In vitro and in vivo effects of lead on specific 3H-MK-801 binding to NMDA-receptors in the brain of mice. 1995

S Schulte, and W E Müller, and K D Friedberg
Institut für Pharmakologie und Toxikologie Fakultät für Klinische Medizin Mannheim, Universität Heidelberg, Germany.

The in vitro and vivo effects of lead on the NMDA-receptors in adult and juvenile mice were studied by means of receptor binding assays. Adult female NMRI-mice received 100 and 1,000 ppm lead as nitrate in their drinking water for 30 and 90 days. Perinatal exposure was achieved by treating gestating mice from the 5th day post conception with 0, 100 or 1,000 ppm lead in their drinking water. Characterization of the NMDA N-methyl-D-aspartate)-receptor was carried out ex vivo using binding studies on homogenates of the forebrain with the non competitive NMDA-antagonist 3H-MK-801. In vitro, complete inhibition of the radioligand binding was found with half maximal inhibiting concentrations (IC50-values) of 19.7 +/- 2.6 microM (SEM) in absence of amino acids and 9.5 +/- 0.9 in presence of glutamate and glycine. These concentrations are in a range which could be achieved in vivo, e.g. the lead content in the forebrain of juvenile mice treated with 1,000 ppm lead was 10.0 +/- 1.8 mumol/kg wet weight. It was speculated that lead binds at the zinc binding site. In the presence of amino acids and divalent cations, such as calcium or magnesium, low lead concentrations lead to a significant increase in receptor affinity. Analysis of the saturation experiments carried out on forebrain homogenates of lead-treated animals showed a slight increase in receptor density of 13 or 15% with an unchanged Kd-value only in the adult animals treated with 100 ppm lead and in absence of stimulating amino acids.(ABSTRACT TRUNCATED AT 250 WORDS)

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D007854 Lead A soft, grayish metal with poisonous salts; atomic number 82, atomic weight 207.2, symbol Pb.
D009929 Organ Size The measurement of an organ in volume, mass, or heaviness. Organ Volume,Organ Weight,Size, Organ,Weight, Organ
D001835 Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms. Body Weights,Weight, Body,Weights, Body
D001921 Brain The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM. Encephalon
D005260 Female Females
D000375 Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. Senescence,Aging, Biological,Biological Aging
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding
D015032 Zinc A metallic element of atomic number 30 and atomic weight 65.38. It is a necessary trace element in the diet, forming an essential part of many enzymes, and playing an important role in protein synthesis and in cell division. Zinc deficiency is associated with ANEMIA, short stature, HYPOGONADISM, impaired WOUND HEALING, and geophagia. It is known by the symbol Zn.

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