Title: Peripheral Benzodiazepine Receptor (PBR) New Insight in Cell Proliferation and Cell Differentiation Review. VOLUME: 3 ISSUE: 1. Author(s):Lorenzo Corsi, Elisa Geminiani and Mario Baraldi. Affiliation:Department of Biomedical Sciences, University of Modena and Reggio Emilia, 41100 Modena, Italy.. Keywords:Cell proliferation, tumour, PBR, translocator protein, cell survival, PK11195. Abstract: The peripheral benzodiazepine receptor (PBR), is an 18 kDa protein of the mammalian mitochondrial membrane and is a highly conserved protein among the mammalian. PBR is involved in numerous biological functions, including steroid biosynthesis, mitochondrial oxidative phosporylation and cell proliferation. The presence of PBR at the nuclear subcellular level has been demonstrated in aggressive breast cancer cell line and human glioma cells, where it seems to be involved in cell proliferation. In our previous studies we investigated the presence of nuclear PBR in different hepatic tumour cell lines with ...
In the present study, cerebellar granule cells were identified morphologically in primary culture and their characteristics were examined. The apparent affinity of the receptor for GABA increased during development in vitro (Fig. 1) and furosemide, an antagonist of the α6 subunit-containing GABAA receptor, inhibited GABA-induced currents more potently at 14 DIV than at 7 DIV (Fig. 2). These findings might be related to an increase in the amount of GABAA receptors containing the α6 subunit during granule cell maturation in vitro (Zheng et al., 1994).. The GABAA receptor system has long been hypothesized to be a target of ethanol action. Despite numerous studies conducted so far, the effects of alcohol on the GABAA receptor function remain controversial (Aguayo et al., 2002). A recent study has shown that low concentrations of ethanol enhance tonic inhibition mediated by the δ subunit-containing GABAA receptors in the hippocampal (Wei et al., 2004) and the cerebellar granule cells (Hanchar et ...
TY - JOUR. T1 - The peripheral benzodiazepine receptor modulates Ca2+ transport through the VDAC in rat heart mitochondria. AU - Tamse, C. T.. AU - Lu, X.. AU - Mortel, E. G.. AU - Cabrales, E.. AU - Feng, W.. AU - Schaefer, Saul. PY - 2008. Y1 - 2008. N2 - The voltage-dependent anion channel (VDAC) is a key mitochondrial protein involved in the transport of calcium. Its function is, in part, regulated by associated proteins such as the 18 kD peripheral benzodiazepine receptor (PBR). We tested the hypothesis that an endogenous ligand of the PBR, hemin, could modulate calcium transport by modifying VDAC conductance. In isolated rat cardiac mitochondria, hemin (0-10 μM) exhibited multiple, time-dependent effects. Initially, hemin reduced the calcium uptake rate in a dose-dependent manner, an effect independent of the mitochondrial permeability transition (MPT) as it was not altered by cyclosporine A (CsA). However, subsequent to this inhibitory effect on calcium influx, hemin facilitated MPT as ...
Gamma-aminobutyric acid receptor subunit alpha-1 is a protein that in humans is encoded by the GABRA1 gene. GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified. The GABRA1 receptor is the specific target of the z-drug class of nonbenzodiazepine hypnotic agents and is responsible for their hypnotic and hallucinogenic effects. GABAA receptor GRCh38: Ensembl release 89: ENSG00000022355 - Ensembl, May 2017 GRCm38: Ensembl release 89: ENSMUSG00000010803 - Ensembl, May 2017 "Human PubMed Reference:". "Mouse PubMed Reference:". Johnson KJ, Sander T, Hicks AA, van Marle A, Janz D, Mullan MJ, Riley BP, Darlison MG (Dec 1992). "Confirmation of the localization of the human GABAA receptor alpha 1-subunit gene (GABRA1) to ...
The "ambient" GABA that is present in the extracellular space surrounding all neurons of the brain is believed to be capable of persistently activating high‐affinity extrasynaptic GABA-A receptors to generate a tonic membrane conductance. This generates a form of shunting inhibition that is capable of influencing cellular and network excitability. Extrasynaptic δ subunit-containing GABA-A receptors are known to generate this form of tonic inhibition in a number of defined brain regions and these are emerging as important clinical drug targets for the treatment of a number of neurological conditions. This thesis examines the functional and pharmacological properties of recombinant and native GABA-A receptors that allow them to function as ambient GABA detectors. Surprisingly, the data presented in this Thesis shows that the behaviour of these extrasynaptic GABA-A receptor populations is dramatically influenced by the steady-state GABA concentration they experience. For example, recombinant ...
