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Title: Differential effect of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on (/sup 3/H)SCH23390 and (/sup numberH/)forskolin binding in rat striatum

Abstract

The binding of (/sup 3/H)forskolin to a homogeneous population of binding sites in rat striatum was enhanced by NaF, guanine nucleotides and MgCl/sub 2/. These effects of NaF and guanylylimidodiphosphate (Gpp(NH)p) were synergistic with MgCl/sub 2/, but NaF and Gpp(NH)p together elicited no greater enhancement of (/sup 3/H)forskolin binding. These data suggest that (/sup 3/H)forskolin may label a site which is modulated by the guanine nucleotide regulatory subunit which mediates the stimulation of adenylate cyclase (N/sub S/). The D/sub 1/ dopamine receptor is known to stimulate adenylate cyclase via N/sub S/. In rat striatum, the B/sub max/ of (/sup 3/H)forskolin binding sites in the presence of MgCl/sub 2/ and NaF was approximately two fold greater than the B/sub max/ of (/sup 3/H)SCH23390-labeled D/sub 1/ dopamine receptors. Incubation of striatal homogenates with the protein modifying reagent EEDQ elicited a concentration-dependent decrease in the binding of both (/sup 3/H)SCH23390 and (/sup 3/H)forskolin, although EEDQ was approximately 14 fold more potent at inactivating the D/sub 1/ dopamine receptor. Following in vivo administration of EEDQ there was no significant effect on (/sup 3/H)forskolin binding sites using a dose of EEDQ that irreversibly inactivated greater than 90% of D/sub 1/ dopamine receptors. These data suggestmore » that EEDQ is a suitable tool for investigating changes in the stoichiometry of receptors and their second messenger systems.« less

Authors:
; ;
Publication Date:
Research Org.:
Univ. of Cincinnati College of Medicine, OH (USA)
OSTI Identifier:
5990893
Resource Type:
Journal Article
Journal Name:
Life Sci.; (United States)
Additional Journal Information:
Journal Volume: 44:13
Country of Publication:
United States
Language:
English
Subject:
59 BASIC BIOLOGICAL SCIENCES; DOPAMINE; RECEPTORS; PHOSPHOLIPIDS; BIOCHEMICAL REACTION KINETICS; QUINOLINES; BIOLOGICAL EFFECTS; BRAIN; CYCLASES; RATS; REAGENTS; STOICHIOMETRY; TRACER TECHNIQUES; TRITIUM COMPOUNDS; AMINES; ANIMALS; AROMATICS; AUTONOMIC NERVOUS SYSTEM AGENTS; AZAARENES; AZINES; BODY; CARDIOTONICS; CARDIOVASCULAR AGENTS; CENTRAL NERVOUS SYSTEM; DRUGS; ENZYMES; ESTERS; HETEROCYCLIC COMPOUNDS; HYDROXY COMPOUNDS; ISOTOPE APPLICATIONS; KINETICS; LABELLED COMPOUNDS; LIPIDS; LYASES; MAMMALS; MEMBRANE PROTEINS; NERVOUS SYSTEM; NEUROREGULATORS; ORGANIC COMPOUNDS; ORGANIC NITROGEN COMPOUNDS; ORGANIC PHOSPHORUS COMPOUNDS; ORGANS; PHENOLS; POLYPHENOLS; PROTEINS; PYRIDINES; REACTION KINETICS; RODENTS; SYMPATHOMIMETICS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

Citation Formats

Norman, A B, Wachendorf, T J, and Sanberg, P R. Differential effect of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on (/sup 3/H)SCH23390 and (/sup numberH/)forskolin binding in rat striatum. United States: N. p., 1989. Web. doi:10.1016/0024-3205(89)90583-3.
Norman, A B, Wachendorf, T J, & Sanberg, P R. Differential effect of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on (/sup 3/H)SCH23390 and (/sup numberH/)forskolin binding in rat striatum. United States. https://doi.org/10.1016/0024-3205(89)90583-3
Norman, A B, Wachendorf, T J, and Sanberg, P R. 1989. "Differential effect of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on (/sup 3/H)SCH23390 and (/sup numberH/)forskolin binding in rat striatum". United States. https://doi.org/10.1016/0024-3205(89)90583-3.
@article{osti_5990893,
title = {Differential effect of N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ) on (/sup 3/H)SCH23390 and (/sup numberH/)forskolin binding in rat striatum},
author = {Norman, A B and Wachendorf, T J and Sanberg, P R},
abstractNote = {The binding of (/sup 3/H)forskolin to a homogeneous population of binding sites in rat striatum was enhanced by NaF, guanine nucleotides and MgCl/sub 2/. These effects of NaF and guanylylimidodiphosphate (Gpp(NH)p) were synergistic with MgCl/sub 2/, but NaF and Gpp(NH)p together elicited no greater enhancement of (/sup 3/H)forskolin binding. These data suggest that (/sup 3/H)forskolin may label a site which is modulated by the guanine nucleotide regulatory subunit which mediates the stimulation of adenylate cyclase (N/sub S/). The D/sub 1/ dopamine receptor is known to stimulate adenylate cyclase via N/sub S/. In rat striatum, the B/sub max/ of (/sup 3/H)forskolin binding sites in the presence of MgCl/sub 2/ and NaF was approximately two fold greater than the B/sub max/ of (/sup 3/H)SCH23390-labeled D/sub 1/ dopamine receptors. Incubation of striatal homogenates with the protein modifying reagent EEDQ elicited a concentration-dependent decrease in the binding of both (/sup 3/H)SCH23390 and (/sup 3/H)forskolin, although EEDQ was approximately 14 fold more potent at inactivating the D/sub 1/ dopamine receptor. Following in vivo administration of EEDQ there was no significant effect on (/sup 3/H)forskolin binding sites using a dose of EEDQ that irreversibly inactivated greater than 90% of D/sub 1/ dopamine receptors. These data suggest that EEDQ is a suitable tool for investigating changes in the stoichiometry of receptors and their second messenger systems.},
doi = {10.1016/0024-3205(89)90583-3},
url = {https://www.osti.gov/biblio/5990893}, journal = {Life Sci.; (United States)},
number = ,
volume = 44:13,
place = {United States},
year = {Sun Jan 01 00:00:00 EST 1989},
month = {Sun Jan 01 00:00:00 EST 1989}
}