Autoradiographic analysis of the in vivo distribution of 3H-imipramine and 3H-desipramine in brain: Comparison to in vitro binding patterns

Journal Article · Fri Mar 01 00:00:00 EST 1991 · Pharmacology, Biochemistry and Behavior; (United States)

DOI:https://doi.org/10.1016/0091-3057(91)90024-V· OSTI ID:5323499

Duncan, G E; Paul, I A; Fassberg, J B; Powell, K R; Stumpf, W E; Breese, G R ^[1]

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1. Department of Cell Biology and Anatomy, School of Medicine, University of North Carolina, Chapel Hill (USA)

Using high resolution autoradiographic techniques, the distribution of radioactivity in forebrain and brainstem was assessed after 4 injection of 3H-impramine or 3H-desipramine. Results were compared with regional binding of the drugs to brain sections in vitro. Similar topographic binding of 3H-imipramine and 3H-desipramine was observed in vitro among brain regions, except in the paraventricular nucleus of the hypothalamus and locus coeruleus, where binding was greater for 3H-desipramine. For both 3H-desipramine and 3H-imipramine, some brain regions that exhibited high binding in vitro also showed high accumulation after in vivo injection. However, certain regions that contained high densities of binding sites for the antidepressant drugs as measured by in vitro binding showed very low accumulation of radioactivity after in vivo treatment. Such regions included the dentate gyrus of the hippocampus, layer 1 of piriform cortex, caudate-putamen, pontine and midbrain central gray, and cerebellar granular layer. Compared to in vitro binding of the drugs, the distribution of imipramine and desipramine in vivo appears more anatomically selective. For imipramine, primary sites of action in vivo, as indicated by the topographic distribution in brain, appear to be the locus coeruleus, hippocampus, lateral septal nucleus, and amygdala. For desipramine, the greatest accumulation in vivo was found in the locus coeruleus, paraventricular nucleus of the hypothalamus, and anterior thalamic nuclei.

• OSTI ID: 5323499
• Journal Information: Pharmacology, Biochemistry and Behavior; (United States), Vol. 38:3; ISSN 0091-3057
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
AMINES
TISSUE DISTRIBUTION
AUTORADIOGRAPHY
BIOCHEMICAL REACTION KINETICS
BRAIN
COMPARATIVE EVALUATIONS
IMIPRAMINE
IN VITRO
RATS
TRITIUM COMPOUNDS
ANIMALS
ANTIDEPRESSANTS
BODY
CENTRAL NERVOUS SYSTEM
CENTRAL NERVOUS SYSTEM AGENTS
DISTRIBUTION
DRUGS
EVALUATION
HETEROCYCLIC COMPOUNDS
HYDROGEN COMPOUNDS
KINETICS
MAMMALS
NERVOUS SYSTEM
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PSYCHOTROPIC DRUGS
REACTION KINETICS
RODENTS
VERTEBRATES
550201* - Biochemistry- Tracer Techniques