Tonic GABAA Receptor Currents in the Thalamus Delia Belelli, Dianne R. Peden, Thomas W. Rosahl, Keith A. Wafford, and Jeremy J. Lambert. (see pages 11513-11520). David W. Cope, Stuart W. Hughes, and Vincenzo Crunelli. (see pages 11553-11563). Several recent studies have reported "tonic" activation of extrasynaptic GABAA receptors containing the δ subunit. This week, two papers examined the action of tonic GABAA currents in the thalamus. Cope et al. report that most thalamocortical neurons of the dorsal lateral geniculate nucleus and ventrobasal (VB) complex, but not the nucleus reticularis, had tonic GABAA currents. Block of the tonic current caused cells to switch from low-threshold bursts of actions potentials to tonic firing. Belelli et al. also examined tonic GABAA current in VB cells using the hypnotic drug etomidate, which acts on β2 subunit-containing receptors. Activation of the tonic current in VB cells was associated with increases in the slow-wave activity characteristic of the ...
Compounds which bind with high affinity to peripheral benzodiazepine receptors are useful as antiinflammatory agents. Such compounds include isoquinoline and benzodiazepine derivatives, such as PK 111
The embryonic and postnatal expression of 13 GABAA receptor subunit genes in the rat CNS was studied by in situ hybridization. Each transcript exhibited a unique regional and temporal developmental expression profile. For example, in both embryonic and early postnatal cortex and thalamus, expression of the alpha 2, alpha 3, alpha 5, and beta 3 mRNAs was pronounced. In particular, the alpha 5 gene expression underwent a prominent peak in early brain. Subsequently, the thalamocortical expression of these four genes substantially diminished and was superseded in the adult by the alpha 1, alpha 4, beta 2, and delta subunit mRNAs. Similarly, gamma 1 and gamma 3 gene expression also dropped markedly during development, their initial stronger expression being restricted to relatively few structures. In contrast, gamma 2 gene expression was widespread and mostly remained constant with increasing age. The medial septum and globus pallidus were regions expressing few subunits in both early postnatal and ...
The goal of the present studies was to determine whether fyn gene deletion altered the behavioral and functional actions of drugs that act at GABAA receptors. To this end, we obtained our own colony of fyn-null mutant and wild-type mice. Similar to the results of Miyakawa et al. (1997) using mice that were developed by a different research group, our null mutants were more sensitive to the hypnotic effects of ethanol (Boehm et al., 2003), a compound known to enhance GABAA receptor function. Moreover, although the genotypes did not differ in hypnotic sensitivity to the positive allosteric modulators pentobarbital, flurazepam, and alfaxalone, our fyn-deficient mice exhibited a shorter duration of loss of righting reflex following administration of the GABAA receptor agonist, THIP.. The above results were consistent with those of Kitazawa et al. (1998) and suggested that fyn gene deletion altered GABAA receptor function, so we next assessed the actions of THIP using a functional assay. ...
Tonic inhibitory conductances mediated by GABAA receptors have now been identified and characterised in many different brain regions. Most experimental studies of tonic GABAergic inhibition have been carried out using acute brain slice preparations but tonic currents have been recorded under a variety of different conditions. This diversity of recording conditions is likely to impact upon many of the factors responsible for controlling tonic inhibition and can make comparison between different studies difficult. In this review, we will firstly consider how various experimental conditions, including age of animal, recording temperature and solution composition, are likely to influence tonic GABAA conductances. We will then consider some technical considerations related to how the tonic conductance is measured and subsequently analysed, including how the use of current noise may provide a complementary and reliable method for quantifying changes in tonic current.
Behavioral and neurochemical evidence indicates links between the opioid and GABA neurotransmitter systems. To assess effects of chronic opiates on the major site of postsynaptic GABAergic activity,...
BioAssay record AID 389903 submitted by ChEMBL: Displacement of [3H]PK11195 from peripheral benzodiazepine receptor in Sprague-Dawley rat cerebral cortex membrane by liquid scintillation counting.
