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This work was supported by the Finnish Medical Research Council.

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Idänpään-Heikkilä, J.E., Vapaatalo, H.I. & Neuvonen, P.J. Effect of N-hydroxyethylpromethazine (Aprobit®) on the distribution of 35S-chlorpromazine studied by autoradiography in cats and mice. Psychopharmacologia 13, 1–13 (1968). https://doi.org/10.1007/BF00401613

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  • DOI: https://doi.org/10.1007/BF00401613

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