Journal of receptor research最新文献_第5页

GABAA-receptors: drug binding profile and distribution of receptors containing the alpha 2-subunit in situ. gabaa受体:含有α - 2亚基的受体的药物结合谱和分布。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073673

R Marksitzer, D Benke, J M Fritschy, A Trzeciak, W Bannwarth, H Mohler

{"title":"GABAA-receptors: drug binding profile and distribution of receptors containing the alpha 2-subunit in situ.","authors":"R Marksitzer, D Benke, J M Fritschy, A Trzeciak, W Bannwarth, H Mohler","doi":"10.3109/10799899309073673","DOIUrl":"https://doi.org/10.3109/10799899309073673","url":null,"abstract":"The highest structural diversity of GABAA-receptor subunits is observed among members of the alpha-subunit class. Using subunit-specific antisera, the receptors containing the alpha 2-subunit were characterized. Western blots revealed an apparent molecular size of 52 kDa for the alpha 2-subunit. Immunohistochemically, the alpha 2-subunit was most preponderant in areas which lack the alpha 1-subunit, e.g. striatum and olfactory bulb granule cell layer, suggesting that these two subunits represent largely distinct receptor subtypes. Pharmacologically, the receptor population which was immunoprecipitated by the alpha 2-subunit-specific antisera displayed a drug binding profile characterized by a low affinity for CL 218872, beta CCM and zolpidem. This is in striking contrast to the high affinities of these ligands displayed by receptors immunoprecipitated by the alpha 1-subunit-specific antiserum. Thus, the alpha 1- and the alpha 2-subunit characterize two GABAA-receptor populations which greatly differ in brain distribution and pharmacological profile.","PeriodicalId":16948,"journal":{"name":"Journal of receptor research","volume":"13 1-4","pages":"467-77"},"PeriodicalIF":0.0,"publicationDate":"1993-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3109/10799899309073673","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19369687","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 74

Cloning of the long intracellular loop of the AMPA-selective glutamate receptor for phosphorylation studies. 克隆ampa -选择性谷氨酸受体细胞内长环用于磷酸化研究。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073685

M S Wright, I Sefland, S I Walaas

引用次数: 4

Detergent solubilization is a prerequisite for aggregation-induced stimulation of epidermal growth factor (EGF) receptor kinase. 洗涤剂增溶是聚集诱导的表皮生长因子(EGF)受体激酶刺激的先决条件。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073696

R E Gates, L E King

{"title":"Detergent solubilization is a prerequisite for aggregation-induced stimulation of epidermal growth factor (EGF) receptor kinase.","authors":"R E Gates, L E King","doi":"10.3109/10799899309073696","DOIUrl":"https://doi.org/10.3109/10799899309073696","url":null,"abstract":"Unlike EGF, concanavalin A and wheat germ agglutinin do not increase EGF receptor-kinase activity in intact A-431 membranes. However, they increase both autophosphorylation and phosphorylation of exogenous substrates about twice as much as EGF if the membranes are solubilized in detergent. Following solubilization, autophosphorylation due to the combined presence of a lectin and EGF is additive suggesting that each increases kinase activity by a different mechanism. These different mechanisms were studied by autophosphorylating membranes at increasing detergent concentrations after they had been permeabilized to [gamma-32P]ATP with alamethicin. As the detergent concentration increased, EGF stimulated autophosphorylation decreased 3-fold and 6-fold for the native 170 kDa receptor and for a protease-generated 150 kDa receptor form, respectively. However, in the presence of either lectin the same increase in detergent concentration only slightly altered the autophosphorylation rates which never exceeded the rate measured in the absence of EGF and detergent. Hence, the lectins increase kinase activity in solubilized membranes by preventing the adverse effects of detergent on the receptor-kinase and may not be useful models for how EGF activates its receptor.","PeriodicalId":16948,"journal":{"name":"Journal of receptor research","volume":"13 5","pages":"829-47"},"PeriodicalIF":0.0,"publicationDate":"1993-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3109/10799899309073696","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19370407","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 1