A large body of work now shows the importance of GABAA receptor-mediated tonic inhibition in regulating CNS function. However, outside of pathological conditions, there is relatively little evidence that the magnitude of tonic inhibition is itself under regulation. Here we review the mechanisms by which tonic inhibition is known to be modulated, and outline the potential behavioural consequences of this modulation. Specifically, we address the ability of protein kinase A and C to phosphorylate the extrasynaptic receptors responsible for the tonic GABAA current, and how G-protein coupled receptors can regulate tonic inhibition through these effectors. We then speculate about the possible functional consequences of regulating the magnitude of the tonic GABAA current.
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Here, we find that chronic exposure to either immobilization or unpredictable stress results in enduring loss of tonic GABAAR current in LA while leaving the phasic GABAARs unaffected. Such loss is primarily due to the production of CORT with subsequent activation of GR and leads to an impaired GABAergic control over the neuronal excitability in amygdala. Given the essential role of amygdala GABAAR in maintaining the appropriate expression of emotion such as fear and anxiety[9], we propose that the defective tonic inhibition may represent one of the key mechanisms through which prolonged stress exerts its persistent and detrimental action on brains processing of the emotionally salient events.. The GABAARs mediating the tonic and phasic inhibition in CNS differ considerably in terms of their subunit composition, subcellular localization, kinetic and pharmacological properties[23]. Despite these, they both are exquisitely sensitive to the changes in their environment. For instance, the elevated ...
GABA (γ-aminobutyric acid) is the main neuroinhibitory transmitter in mammalian brains. It binds to GABA-A and GABA-B receptors. The GABA-A receptors are ligand-gated chloride channels. A variety of GABA-A receptor agonists and antagonists have been developed to study the GABA-mediated inhibition and to explore new medications. In this thesis I have examined the role of GABA in brain tumors and the effects of the metabolic hormone GLP-1 on GABAergic signaling in neurons.. I studied if GABA-A receptors subunits were expressed and formed functional ion channels in the glioblastoma cell line U3047MG. I identified the mRNA of 11, α2, α3, α5, β1, β2, β3, δ, γ3, π, θ and ρ2, out of the 19 known GABA-A subunits. Immunostaining demonstrated abundant expression of the α3 and β3 subunits. Interestingly, whole-cell GABA-activated currents were recorded in only 12% of the cells. The GABA-activated currents half-maximal concentration (EC50) was 36 µM. The currents were modulated by diazepam (1 ...
Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the GABRA4 gene.[5][6] GABA is the major inhibitory neurotransmitter in the mammalian brain where it acts at GABA-A receptors, which are ligand-gated chloride channels. Chloride conductance of these channels can be modulated by agents such as benzodiazepines that bind to the GABA-A receptor. At least 16 distinct subunits of GABA-A receptors have been identified.[6] ...
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L929 cells expressing the α1β3ε GABAR isoform consistently produced a large holding current when voltage clamped at -75 mV that was sensitive to both positive and negative allosteric modulators of GABARs but was not affected by the application of glycine. Other subunit combinations, including α1β3γ2L, α1β3δ, α1β3, α1ε, and β3ε, and ε alone failed to produce significant holding currents that were sensitive to enhancement by loreclezole or block by picrotoxin or zinc. Specifically, the negative results obtained with transfections of α1ε or β3ε subtypes or the ε subunit alone strongly suggested that channels potentially composed of only one or two of the three transfected subunits were not contributing to the observed holding current.. To date, the only wild-type GABAR isoforms reported to result in spontaneously active currents are β1 (Sigel et al., 1989; Krishek et al., 1996), β3 (Wooltorton et al., 1997), and α4β1 GABAR isoforms (Khrestchatisky et al., 1989). The ...
Pagoclone, also known as CI-1043; IP-456; RP-62955; RP-59037, is a GABA receptor agonist potentially for the treatment of stuttering, panic disorder and generalised anxiety. It binds with roughly equivalent high affinity (0.7-9.1 nM) to the benzodiazepine binding site of human GABAA receptors containing either an α1, α2, α3 or α5 subunit. It is a partial agonist at α1-, α2- and α5-containing GABAA receptors and a full agonist at receptors containing an α3 subunit.
Ocean acidification is one of the most pressing environmental concerns of our time, and not surprisingly, we have seen a recent explosion of research into the physiological impacts and ecological consequences of changes in ocean chemistry. We are gaining considerable insights from this work, but further advances require greater integration across disciplines. Here, we showed that projected near-future CO₂ levels impaired the ability of damselfish to learn the identity of predators. These effects stem from impaired neurotransmitter function; impaired learning under elevated CO₂ was reversed when fish were treated with gabazine, an antagonist of the GABA-A receptor - a major inhibitory neurotransmitter receptor in the brain of vertebrates. The effects of CO₂ on learning and the link to neurotransmitter interference were manifested as major differences in survival for fish released into the wild. Lower survival under elevated CO₂, as a result of impaired learning, could have a major ...
