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












  • Intracellular calcium in NCB-20 cells: elevation by depolarization and ethanol but not by glutamate.

    abstract::Intracellular Ca2+, measured in NCB-20 cells with the fluorescent indicator fura-2, was elevated by K(+)-depolarization and by ethanol, but not by the excitatory amino acids L-glutamate and N-methyl-D-aspartate. These amino acids failed to raise intracellular Ca2+ levels even in the presence of elevated extracellular ...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Chan J,Greenberg DA

    更新日期:1991-01-25 00:00:00

  • A subpopulation of displaced ganglion cells of the pigeon retina exhibits substance P-like immunoreactivity.

    abstract::Immunohistochemical and retrograde tracing techniques were combined to demonstrate the occurrence of displaced ganglion cells (DGCs) exhibiting substance P-like immunoreactivity (SP-LI) in the pigeon retina. Following injections of rhodamine-labeled latex microspheres into the nucleus of the basal optic root (accessor...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Britto LR,Hamassaki DE

    更新日期:1991-04-12 00:00:00

  • Possible involvement of neuropeptide Y in the seasonal control of hydroxyindole-O-methyltransferase activity in the pineal gland of the european hamster (Cricetus cricetus).

    abstract::Hydroxyindole-O-methyltransferase (HIOMT) catalyses the last step of all the 5-methoxyindoles synthesized in the pineal gland. The synthetic activity of this neuroendocrine structure is driven not only by noradrenaline but also by various neuropeptides. Recently we have established (1) that one of these neuropeptides,...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Ribelayga C,Pévet P,Simonneaux V

    更新日期:1998-08-10 00:00:00

  • Augmentation of short-term plasticity in CA1 of rat hippocampus after chronic ethanol treatment.

    abstract::The neurotoxic effects of chronic ethanol exposure were investigated in rat hippocampus by electrophysiological analysis of the Schaffer collateral-commissural input to stratum radiatum of CA1. Experimental animals were fed an ethanol-containing liquid diet for 20 weeks but were withdrawn from the special diet at leas...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Abraham WC,Hunter BE,Zornetzer SF,Walker DW

    更新日期:1981-09-28 00:00:00

  • Functional neuroanatomy of visual search with differential attentional demands: an fMRI study.

    abstract::Visual search is characterized as efficient (RT independent of distractor number) or inefficient (RT increasing with distractor number). Our goal was to determine if any brain regions are differentially activated by the attentional demands of these two search modes. We used fMRI to examine activation patterns during s...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Kim KK,Eliassen JC,Lee SK,Kang E

    更新日期:2012-09-26 00:00:00

  • Phosphodiesterase 4B (PDE4B) and cAMP-level regulation within different tissue fractions of rat hippocampal slices during long-term potentiation in vitro.

    abstract::Molecular events associated with mnemonic processes and neuronal plasticity are postulated to result in functional changes in synaptic structure. One possible site is the post-synaptic density, where activity-dependent changes modulate signal transduction cascades. In this report, we detail spatial-temporal changes fo...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Ahmed T,Frey JU

    更新日期:2005-04-18 00:00:00

  • Angiotensin AT1 receptors in the preoptic area negatively modulate the cardiovascular and ACTH responses induced in rats by intrapreoptic injection of prostaglandin E2.

    abstract::We previously reported that brain angiotensin II type 2 (AT2) receptors contribute to the hyperthermia induced by intrahypothalamic (intrapreoptic (i.p.o.)) administration of prostaglandin E2 (PGE2) in rats. The present study was carried out to investigate the role of angiotensin II (ANG II) receptors in the cardiovas...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Watanabe T,Sakata Y,Wada M

    更新日期:2000-01-03 00:00:00

  • Release of amino acids from the maturing cobalt-induced epileptic focus.

    abstract::A study was made of the release of excitatory, inhibitory and other amino acids from epileptic foci induced in the sensorimotor cortex of rats by cobalt implantation. A new in vivo superfusion method was employed which gives free movement to the animals and allows study over periods of days and weeks. Most amino acids...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Dodd PR,Bradford HF

