Membrane-delimited proteolytic regulation of opioid receptors.


:Prolonged exposure of opioid receptors to agonists leads to their regulation by the classical process of clathrin-dependent internalization, followed by their intracellular degradation (down regulation). We have previously shown that the opioid agonist etorphine induced an additional process of down regulation of mu-opioid receptors (MOR) that occurred in intact MOR-transfected HEK-293 cells, as well as in isolated membranes. In the present study we show that etorphine similarly down regulated rat kappa-opioid receptors (KORs), which do not undergo the classical process of internalization and down regulation. This process was resistant to inhibitors of clathrin-coated pit formation (hypertonic sucrose, mono-dansyl-cadaverine) and was mainly mediated by membranous serine- and amino-peptidases. We further show that various opioid ligands, besides etorphine, induced down regulation of either KOR or MOR in isolated membranes. The ability of the various opioid ligands to induce membrane-delimited KOR or MOR down regulation did not correlate to their classical pharmacological profile, suggesting functional selectivity of the effect. Levorphanol, but not its stereoisomer dextrophan, induced membrane-delimited down regulation of both KOR and MOR, indicating that stereoselective binding to the receptor was necessary to initiate the process. Our findings that this proteolytic regulation of opioid receptors occurs not only in isolated membranes but also in intact cells and that it occurs even when the receptors are resistant to the conventional process of down regulation indicate its possible physiological role in the regulation of opioid activity.


Brain Res


Brain research


Kaplan E,Binyaminy B,Gafni M,Keren O,Sarne Y




Has Abstract


2011-04-22 00:00:00












  • Gap-like junctions between neuron cell bodies and glial cells of crayfish.

    abstract::Data reported up to now on neuron-glia relationships, show that neuron cell bodies and glial cells are separated by a narrow intercellular cleft which is considered as the microenvironment of the nervous system, and where neuron-glia exchange occurs. We present here evidence that neuron perikarya and ensheathing glial...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Cuadras J,Martin G,Czternasty G,Bruner J

    更新日期:1985-02-04 00:00:00

  • Dopaminergic sprouting in the rat striatum after partial lesion of the substantia nigra.

    abstract::The capacity of the dopaminergic nerve system to reinnervate the denervated adult striatum was analyzed in a model of partial 6-hydroxydopamine-induced unilateral lesion of rat substantia nigra pars compacta. Sprouting of dopaminergic fibers entering the ventrolateral part of the striatum from a narrow zone of the ext...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Blanchard V,Anglade P,Dziewczapolski G,Savasta M,Agid Y,Raisman-Vozari R

    更新日期:1996-02-19 00:00:00

  • Regeneration of descending projections in Xenopus laevis tadpole spinal cord demonstrated by retrograde double labeling.

    abstract::Xenopus laevis tadpoles functionally recover from spinal cord transection. Because this recovery requires the tadpole to metamorphose, it may result from compensatory changes initiated by de novo growth of axons involved in limb dominant locomotion rather than from regeneration of cut axons. To determine whether axona...

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    pub_type: 杂志文章


    authors: Gibbs KM,Szaro BG

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    abstract::Rapid progress in our understanding of macrostructural abnormalities in autism spectrum disorders (ASD) has occurred in recent years. However, the relationship between the integrity of neural tissue and neural function has not been previously investigated. Single-voxel proton magnetic resonance spectroscopy and functi...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Kleinhans NM,Schweinsburg BC,Cohen DN,Müller RA,Courchesne E

    更新日期:2007-08-08 00:00:00

  • Contribution of nucleus medianus to the drinking and pressor responses to angiotensin II acting at subfornical organ.

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    pub_type: 杂志文章


    authors: Gutman MB,Jones DL,Ciriello J

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    abstract::Early adverse events have been shown to increase the incidence of interstitial cystitis/painful bladder syndrome in adulthood. Despite high clinical relevance and reports of stress-related symptom exacerbation, animal models investigating the contribution of early life stress to female urological pain are lacking. We ...