Introduction. Interictal spikes, identifiable as sharp transient deflections (30-50 ms) in electroencephalographic recordings, are electrographic markers of epilepsy (Pedley, 1984). Recordings during epileptic surgery operations show that up to 50% of cells exhibit burst discharge in the focus during interictal spikes (Wyler & Ward, 1981). These studies demonstrate directly that synchronized burst firing in populations of cortical neurons sustains the epileptiform activity. Clearly, information concerning the mechanisms underlying synchronized burst discharge are of fundamental importance to the understanding of epileptogenesis.. That GABAergic (GABA is γ-aminobutyric acid) inhibitory transmission regulates epileptiform activity is indicated by the action of several convulsant compounds. Analogues of interictal spikes can be produced experimentally with agents such as penicillin, bicuculline, and picrotoxin. These agents are all potent blockers of GABAA receptor function (see e.g., Macdonald, ...
TY - JOUR. T1 - GABA-A receptors and the response to CO2 inhalation - a translational trans-species model of anxiety?. AU - Bailey, JE. AU - Nutt, DJ. PY - 2008/7. Y1 - 2008/7. M3 - Article (Academic Journal). VL - 90(1). SP - 51. EP - 57. JO - Pharmacology, Biochemistry and Behavior. JF - Pharmacology, Biochemistry and Behavior. SN - 0091-3057. ER - ...
Reviews the interaction between anxiety and the immune system and modulating effects of benzodiazepines. Research indicates that anxiety induces immune-inflammatory changes pointing toward the complex regulatory responses in interleukin-6 signalling, decreased anti-inflammatory capacity of the serum, and interactions with T cell and monocytic activation. Experimental and clinical studies suggest that the central and peripheral benzodiazepine receptors together with their ligands form a network Show moreReviews the interaction between anxiety and the immune system and modulating effects of benzodiazepines. Research indicates that anxiety induces immune-inflammatory changes pointing toward the complex regulatory responses in interleukin-6 signalling, decreased anti-inflammatory capacity of the serum, and interactions with T cell and monocytic activation. Experimental and clinical studies suggest that the central and peripheral benzodiazepine receptors together with their ligands form a network ...
The effect of a 70% (v/v) ethanolic leaf extract of Palisota hirsuta, a traditional West African plant used for CNS disorders and pain, in animal models of anxiety and depression-the open field test, the light/dark box, the Elevated plus Maze (EPM), the Forced Swimming Test (FST) and Tail Suspension Test (TST) has been reported. P. hirsuta (30-300 mg kg-1) treated mice exhibited anxiolytic activity in all the anxiety models used by significantly increasing the percentage of center entries and the percentage time spent in the center of the open field. P. hirsuta also significantly increased the time spent in the lit area in comparison to the time spent in the dark area of the light/dark box. In the EPM, it significantly increased open arm activity which was completely reversed by flumazenil (3 mg kg-1), a specific antagonist of the GABAA benzodiazepine receptor complex. In the antidepressant test, the extract also dose-dependently reduced the duration of immobility in both the FST (ED50: ...
Feature :. GABAA receptors containing the H101R point mutation are insensitive to modulation by benzodiazepines such as diazepam. In GABRA2-H101R mice, the anxiolytic-like action of diazepam and in part its myorelaxant action are missing.. ...
In part, the underlying reason is that preembedding techniques fail to detect a majority of epitopes located at postsynaptic sites (Somogyi et al. 1989; Soltesz et al. 1990). , using Lowicryl-embedded tissue, are required for studying postsynaptic GABAAR (Baude et al. 1992; Nusser and Somogyi 1994; Somogyi et al. 1996). In this case, however, the majority of antibodies available lack sensitivity and, therefore, information is available for the α1, α2, α4, α5, α6, β2, 3, δ, and γ2 subunits only in selected brain areas (such as cerebral cortex, hippocampus, olfactory bulb, pallidum, thalamus, cerebellum, and spinal cord) (Nusser and Somogyi 1994; Nusser et al. For example, multiple γ subunit subtypes have been reported in a subset of native (Quirk et al. 1994; Khan et al. 1994; Benke et al. 1996) and recombinant (Backus et al. 1993) receptors. Although it is unclear if multiple δ subunits can also be incorporated in the same pentamer, recent evidence using concatenated subunits suggests ...