    更新日期:1976-07-30 00:00:00

  • Cerebrospinal fluid (CSF) and brain monoamine metabolites in the developing rat pup.

    abstract::Concentrations of the neurotransmitters, serotonin (5-HT), dopamine (DA), and norepinephrine (NE) were measured in the developing rat brain at 12, 19, 26 and 42 days of age. The amino acid precursors, tryptophan (TRP) and tyrosine (TYR) were measured along with the 5-HT and DA metabolites, 5-hydroxyindoleacetic acid (...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Shaywitz BA,Anderson GM,Cohen DJ

    更新日期:1985-01-01 00:00:00

  • Involvement of M1 muscarinic receptors in the initiation of cholinergically induced epileptic seizures in the rat brain.

    abstract::The present study was designed to determine the types of acetylcholine receptors involved in the initiation of epileptic seizures from the zona incerta and surrounding structures by cholinergic stimulation in rats. Unilateral intracerebral microinjection of the mixed muscarinic and nicotinic agonist carbachol (3 micro...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Cruickshank JW,Brudzynski SM,McLachlan RS

    更新日期:1994-04-18 00:00:00

  • Release of serotonin from perikarya in cat nodose ganglia.

    abstract::Newly synthesized serotonin (5-HT) can be released in the nodose ganglion from the nerve cell bodies of vago-aortic serotoninergic neurones. Free-calcium led to a decrease of spontaneous and potassium-evoked release. The veratridine-stimulating response was abolished by TTX. The concept that 5-HT released from perikar...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Fueri C,Faudon M,Hery M,Hery F

    更新日期:1984-06-18 00:00:00

  • Cognitive inflexibility after archicortical and paleocortical prefrontal lesions in marmosets.

    abstract::The behaviour and cognitive abilities of marmosets with bilateral ablations of either the archicortex on the mediodorsal surface or the paleocortex on the ventrolateral surface of the frontal lobes were assessed in terms of the types of information being handled, the mode of action (inhibitory versus productive mechan...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Ridley RM,Durnford LJ,Baker JA,Baker HF

    更新日期:1993-11-19 00:00:00

  • Thyrotropin-releasing hormone (TRH) improves survival in anaphylactic shock: a central effect mediated by the sympatho-adrenomedullary beta-adrenoceptive system.

    abstract::Treatment with thyrotropin-releasing hormone (TRH) significantly improved survival following induction of fatal systemic anaphylaxis in mice. The protective effect was mediated centrally since survival was increased by intracerebroventricular (i.c.v.) administration of TRH at doses which had no effect when given syste...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Amir S,Harel M,Schachar A

    更新日期:1984-04-30 00:00:00

  • Alterations in the cortical thickness and the amplitude of low-frequency fluctuation in patients with post-traumatic stress disorder.

    abstract::The core neuropsychological processes underlying post-traumatic stress disorder (PTSD) have yet to be elucidated, and the association between anatomical and functional deficits in PTSD remains largely unknown. The aim of our study was to investigate the alterations in cortical thickness and amplitude of low-frequency ...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Bing X,Ming-Guo Q,Ye Z,Jing-Na Z,Min L,Han C,Yu Z,Jia-Jia Z,Jian W,Wei C,Han-Jian D,Shao-Xiang Z

    更新日期:2013-01-15 00:00:00

  • Dopamine receptors regulate Met-enkephalin content in pituitary.

    abstract::Met-enkephalin-like immunoreactive material (ME-LI) in the neurointermediate lobe of rat pituitary was dramatically altered by the long-term administration of drugs altering dopamine receptor activity. Treatment with the dopamine receptor antagonist haloperidol resulted in significant increases of ME-LI and treatment ...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: George SR,Kertesz M

    更新日期:1985-05-13 00:00:00

  • Isolation of pseudoperoxidase-positive astrocyte granules from intact rat brain and cysteamine-treated neuroglial cultures.

