Regional differences in μ1-binding of [(3)H][d-Ala(2),d-Leu(5)]-enkephalin: Comparisons of thalamus and cortex in the rat Journal Article


Authors: Goodman, R. R.; Adler, B. A.; Pasternak, G. W.
Article Title: Regional differences in μ1-binding of [(3)H][d-Ala(2),d-Leu(5)]-enkephalin: Comparisons of thalamus and cortex in the rat
Abstract: Typically, μ1-sites represent approximately 25-35% of binding in rat brain homogenates. Competition studies indicated that approximately 60% of [3H][d-Ala2,d-Leu5]-enkephalin ([3H]DADLE) binding in the thalamus was inhibited by low concentrations of morphine (2-5 nM). This high proportion of μ1-binding was anticipated based upon the low levels of δ-sites and the high levels of μ1-sites in this region observed in autoradiography studies. In contrast, morphine lowered [3H]DADLE binding by only approximately 5-15% in the cortex, a region known to possess large amounts of δ- and few μ1-receptors. These results support previous autoradiography studies and illustrate the advantages of using tissue regions in the characterization of opiate receptor subtypes. © 1985.
Keywords: dose response; nonhuman; comparative study; animal cell; animal; brain cortex; central nervous system; drug receptor binding; drug antagonism; brain; drug response; rat; rats; radioisotope; morphine; frontal lobe; drug sensitivity; mu opiate receptor; receptors, opioid, mu; pharmacokinetics; naloxone; opiate receptor; receptors, opioid, delta; thalamus; enkephalin; naloxonazine; drug comparison; topical drug administration; receptors, opioid; priority journal; enkephalin, leucine-2-alanine; support, u.s. gov't, p.h.s.; enkephalin, leucine; enkephalin[2 alanine 5 leucine] h 3; μ1-receptor; enkephalin h 3; naloxazine
Journal Title: Neuroscience Letters
Volume: 59
Issue: 2
ISSN: 0304-3940
Publisher: Elsevier Science, Inc.  
Date Published: 1985-08-30
Start Page: 155
End Page: 158
Language: English
DOI: 10.1016/0304-3940(85)90192-2
PUBMED: 2997666
PROVIDER: scopus
DOI/URL:
Notes: Article -- Export Date: 26 October 2021 -- Source: Scopus
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  1. Gavril W Pasternak
    414 Pasternak