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Title Multiple opiate receptors in the brain of spontaneously hypertensive rats
Creator/Author Das, S. ; Bhargava, H.N.
Publication Date1986 Mar 01
OSTI IdentifierOSTI ID: 5383631
Report Number(s)CONF-8604222-
Other Number(s)Journal ID: CODEN: FEPRA
Resource TypeConference
Specific TypeJournal Article
Resource RelationJournal Name: Fed. Proc., Fed. Am. Soc. Exp. Biol.; (United States); Journal Volume: 45:3; Conference: 70. annual meeting of the Federation of American Society for Experimental Biology, St. Louis, MO, USA, 13 Apr 1986
Research OrgUniv. of Illinois, Chicago
Subject59 BASIC BIOLOGICAL SCIENCES; CENTRAL NERVOUS SYSTEM DEPRESSANTS; RECEPTORS; HYPERTENSION; PATHOGENESIS; BIOCHEMICAL REACTION KINETICS; BRAIN; LIGANDS; RATS; TRACER TECHNIQUES; TRITIUM COMPOUNDS; ANIMALS; BODY; CARDIOVASCULAR DISEASES; CENTRAL NERVOUS SYSTEM; DISEASES; DRUGS; ISOTOPE APPLICATIONS; KINETICS; LABELLED COMPOUNDS; MAMMALS; MEMBRANE PROTEINS; NERVOUS SYSTEM; ORGANIC COMPOUNDS; ORGANS; PROTEINS; REACTION KINETICS; RODENTS; SYMPTOMS; VASCULAR DISEASES; VERTEBRATES
Description/AbstractThe characteristics of ..mu.., delta and kappa -opiate receptors in the brain of spontaneously hypertensive (SH) and normotensive Wistar-Kyoto (WKY) rats were determined using the receptor binding assays. The ligands used were /sup 3/H-naltrexone (..mu..), /sup 3/H-ethylketocyclazocine (EKC, kappa) and /sup 3/H-Tyr-D-Ser-Gly-Phe-Leu-Thr (DSTLE, delta). Since EKC binds to ..mu.. and delta receptors in addition to kappa, the binding was done in the presence of 100 nM each of DAGO and DADLE to suppress ..mu.. and delta sites, respectively. All three ligands bound to brain membranes of WKY rats at a single high affinity site with the following B/sub max/ (fmol/mg protein) and K/sub d/ (nM) values: /sup 3/H-naltrexone (130.5; 0.43) /sup 3/H-EKC (19.8, 1.7) and /sup 3/H-DSTLE (139, 2.5). The binding of /sup 3/H-naltrexone and /sup 3/H-DSTLE in the brain of WKY and SH did not differ. A consistent increase (22%) in B/sub max/ of /sup 3/H-EKC was found in SHR compared to WKY rats. However, the K/sub d/ values did not differ. The increase in B/sub max/ was due to increases in hypothalamus and cortex. It is concluded that SH rats have higher density of kappa-opiate receptors, particularly in hypothalamus and cortex, compared to WKY rats, and that kappa-opiate receptors may be involved in the pathophysiology of hypertension.
Country of PublicationUnited States
LanguageEnglish
FormatMedium: X; Size: Pages: 188
System Entry Date2008 Feb 06

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