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Title: Pituitary and brain D2 receptor density measured in vitro and in vivo in EEDQ treated male rats

Abstract

The effect of the alkylating compound N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on dopamine D2 receptor density in rat pituitary and brain was measured using in vitro and in vivo radioligand binding techniques. In the in vitro radioligand binding experiments EEDQ was found to reduce the density (B{sub max}) of ({sup 3}H)-spiperone binding sites in the striatum by 86% while in the pituitary the corresponding decrease was only 37%. The affinity (K{sub D}) of the remaining striatal and pituitary D2 receptors was not different in EEDQ treated animals as compared to controls. When D2 receptor density was measured in vivo the effect of EEDQ was less pronounced. Thus, in rats given EEDQ the specific binding of either of the two D2 ligands ({sup 3}H)-raclopride or ({sup 3}H)-spiperone in striatum and in the limbic forebrain was reduced by 45-62%; moreover, no significant decrease in pituitary D2 receptor density was observed. The data are discussed in relation to the finding that the same dose of EEDQ that failed to influence pituitary D2 receptor density as measured in vivo effectively antagonizes the prolactin decreasing effect of the partial D2 agonist (-)-3-(3-hydroxyphenyl)-N-n-propyl-piperidine ((-)-3-PPP).

Authors:
;  [1]
  1. Univ. of Goeteborg (Sweden)
Publication Date:
OSTI Identifier:
5945968
Resource Type:
Journal Article
Journal Name:
Life Sciences; (USA)
Additional Journal Information:
Journal Volume: 48:4; Journal ID: ISSN 0024-3205
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; ALKYLATING AGENTS; BIOCHEMICAL REACTION KINETICS; DOPAMINE; RECEPTORS; DENSITY; BRAIN; IN VITRO; IN VIVO; LIGANDS; PITUITARY GLAND; RATS; SPIPERONE; TRACER TECHNIQUES; TRITIUM COMPOUNDS; AMINES; ANIMALS; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENTS; BODY; CARDIOTONICS; CARDIOVASCULAR AGENTS; CENTRAL NERVOUS SYSTEM; DRUGS; ENDOCRINE GLANDS; GLANDS; HYDROGEN COMPOUNDS; HYDROXY COMPOUNDS; ISOTOPE APPLICATIONS; KINETICS; MAMMALS; MEMBRANE PROTEINS; NERVOUS SYSTEM; NEUROREGULATORS; ORGANIC COMPOUNDS; ORGANS; PHENOLS; PHYSICAL PROPERTIES; POLYPHENOLS; PROTEINS; REACTION KINETICS; RODENTS; SYMPATHOMIMETICS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Ekman, A, and Eriksson, E. Pituitary and brain D2 receptor density measured in vitro and in vivo in EEDQ treated male rats. United States: N. p., 1991. Web. doi:10.1016/0024-3205(91)90552-M.
Ekman, A, & Eriksson, E. Pituitary and brain D2 receptor density measured in vitro and in vivo in EEDQ treated male rats. United States. https://doi.org/10.1016/0024-3205(91)90552-M
Ekman, A, and Eriksson, E. 1991. "Pituitary and brain D2 receptor density measured in vitro and in vivo in EEDQ treated male rats". United States. https://doi.org/10.1016/0024-3205(91)90552-M.
@article{osti_5945968,
title = {Pituitary and brain D2 receptor density measured in vitro and in vivo in EEDQ treated male rats},
author = {Ekman, A and Eriksson, E},
abstractNote = {The effect of the alkylating compound N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on dopamine D2 receptor density in rat pituitary and brain was measured using in vitro and in vivo radioligand binding techniques. In the in vitro radioligand binding experiments EEDQ was found to reduce the density (B{sub max}) of ({sup 3}H)-spiperone binding sites in the striatum by 86% while in the pituitary the corresponding decrease was only 37%. The affinity (K{sub D}) of the remaining striatal and pituitary D2 receptors was not different in EEDQ treated animals as compared to controls. When D2 receptor density was measured in vivo the effect of EEDQ was less pronounced. Thus, in rats given EEDQ the specific binding of either of the two D2 ligands ({sup 3}H)-raclopride or ({sup 3}H)-spiperone in striatum and in the limbic forebrain was reduced by 45-62%; moreover, no significant decrease in pituitary D2 receptor density was observed. The data are discussed in relation to the finding that the same dose of EEDQ that failed to influence pituitary D2 receptor density as measured in vivo effectively antagonizes the prolactin decreasing effect of the partial D2 agonist (-)-3-(3-hydroxyphenyl)-N-n-propyl-piperidine ((-)-3-PPP).},
doi = {10.1016/0024-3205(91)90552-M},
url = {https://www.osti.gov/biblio/5945968}, journal = {Life Sciences; (USA)},
issn = {0024-3205},
number = ,
volume = 48:4,
place = {United States},
year = {Tue Jan 01 00:00:00 EST 1991},
month = {Tue Jan 01 00:00:00 EST 1991}
}