Lack of interaction of vasopressin with its antisense peptides: a functional and immunological study. 抗利尿激素与其反义肽缺乏相互作用:一项功能和免疫学研究。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073699

M Jurzak, I Pavo, F Fahrenholz

{"title":"Lack of interaction of vasopressin with its antisense peptides: a functional and immunological study.","authors":"M Jurzak, I Pavo, F Fahrenholz","doi":"10.3109/10799899309073699","DOIUrl":"https://doi.org/10.3109/10799899309073699","url":null,"abstract":"The peptide encoded in the 5' to 3' direction by rat vasopressin complementary RNA, rat PVA (H-Ser-Ser-Trp-Ala-Val-Leu-Glu-Val-Ala- OH) and the corresponding bovine PVA (H-Ala-Pro-Trp-Ala-Val-Leu-Glu-Val-Ala-OH) were investigated with respect to their interaction with [8-arginine] vasopressin (AVP) and V2 vasopressin receptor binding and function. Rat or bovine PVA did neither affect the binding of the hormone to the V2 receptor of bovine kidney membranes and LLC-PK1 pig kidney cells nor influence the AVP-induced cAMP-production in LLC-PK1 cells. Rat PVA was further investigated by the use of vasopressin-specific polyclonal and monoclonal antibodies with different affinity and epitope specificity. Consistent with receptor binding studies no inhibition of [3H]AVP-binding in fluid- or solid-phase antibody binding tests after preincubation with PVA was found. Direct interaction of rat PVA and [3H]AVP measured on solid surface was not observed in contrast to specific binding of the hormone with NP II and antibodies. In our study no evidence for an interaction of AVP and its antisense peptides was found.","PeriodicalId":16948,"journal":{"name":"Journal of receptor research","volume":"13 5","pages":"881-902"},"PeriodicalIF":0.0,"publicationDate":"1993-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3109/10799899309073699","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19370408","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 10

Mechanotransduction in stretch-induced hypertrophy of cardiac myocytes. 拉伸诱导心肌细胞肥大的机械转导。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073692

J Sadoshima, S Izumo

{"title":"Mechanotransduction in stretch-induced hypertrophy of cardiac myocytes.","authors":"J Sadoshima, S Izumo","doi":"10.3109/10799899309073692","DOIUrl":"https://doi.org/10.3109/10799899309073692","url":null,"abstract":"Mechanical loading of cardiac muscles causes rapid activation of a number of immediate-early (IE) genes and hypertrophy. However, little is known as to how muscle cells sense mechanical load and regulate gene expression. We examined roles of several putative mechanotransducers in stretch-induced hypertrophy of cardiac myocytes grown on a deformable silicone sheet. Using the patch-clamp technique, we found a single class of stretch-activated cation channels which was completely and reversibly blocked by gadolinium. The inhibition of this channel by gadolinium did not affect either stretch-induced expression of the IE genes or hypertrophy. Neither disruption of microtubules with colchicine nor that of actin microfilaments by cytochalasin D prevented the stretch-induced IE gene expression. Arresting contractile activity by tetrodotoxin did not affect the stretch-induced IE gene expression or hypertrophy. These results suggest that stretch-activated cation channels, microtubules, microfilaments, and contractile activity are not the mechanotransducers. Preliminary results suggest that cell stretch may cause a release of a growth factor(s), which in turn initiates a cascade of hypertrophic response of cardiac myocytes.","PeriodicalId":16948,"journal":{"name":"Journal of receptor research","volume":"13 1-4","pages":"777-94"},"PeriodicalIF":0.0,"publicationDate":"1993-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3109/10799899309073692","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19432901","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 51

Cyclopeptide analogs for characterization of the neuropeptide Y Y2-receptor. 表征神经肽yy2受体的环肽类似物。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073656

A G Beck-Sickinger, H Köppen, E Hoffmann, W Gaida, G Jung

引用次数: 6

Solubilization and characterization of high affinity follicle-stimulating hormone receptors from porcine granulosa cells. 猪颗粒细胞高亲和性促卵泡激素受体的增溶和特性研究。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073701