GABAA receptors are ligand-gated ion channels composed of five subunits that can be opened by GABA and be modulated by multiple pharmacologically and clinically important drugs. Over the time, hundreds of compounds from different structural classes have been demonstrated to modulate, directly activa …
Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
The main focus of the Orser Lab is to understand the molecular mechanism of general anesthesia, repurpose general anesthetics for novel treatment of neurological disorders, and to the study the role of GABAA receptor in health and disease. Their studies also offer insights into the neuronal substrates that underlie pain, memory and consciousness.. They are the first to demonstrate the exquisite sensitivity of a population of extrasynaptic GABAA receptors to volatile and inhaled anesthetics. Behavioural studies using preclinical models have shown that the actions of anesthetics at extrasynaptic GABAA receptors in the hippocampus contribute to the amnestic properties of the drugs. The findings challenged the prevailing dogma that anesthetics act by increasing inhibitory synaptic transmission. These results have stimulated new areas of anesthetic research in laboratories around the world. In addition, the laboratory was the first to demonstrate the ability of anesthetics to reduce desensitization ...
Recent research has shown that it is possible to design GABAA receptor targeting with fewer side effects by fine tuning their selectivity profile. It should further be possible to treat disorders not addressable with standard GABAA modulators like the benzodiazeopines.. Our lead program will seek compounds that selectively target GABAA receptors that contain the α2 and α3 subunits. These molecules will be initially developed to treat neuropathic pain. However, we also expect that they will be useful for a variety of other indications including anxiety, depression, autism and startle disorder.. We will also develop neurosteroids that modulate the GABAA receptor. Neurosteroids bind the GABAA receptor at a different site than benzodiazeopines. As a result, they inherently have a different selectivity profile and are typically strong activators of the receptor. In addition to the indications indicated for our lead program, these molecules may have special utility for certain epilepsies.. ...
Six wild-type and mutant GABAAreceptors were expressed by transfection of HEK 293 cells: α2β1 wild-type, α2(S270I)β1, α2(S270H)β1, α2(A291W)β1, α2β1(S265I), or α2β1(M286W). After transient expression in HEK 293 cells, all of the wild-type and mutant receptors tested in this study produced inward currents in response to application of GABA via the rapid solution changer. The EC50 and Hill slope values estimated from GABA concentration-response curves for receptors that contain either mutant α2 or β1 subunits demonstrate that these receptors retain GABA concentration-response relationships that are similar to those of wild-type α2β1 receptors: α2β1 wild-type (EC50 = 8.7 ± 0.4 μm, nH = 1.9 ± 0.2, nine experiments), α2(S270I)β1 (EC50 = 14.6 ± 0.1 μm,nH = 2.4 ± 0.1, six experiments), α2(S270H)β1 (EC50 = 3.5 ± 0.2 μm, nH = 1.5 ± 0.1, five experiments), α2(A291W)β1 (EC50 = 2.4 ± 0.1 μm, nH = 1.7 ± 0.2, five experiments), α2β1(S265I) (EC50 = 37.5 ± 8.5 μm, nH = ...
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Alcohol abuse and alcoholism are widespread public health problems that are associated with debilitating medical, social, and psychological consequences. The ab...
Benzodiazepines, also referred to as benzos, are a class of agents that work on the central nervous system, acting selectively on gamma-aminobutyric acid-A (GABA-A) receptors in the brain. GABA is a neurotransmitter that inhibits or reduces the activity of nerve cells (neurons) within the brain. Benzodiazepines open GABA-activated chloride channels, [...]. ...
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GABRG1 - GABRG1 (untagged)-Human gamma-aminobutyric acid (GABA) A receptor, gamma 1 (GABRG1) available for purchase from OriGene - Your Gene Company.
Autism is a condition which demands more research - even if some autistic people do not want their condition to be cured, most would like some of their symptoms to be alleviated.
BioAssay record AID 385597 submitted by ChEMBL: Activity of human GABA alpha-1-beta-2-gamma-2L receptor in HEK293 cells expressing as-PKCepsilon assessed as inhibition of ethanol induced GABA current at 30 uM.
[email protected] Biomarkers Consortiums PET Radioligand Project, completed in December 2012, developed improved, more sensitive PET radioligands with higher binding to the peripheral benzodiazepine receptor. Findings from this study suggest that the [11C]PBR38 ligand, in particular, may be useful in detecting progression from mild cognitive impairment or treatment response in Alzheimers Disease.. ...