    abstract::A subpopulation of astrocytes in periventricular regions of aging brain and in cysteamine (CSH)-treated glial cultures contain autofluorescent cytoplasmic granules that exhibit an affinity for Gomori's chrome alum hematoxylin (CAH), and non-enzymatic peroxidase activity. Although shown to be histochemically distinct f...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Cissé S,Schipper HM

    更新日期:1993-06-25 00:00:00

  • Dissociable neural systems for moral judgment of anti- and pro-social lying.

    abstract::Pro-social lying, which serves to benefit listeners, is considered more socially and morally acceptable than anti-social lying, which serves to harm listeners. However, it is still unclear whether the neural mechanisms underlying the moral judgment of pro-social lying differ from those underlying the moral judgment of...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Hayashi A,Abe N,Fujii T,Ito A,Ueno A,Koseki Y,Mugikura S,Takahashi S,Mori E

    更新日期:2014-03-27 00:00:00

  • Prefrontal representation of stimulus attributes during delay tasks. I. Unit activity in cross-temporal integration of sensory and sensory-motor information.

    abstract::The activity of 294 single units was recorded from the dorsolateral prefrontal cortex of monkeys performing two visual discrimination tasks with delayed response. One task, delayed matching-to-sample (DMS), required memory of a colored cue for later (18 s) matching and choice of color; the cue did not connote the loca...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Quintana J,Yajeya J,Fuster JM

    更新日期:1988-12-06 00:00:00

  • A [14C]2-deoxyglucose analysis of the functional neural pathways of the limbic forebrain in the rat. IV. A pathway from the prefrontal cortical-medial thalamic system to the hypothalamus.

    abstract::The present study utilized the [14C]2-deoxyglucose (2-DG) cell labeling procedure to characterize a functional pathway from the prefrontal cortex (Pfc) and mediodorsal thalamic nucleus (MD) to the hypothalamus. Rats were injected with 2-DG prior to a 45 min experimental paradigm consisting of alternating 30 s on-off p...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Brutus M,Watson RE Jr,Shaikh MB,Siegel HE,Weiner S,Siegel A

    更新日期:1984-09-24 00:00:00

  • Age-related increase in oxidized proteins in mouse synaptic mitochondria.

    abstract::Since it has been proposed that oxidized protein accumulation plays a critical role in brain aging, we have investigated their contents in synaptic mitochondria from five age groups of mice. Protein carbonyl content in synaptic mitochondria showed a significant positive correlation with age (r = 0.95, P = 0.01). A lin...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Martinez M,Hernández AI,Martínez N,Ferrándiz ML

    更新日期:1996-08-26 00:00:00

  • Regional effects of hypothyroidism on 5'-nucleotidase and cyclic nucleotide phosphohydrolase activities in developing rat brain.

    abstract::The activities of 5'-nucleotidase (EC and of 2',3'-cyclic nucleotide 3'-phosphohydrolase (CNP) (EC were measured in crude membrane preparations from 6 brain regions of hypothyroid rats 31 days and 42 days after conception (8-9 days and 19-20 days after birth respectively) and from normal rats 31, 36...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: King RA,Smith RM,Dreosti IE

    更新日期:1983-04-01 00:00:00

  • Differential ultrastructural distribution of synapsin and synaptophysin proximal to a ligation in bovine splenic nerve.

    abstract::Synaptophysin and synapsin, closely correlated on synaptic vesicles in terminals, may show a differential distribution at synapse formation and maturation. In order to disclose the fine structural details of these differences, synapsin and synaptophysin distribution was studied by immunocytochemistry on ligated bovine...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Quatacker J,Partoens P,De Potter W

    更新日期:1998-08-17 00:00:00

  • Kv1.2-immunoreactive primary sensory neurons in the rat trigeminal ganglion.

