Characterization of novel fluorescent ligands with high affinity for D1 and D2 dopaminergic receptors.

Abstract:

:We have synthesized and characterized a series of novel fluorescently labeled ligands with high affinity and specificity for D1 and D2 dopamine receptors. D1-selective probes were synthesized using (R,S)-5-(4'-aminophenyl)-8-chloro-2,3,4,5-tetrahydro-3-methyl- [1H]-3-benzazepin-7-ol, the 4'-amino derivative of the high-affinity, D1-selective antagonist SCH-23390, whereas D2-selective probes were synthesized using the high-affinity, D2-selective antagonist N-(p-aminophenethyl)spiperone (NAPS). These ligands were coupled via spacer arms of various lengths to the fluorophores fluorescein and bodipy, which fluoresce in the yellow-green region, and to tetramethylrhodamine, which is a red fluorophore. The interaction of these fluorescent ligands with dopamine receptors was evaluated by examining their ability to compete for the binding of the radiolabeled antagonists [3H]SCH-23390 or [3H]methylspiperone to rat striatal D1 or D2 dopamine receptors, respectively. We report here that these novel fluorescent ligands exhibit very high affinity and specificity for either D1 or D2 dopamine receptors. The availability of various fluorescent ligands with different emission maxima and with high affinity and specificity for D1 and D2 dopamine receptors will now permit investigations involving the visualization and localization of these receptor subtypes at the single cell and intracellular levels in the CNS and on intact cells in culture.

journal_name

J Neurochem

authors

Monsma FJ Jr,Barton AC,Kang HC,Brassard DL,Haugland RP,Sibley DR

doi

10.1111/j.1471-4159.1989.tb09220.x

subject

Has Abstract

pub_date

1989-05-01 00:00:00

pages

1641-4

issue

5

eissn

0022-3042

issn

1471-4159

journal_volume

52

pub_type

杂志文章
  • Influence of monoclonal antibodies on microtubule assembly.

    abstract::The influence on microtubule assembly in vitro of monoclonal antibodies against microtubule-associated proteins (MAPs) was studied. Light scattering was used for measuring net polymer formation and electron microscopy for determining the influence of antibodies on microtubule morphology. Control experiments showed tha...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1987.tb00952.x

    authors: Matus A,Riederer B,Huber G

    更新日期:1987-09-01 00:00:00

  • Endoplasmic reticulum calcium release is modulated by actin polymerization.

    abstract::Intracellular calcium ions regulate the structure and functions of cytoskeletal proteins. On the other hand, recent studies have shown that the cytoskeleton, and actin filaments in particular, can modulate calcium influx through plasma membrane ligand- and voltage-gated channels. We now report that calcium release fro...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2002.01059.x

    authors: Wang Y,Mattson MP,Furukawa K

    更新日期:2002-08-01 00:00:00

  • Angiotensin II synthesis studies in dissociated brain cell cultures.

    abstract::The biosynthesis of angiotensin II-like peptide was measured in primary cultured brain cells from the fetal rat. Cells from the whole brains of 20-day gestational age Sprague-Dawley rats were dissociated by mild trypsinization and grown for 5 days in supplemented (serum-free) medium prior to experimental analysis. The...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1984.tb12791.x

    authors: Weyhenmeyer JA,Meyer JM,Watkins JE

    更新日期:1984-09-01 00:00:00

  • Drug testing complementary metal-oxide-semiconductor chip reveals drug modulation of transmitter release for potential therapeutic applications.

    abstract::Neurodegenerative diseases, such as Parkinson's disease, Alzheimer's disease, and Huntington's disease, are considered incurable and significantly reduce the quality of life of the patients. A variety of drugs that modulate neurotransmitter levels have been used for the treatment of the neurodegenerative diseases but ...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/jnc.14815

    authors: Huang M,Rathore SS,Lindau M

    更新日期:2019-10-01 00:00:00

  • High calcium permeability of serotonin 5-HT3 receptors on presynaptic nerve terminals from rat striatum.

    abstract::The serotonin 5-HT3 receptor, a ligand-gated ion channel, has previously been shown to be present on a subpopulation of brain nerve terminals, where, on activation, the 5-HT3 receptors induce Ca2+ influx. Whereas postsynaptic 5-HT3 receptors induce depolarization, being permeant to Na+ and K+, the basis of presynaptic...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1998.70031094.x

    authors: Rondé P,Nichols RA

    更新日期:1998-03-01 00:00:00

  • Determination of amino acids and monoamine neurotransmitters in caudate nucleus of seizure-resistant and seizure-prone BALB/c mice.

    abstract::Amino acid and monoamine concentrations were examined in tissue extracts of caudate nucleus of genetic substrains of BALB/c mice susceptible or resistant to audiogenic seizures. Amino acids [aspartate, glutamate, glycine, taurine, serine, gamma-aminobutyric acid (GABA)], monoamines, and related metabolites were separa...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1993.tb03290.x

    authors: Vriend J,Alexiuk NA,Green-Johnson J,Ryan E

    更新日期:1993-04-01 00:00:00

  • Cystathionine accumulation in various regions of brain of DL-propargylglycine-treated rats.

