Document Detail

High-affinity [3H]6-nitroquipazine binding sites in rat brain.
MedLine Citation:
PMID:  1694774     Owner:  NLM     Status:  MEDLINE    
6-Nitroquipazine is a very potent and selective inhibitor of neuronal 5-hydroxytryptamine (5-HT; serotonin) uptake. We have characterized the specific binding of [3H]6-nitroquipazine to rat brain membranes at 22 degrees C. The present results indicate the presence of a single saturable high-affinity binding component for [3H]6-nitroquipazine. Scatchard analysis revealed an apparent equilibrium dissociation constant (Kd) of 93.0 +/- 2.23 pM, and a maximal number of binding sites (Bmax) of 831.7 +/- 18.7 fmol/mg protein (mean +/- S.D., n = 4). The kinetically derived dissociation constant was 74.5 pM. [3H]6-Nitroquipazine binding was inhibited selectively by 5-HT uptake inhibitors, and a good correlation was demonstrated between the potency of various drugs to inhibit [3H]6-nitroquipazine binding and [3H]5-HT uptake. The highest densities of [3H]6-nitroquipazine binding were obtained in the hypothalamus and midbrain, intermediate binding was observed in the striatum, hippocampus, medulla oblongata and cortex, and the lowest binding was observed in the cerebellum. Lesioning of 5-HT neurons with p-chloroamphetamine resulted in a 72% reduction in [3H]6-nitroquipazine binding compared to controls. These results indicate that the binding site specifically labelled by [3H]6-nitroquipazine is associated with the neuronal 5-HT transporter complex. [3H]6-Nitroquipazine is an excellent radioligand for the study of the 5-HT uptake system.
K Hashimoto; T Goromaru
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmacology     Volume:  180     ISSN:  0014-2999     ISO Abbreviation:  Eur. J. Pharmacol.     Publication Date:  1990 May 
Date Detail:
Created Date:  1990-08-13     Completed Date:  1990-08-13     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  1254354     Medline TA:  Eur J Pharmacol     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  273-81     Citation Subset:  IM    
Department of Radiopharmaceutical Chemistry, Faculty of Pharmacy, University of Fukuyama, Japan.
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MeSH Terms
Binding Sites
Binding, Competitive / drug effects
Brain Chemistry / drug effects*
Hydroxyindoleacetic Acid / metabolism
Membranes / drug effects,  metabolism
Nerve Endings / drug effects,  metabolism
Quipazine / analogs & derivatives*,  metabolism,  pharmacokinetics
Rats, Inbred Strains
Serotonin / metabolism
Serotonin Antagonists / metabolism*
p-Chloroamphetamine / pharmacology
Reg. No./Substance:
0/Quinolines; 0/Serotonin Antagonists; 4774-24-7/Quipazine; 50-67-9/Serotonin; 54-16-0/Hydroxyindoleacetic Acid; 64-12-0/p-Chloroamphetamine; 77372-73-7/6-nitroquipazine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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