S J Sperbeck, D Y Song, A R LaBarbera

{"title":"Solubilization and characterization of high affinity follicle-stimulating hormone receptors from porcine granulosa cells.","authors":"S J Sperbeck, D Y Song, A R LaBarbera","doi":"10.3109/10799899309073701","DOIUrl":"https://doi.org/10.3109/10799899309073701","url":null,"abstract":"Follicle-stimulating hormone (FSH)-receptors were solubilized from immature porcine ovarian granulosa cells with retention of high affinity 125I-porcine FSH-binding activity. The optimal concentration of Triton X-100 for solubilization was 0.5% (w/v), and the optimal cellular protein concentration 25 mg/ml. Glycerol (30%) increased recovery of solubilized receptor. 125I-pFSH-binding affinity ranged from 4 x 10(10) M-1 to 8 x 10(10) M-1 in either the absence or presence of glycerol. 125I-pFSH-binding capacity was 5 fmol/mg protein in the absence of glycerol and 58 fmol/mg protein in the presence of glycerol as determined by equilibrium saturation binding analysis. By gel permeation chromatography, the apparent size of the 125I-pFSH-receptor complex was 462 kDa in the absence of glycerol and 762 kDa in the presence of glycerol. Ligand blotting of solubilized receptor yielded a single species with an apparent molecular weight of 200 kDa under nonreducing conditions and a single species with an apparent molecular weight of 60 kDa under reducing conditions. These studies indicated that high affinity FSH-binding activity can be solubilized from membranes of immature porcine granulosa.","PeriodicalId":16948,"journal":{"name":"Journal of receptor research","volume":"13 6","pages":"925-42"},"PeriodicalIF":0.0,"publicationDate":"1993-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3109/10799899309073701","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"19490650","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 2

Expression of a rat PDGF receptor beta ectodomain generates a low affinity ligand antagonist. 大鼠PDGF受体β外结构域的表达产生低亲和力配体拮抗剂。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073689

B Herren, M Pech

引用次数: 4

Biochemical characterization of a novel channel-activating site on nicotinic acetylcholine receptors. 烟碱乙酰胆碱受体新通道激活位点的生化表征。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309073669

A Schrattenholz, T Coban, B Schröder, K O Okonjo, J Kuhlmann, E F Pereira, E X Albuquerque, A Maelicke

{"title":"Biochemical characterization of a novel channel-activating site on nicotinic acetylcholine receptors.","authors":"A Schrattenholz, T Coban, B Schröder, K O Okonjo, J Kuhlmann, E F Pereira, E X Albuquerque, A Maelicke","doi":"10.3109/10799899309073669","DOIUrl":"https://doi.org/10.3109/10799899309073669","url":null,"abstract":"We have studied the interaction of the reversible acetylcholine esterase inhibitor (-)physostigmine and several structurally related compounds with the nicotinic acetylcholine receptor (nAChR) from Torpedo marmorata electric tissue by means of ligand-induced ion flux into nAChR-rich membrane vesicles, direct binding studies and photoaffinity labeling. (-)Physostigmine acts as a channel-activating ligand at low concentrations and as a direct channel blocker at elevated concentrations. Channel activation is not inhibited by desensitizing concentrations of ACh or ACh-competitive ligands (including alpha-bungarotoxin and D-tubocurarine) but is inhibited by antibody FK1 and several other compounds. From photoaffinity labeling using tritiated physostigmine and mapping of the epitope for the Phy-competitive antibody FK1, the binding site for physostigmine is located within the alpha-subunit of the Torpedo nAChR and is distinct from the acetylcholine binding site. Our data suggest a second pathway of nAChR channel activation that may function physiologically as an allosteric control of receptor activity.","PeriodicalId":16948,"journal":{"name":"Journal of receptor research","volume":"13 1-4","pages":"393-412"},"PeriodicalIF":0.0,"publicationDate":"1993-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.3109/10799899309073669","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"18685326","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 22

Nonlinear regression analysis of the time course of ligand binding experiments. 配体结合实验时间过程的非线性回归分析。

Journal of receptor research Pub Date : 1993-01-01 DOI: 10.3109/10799899309063268

R G Duggleby, M J Waters

引用次数: 2