    abstract::Immunohistochemistry for Kv1.2, a subunit of voltage-gated K(+) channels, was performed on the trigeminal ganglion (TG). Immunoreactivity (ir) was detected in half (48%) the TG neurons. These neurons were mostly medium-sized to large (range 137.6-2664.8 microm(2), mean+/-S.D. 892.6+/-413.3 microm(2)). A double immunof...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Ichikawa H,Sugimoto T

    更新日期:2003-06-06 00:00:00

  • Electromyographic and neuromuscular force patterns associated with unexpectedly loaded rapid limb movements.

    abstract::A series of ballistic, unidirectional arm movements were studied to evaluate the electromyographic (EMG) and neuromuscular force patterns that occur when a limb is unexpectedly perturbed. Multiple training trials were continued with a control load spring attached to the apparatus until a pre-specified criterion for le...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Richardson C,Simmons RW

    更新日期:1985-09-23 00:00:00

  • Changes in proteolytic enzymes and proteins during maturation of the brain.

    abstract::(1) Changes during development in the levels of proteinases and peptidases were measured in brain homogenates. At all ages di- and tripeptidase levels were 7-15-fold higher than proteinase activity. (2) Cathepsin A and D and neutral proteinase activity first decreased (during the 5 days before birth) and then increase...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Marks N,Stern F,Lajtha A

    更新日期:1975-03-21 00:00:00

  • Towards a neuroprotective gene therapy for Parkinson's disease: use of adenovirus, AAV and lentivirus vectors for gene transfer of GDNF to the nigrostriatal system in the rat Parkinson model.

    abstract::During the last few years, recombinant viral vectors derived from adenovirus (Ad), adeno-associated virus (AAV) or lentivirus (LV) have been developed into highly effective vehicles for gene transfer to the adult central nervous system. In recent experiments, in the rat model of Parkinson's disease, all three vector s...

    journal_title:Brain research

    pub_type: 杂志文章,评审


    authors: Björklund A,Kirik D,Rosenblad C,Georgievska B,Lundberg C,Mandel RJ

    更新日期:2000-12-15 00:00:00

  • Dopaminergic amacrine cells in the retina of Japanese dace.

    abstract::The morphological and physiological identification of the cells in the inner retina of Japanese dace was made by means of intracellular single cell recording and dye injection techniques. Our flat mounts and physiological classification revealed that 97 out of 102 sample cells were amacrine cells except for 3 transien...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Chino YM,Hashimoto Y

    更新日期:1986-05-07 00:00:00

  • Loss of active avoidance of responding after lateral hypothalamic injections of 6-hydroxydopamine.

    abstract::After injections of 6-hydroxydopamine (6-OHDA) along the medial forebrain bundle in the lateral hypothalamus, rats failed to acquire a one-way active avoidance response or failed to perform a previously acquired active avoidance response. Such rats, however, acquired a passive avoidance response and a conditioned tast...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Smith GP,Levin BE,Ervin GN

    更新日期:1975-05-09 00:00:00

  • The human lateral tuberal nucleus: Immunohistochemical characterization and analogy to the rodent PV1-nucleus.

    abstract::The lateral tuberal nucleus (LTN) is a hypothalamic region that has been identified with certainty only in humans and primates. It is composed of three small round globular units which protrude the basal surface of the brain along the optic tract. The function of the LTN is unknown. Recently, a tiny, parvalbumin-posit...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Gerig AT,Celio MR

    更新日期:2007-03-30 00:00:00

  • Preservation of autoregulatory cerebral vasodilator responses to hypotension after inhibition of nitric oxide synthesis.

    abstract::Effects of inhibition of nitric oxide (NO) synthesis on the cerebrovascular autoregulatory vasodilator response to hypotension were studied in conscious rats. Cerebral blood flow (CBF) was determined with [14C]iodoantipyrine in a saline-treated control group and in three groups following inhibition of NO synthase acti...

    journal_title:Brain research

    pub_type: 杂志文章


    authors: Takahashi S,Cook M,Jehle J,Kennedy C,Sokoloff L

    更新日期:1995-04-24 00:00:00