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    authors: Pierce AN,Di Silvestro ER,Eller OC,Wang R,Ryals JM,Christianson JA

    更新日期:2016-05-15 00:00:00

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    abstract::The distribution of degeneration in the vestibular nuclei (VN) has been studied in transversely cut sections from 9 cats with stereotaxically performed lesions in the main reticular formation (RF) of the brain stem (Nauta of Fink and Heimer method). No projection was found from the mesencephalic reticular formation (R...

    journal_title:Brain research

    pub_type: 杂志文章


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    更新日期:1975-09-05 00:00:00

  • Distribution of the ganglioside GD3 in the human nervous system detected by R24 mouse monoclonal antibody.

    abstract::Immunohistochemical staining with mouse monoclonal antibody R24 recognizing the ganglioside GD3 was used to study the distribution of GD3 in the human brain. Positive staining was primarily found in the surrounding neuropil of many neuronal groups in the brainstem and spinal cord, cerebellum, retina and dentate gyrus ...

    journal_title:Brain research

    pub_type: 杂志文章


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    更新日期:1984-12-17 00:00:00

  • Neurotensin and neuromedin N brain levels after fornix transection: evidence for an efficient neurotensin precursor processing in subicular neurons.

    abstract::High levels of neurotensin/neuromedin N precursor mRNA, but few if any NT-positive perikarya have been detected in the dorsal subiculum of the adult rat or human hippocampus. This apparent discrepancy was tentatively ascribed to a lack of precursor mRNA translation or to a poor precursor posttranslational processing i...

    journal_title:Brain research

    pub_type: 杂志文章


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    更新日期:1995-12-08 00:00:00

  • Possible involvement of brain somatostatin in the memory formation of rats and the cognitive enhancing action of FR121196 in passive avoidance task.

    abstract::Using the passive avoidance learning task in rats, the role of brain somatostatin in cognitive function was investigated with special reference to that of the brain cholinergic system. In addition, the involvement of both the brain somatostatinergic and cholinergic systems in the anti-amnesic action of a newly introdu...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Matsuoka N,Maeda N,Yamaguchi I,Satoh M

    更新日期:1994-04-11 00:00:00

  • Thalamo-striatal projections in the hedgehog tenrec.

    abstract::Unlike the basal ganglia input from the midline and intralaminar nuclei, the origin and prominence of striatal projections arising in the lateral thalamus varies considerably among mammals being most restricted in the opossum and monkey, most extensive in the rat. To get further insight into the evolution of thalamo-s...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Künzle H

    更新日期:2006-07-19 00:00:00

  • Calorie restriction attenuates astrogliosis but not amyloid plaque load in aged rhesus macaques: a preliminary quantitative imaging study.

    abstract::While moderate calorie restriction (CR) in the absence of malnutrition has been consistently shown to have a systemic, beneficial effect against aging in several animals models, its effect on the brain microstructure in a non-human primate model remains to be studied using post-mortem histopathologic techniques. In th...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Sridharan A,Pehar M,Salamat MS,Pugh TD,Bendlin BB,Willette AA,Anderson RM,Kemnitz JW,Colman RJ,Weindruch RH,Puglielli L,Johnson SC

    更新日期:2013-05-01 00:00:00

  • Differential and persistent expression patterns of CNS gene transfer by an adeno-associated virus (AAV) vector.

    abstract::Safe, long-term gene expression is a primary criteria for effective gene therapy in the brain, so studies were initiated to evaluate adeno-associated virus (AAV) vector transfer of a reporter gene into specific sites of the rat brain. In the 4 day old rat, site infusions of AAV-CMV-lacZ (1 microliter; 5 x 10(4) partic...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: McCown TJ,Xiao X,Li J,Breese GR,Samulski RJ

    更新日期:1996-03-25 00:00:00

  • Different stimulatory opioid effects on intracellular Ca(2+) in SH-SY5Y cells.

    abstract::Present study revealed the stimulatory effects of delta opioid receptor on intracellular Ca(2+) concentration ([Ca(2+)](i)) in SH-SY5Y cells. Fura-2 based single cell fluorescence ratio (F345/F380) was used to monitor the fluctuation of [Ca(2+)](i). Application of the selective delta-opioid receptor agonist alone, [D-...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Chen L,Zou S,Lou X,Kang HG

    更新日期:2000-11-03 00:00:00

  • In vivo test for myelinotoxicity of cerebrospinal fluid.

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    authors: Tabira T,Webster HD,Wray SH

    更新日期:1977-01-14 00:00:00

  • Tetrodotoxin-sensitive and -resistant Na+ channel currents in subsets of small sensory neurons of rats.

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    journal_title:Brain research

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  • Population coding in spike trains of simultaneously recorded retinal ganglion cells.