[email protected] Biomarkers Consortiums PET Radioligand Project, completed in December 2012, developed improved, more sensitive PET radioligands with higher binding to the peripheral benzodiazepine receptor. Findings from this study suggest that the [11C]PBR38 ligand, in particular, may be useful in detecting progression from mild cognitive impairment or treatment response in Alzheimers Disease.. ...
We are a clinical-stage biopharmaceutical company committed to developing and commercializing novel medicines to treat life-altering central nervous system, or CNS, disorders, where there are no approved therapies or existing therapies are inadequate. We have a portfolio of product candidates with a current focus on modulating two critical CNS receptor systems, GABA and NMDA. The GABA receptor family, which is recognized as the major inhibitory neurotransmitter in the CNS, mediates downstream neurologic and bodily function via activation of GABAA receptors. The NMDA-type receptors of the glutamate receptor system are a major excitatory receptor system in the CNS. Dysfunction in these systems is implicated in a broad range of CNS disorders. We are targeting CNS indications where patient populations are easily identified, clinical endpoints are well-defined, and development pathways are feasible. ... More ... ...
Lenti ORF particles, GABRA5 (Myc-DDK tagged) - Human gamma-aminobutyric acid (GABA) A receptor, alpha 5 (GABRA5), transcript variant 2 , 200ul, >10^7 TU/mL ...
Gross, Anna, Sims, Robert, Swinny, J.D., Sieghart, W., Bolam, Paul J. and Stanford, Ian (2011). Differential localization of GABAA receptor subunits in relation to rat striatopallidal and pallidopallidal synapses. European Journal of Neuroscience, 33 (5), pp. 868-878. ...
This line was derived from the human embryonic kidney line, 293 (see ATCC CRL-1573). 293 cells were transfected with an expression plasmid containing cDNA encoding the rat GABA-A receptor alpha 1, beta 2 and gamma 2 subunits. Genomic integration of the transfected alpha and gamma subunit genes was confirmed; however, the beta subunit sequences were not detected in Northern and Southern blots. Stable transfectant expressing a type I GABAA receptor (alpha1 and gamma2 subunits).
A strong promoter element is located between alternative exons of a gene encoding the human gamma-aminobutyric acid-type A receptor beta 3 subunit (GABRB3 ...
Complete information for GABRA1 gene (Protein Coding), Gamma-Aminobutyric Acid Type A Receptor Alpha1 Subunit, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
Complete information for GABRB1 gene (Protein Coding), Gamma-Aminobutyric Acid Type A Receptor Beta1 Subunit, including: function, proteins, disorders, pathways, orthologs, and expression. GeneCards - The Human Gene Compendium
Objective. Inflammation in the vascular wall plays an important role in the pathophysiology of atherosclerosis, including development of plaque, plaque destabilization and rupture. Clinical and basic scientific data demonstrate the importance of peripheral white blood cells in this process. Therefore, a noninvasive method to detect inflammatory activity in atherosclerosis may be of great value to help determine prognosis, direct therapy and perhaps assess novel therapies for stabilization of atherosclerotic plaque.. The peripheral benzodiazepine receptor (PBR) is distinct from central benzodiazepine receptors associated with GABAA receptors and has been associated with immune function. PBR is expressed in macrophages, therefore, they may be a clinically useful marker to detect inflammation. Our preliminary autoradiographic data demonstrate specific PBR binding in carotid atherosclerosis samples. Though PBR has been imaged in vivo with positron emission tomography (PET) using ...
ABSTRACT Background: The Peripheral Benzodiazepine Receptor (PBR) can be classified as a distinct receptor from the central benzodiazepine receptor. The PBR gene has been located to chromosome 22q13.31 in humans and has been found to consist of four exons, with the first and half of the fourth exon being untranslated to form the PBR protein. PBR is involved in numerous biological conditions including the regulation of cellular proliferation and apoptosis, steroidogenesis, heme biosynthesis, anion and porphyrin transport and mitochondrial functions such as oxidative phosphorylation and translocation of cholesterol from the outer to the inner mitochondrial membrane. Recent studies showed that the expression of PBR correlated with tumour malignancy and patient survival. Aim: The objectives of this research were to determine the expression pattern and level of PBR mRNA in various types of human normal and cancer tissues and to isolate the PBR protein ...