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    pub_type: 杂志文章


    authors: Fernández E,Ferrandez J,Ammermüller J,Normann RA

    更新日期:2000-12-22 00:00:00

  • Acidic pH promotes the formation of toxic fibrils from beta-amyloid peptide.

    abstract::Beta-amyloid (Abeta) peptides, the major component of senile plaques in brains of patients with Alzheimer's disease (AD), were found in the low pH organelles (i.e. endosome/lysosome) of cultured neuronal cells. Since acidic pH values have been shown to promote the self-assembly of Abetas, which seems to be a prerequis...

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    authors: Su Y,Chang PT

    更新日期:2001-03-02 00:00:00

  • Disrupted pro- and antioxidative balance as a mechanism of neurotoxicity induced by perinatal exposure to lead.

    abstract::The aim of this paper was to examine if pre- and neonatal exposure that results in lead (Pb) concentration below 'safe level' (10 μg/dL) in offspring blood may cause disruption of the pro/antioxidant balance in the developing rat brain. We studied oxidative stress intensity (malondialdehyde (MDA) concentration) as wel...

    journal_title:Brain research

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    authors: Baranowska-Bosiacka I,Gutowska I,Marchlewicz M,Marchetti C,Kurzawski M,Dziedziejko V,Kolasa A,Olszewska M,Rybicka M,Safranow K,Nowacki P,Wiszniewska B,Chlubek D

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  • Effects of kainic acid lesions in rat ventral lateral geniculate nucleus upon field potentials of the superior colliculus: correlation between morphological and physiological observations.

    abstract::Morphological and physiological effects of kainic acid (KA) lesions in rat ventral lateral geniculate nucleus (LGV) were studied 1.5 and 6 h after KA injection. Morphological changes were examined mainly by electron micrographs. At 1.5 h after KA injection dendrites were dilated and some vacuolations occurred in both ...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Nagata T,Tsukamoto Y,Matsuno K,Hayashi Y

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  • Nanoparticles, a drug carrier system to pass the blood-brain barrier, permit central analgesic effects of i.v. dalargin injections.

    abstract::The Leu-enkephalin dalargin does not normally penetrate the blood brain barrier when given intravenously. Drug targeting to the brain was investigated by using poly(butylcyanoacrylate) nanoparticles which were coated with polysorbate 80. When injected intravenously in mice, dalargin-loaded nanoparticles coated with th...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Schröder U,Sabel BA

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  • Central alpha-adrenergic receptors and corticotropin releasing factor mediate hemodynamic responses to acute cold stress.

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    journal_title:Brain research

    pub_type: 杂志文章


    authors: Tan Y,Gan Q,Knuepfer MM

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    journal_title:Brain research

    pub_type: 杂志文章


    authors: Mandelbrod I,Feldman S,Werman R

    更新日期:1983-08-01 00:00:00

  • Antidiabetic sulfonylureas: localization of binding sites in the brain and effects on the hyperpolarization induced by anoxia in hippocampal slices.

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    journal_title:Brain research

    pub_type: 杂志文章


    authors: Mourre C,Ben Ari Y,Bernardi H,Fosset M,Lazdunski M

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    journal_title:Brain research

    pub_type: 杂志文章


    authors: Schaechter JD,Wurtman RJ

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  • Encoding of visual-spatial information in working memory requires more cerebral efforts than retrieval: Evidence from an EEG and virtual reality study.

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    journal_title:Brain research

    pub_type: 杂志文章


    authors: Jaiswal N,Ray W,Slobounov S

    更新日期:2010-08-06 00:00:00

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    journal_title:Brain research

    pub_type: 杂志文章


    authors: Yang CC,Jou IM

    更新日期:2016-03-01 00:00:00

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    journal_title:Brain research

    pub_type: 杂志文章


    authors: Xu H,Smolens I,Gintzler AR

    更新日期:1989-12-11 00:00:00

  • Central glucagon like peptide-1 inhibits reflex swallowing elicited by the superior laryngeal nerve via caudal brainstem in the rat.

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    pub_type: 杂志文章


    authors: Kobashi M,Mizutani S,Fujita M,Mitoh Y,Shimatani Y,Matsuo R

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    journal_title:Brain research

    pub_type: 杂志文章


    authors: Katayama Y,Kiyama H,Arai Y,Tohyama M

    更新日期:1984-09-17 00:00:00