    abstract::The contents of cystathionine and taurine, as well as cystathionine beta-synthase activity in various regions of the brains of normal and DL-propargylglycine-treated rats, were measured. The content of cystathionine in each region of brain increased gradually from 0.5 mg to 20 mg/200 g body weight in relation to the d...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1985.tb08744.x

    authors: Kodama H,Ikeda H,Awata S,Nakayama K

    更新日期:1985-04-01 00:00:00

  • Thiamine triphosphate and membrane-associated thiamine phosphatases in the electric organ of Electrophorus electricus.

    abstract::The main electric organ of Electrophorus electricus is particularly rich in thiamine triphosphate, which represents 87% of the total thiamine content in this tissue. The thiamine pyrophosphate concentration, however, is very low in the eel electric organ and skeletal muscle as compared with other eel or rat tissues. F...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1987.tb02891.x

    authors: Bettendorff L,Michel-Cahay C,Grandfils C,De Rycker C,Schoffeniels E

    更新日期:1987-08-01 00:00:00

  • Distribution of calcitonin gene-related peptide in rat and rabbit spinal cords: effect of intrathecal 5,7-dihydroxytryptamine.

    abstract::Calcitonin gene-related peptide-like immunoreactivity (CGRP-LI) was measured in selected regions of the cervical, thoracic, and lumbar spinal cord of untreated rabbits and, following intrathecal injection of the serotonergic neurotoxin 5,7-dihydroxytryptamine (5,7-DHT), in the thoracolumbar cord in rats using a sheep ...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1992.tb08434.x

    authors: Fone KC

    更新日期:1992-10-01 00:00:00

  • Ionic requirements for the specific binding of [3H]GBR 12783 to a site associated with the dopamine uptake carrier.

    abstract::At 0 degrees C, when Na+ was the only cation present in the incubation medium, increasing the Na+ concentration from 3 to 10 mM enhanced the affinity of [3H]1-[2-(++di-phenylmethoxy)ethyl]-4-(3-phenyl-2-propenyl)piperaz ine [( 3H]GBR 12783) for the specific binding site present in rat striatal membranes without affect...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1988.tb02979.x

    authors: Bonnet JJ,Benmansour S,Vaugeois JM,Costentin J

    更新日期:1988-03-01 00:00:00

  • Role of the polybasic sequence in the Doc2alpha C2B domain in dense-core vesicle exocytosis in PC12 cells.

    abstract::The double C2 (Doc2) family is characterized by an N-terminal Munc13-1-interacting domain and C-terminal tandem C2 domains, and it comprises three isoforms, Doc2alpha, Doc2beta, and Doc2gamma, in humans and mice. Doc2alpha, the best-characterized, brain-specific isoform, exhibits Ca(2+)-dependent phospholipid-binding ...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2010.06739.x

    authors: Sato M,Mori Y,Matsui T,Aoki R,Oya M,Yanagihara Y,Fukuda M,Tsuboi T

    更新日期:2010-07-01 00:00:00

  • SR 140333, a novel, selective, and potent nonpeptide antagonist of the NK1 tachykinin receptor: characterization on the U373MG cell line.

    abstract::The effects of a novel nonpeptide NK1 tachykinin receptor antagonist, SR 140333, on the functional consequences of NK1 receptor activation in a human astrocytoma cell line, U373MG, were investigated. Radioligand binding conducted with 125I-Bolton-Hunter substance P revealed a competitive inhibition by SR 140333 and it...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1994.62041399.x

    authors: Oury-Donat F,Lefevre IA,Thurneyssen O,Gauthier T,Bordey A,Feltz P,Emonds-Alt X,Le Fur G,Soubrie P

    更新日期:1994-04-01 00:00:00

  • The constitutive activity of melanocortin-4 receptors in cAMP pathway is allosterically modulated by zinc and copper ions.

    abstract::Melanocortin-4 receptors (MC4 R) are unique among G-protein-coupled receptors (GPCRs) as they have endogenous ligands that can exhibit inverse agonistic properties in the case of elevated basal activity. It is known that the constitutive activity of GPCRs strongly affects the ligand-dependent physiological responses, ...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/jnc.14933

    authors: Link R,Veiksina S,Tahk MJ,Laasfeld T,Paiste P,Kopanchuk S,Rinken A

    更新日期:2020-05-01 00:00:00

  • Dynorphin A(1-17) biotransformation in striatum of freely moving rats using microdialysis and matrix-assisted laser desorption/ionization mass spectrometry.

    abstract::The biotransformation of the opioid peptide dynorphin A(1-17) was investigated in striatum of freely moving Fischer rats, by direct infusion of this peptide, followed by recovery of the resulting biotransformation products via microdialysis and identification using matrix-assisted laser desorption/ionization mass spec...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2003.01859.x

    authors: Reed B,Zhang Y,Chait BT,Kreek MJ

    更新日期:2003-08-01 00:00:00

  • Growth/differentiation factor 7 is preferentially expressed in the primary motor area of the monkey neocortex.

    abstract::We applied a differential display PCR technique to isolate molecules that are area-specific in expression in the primate neocortex, and found that growth/differentiation factor 7 (GDF7), a member of the bone morphogenetic protein (BMP)/transforming growth factor (TGF) beta super-family, is preferentially expressed in ...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2001.00177.x

    authors: Watakabe A,Fujita H,Hayashi M,Yamamori T

    更新日期:2001-03-01 00:00:00

  • Glutamate activates GFAP gene promoter from cultured astrocytes through TGF-beta1 pathways.

    abstract::Glial cells are currently viewed as active partners of neurons in synapse formation. The close proximity of astrocytes to the synaptic cleft suggests that these cells might be potential targets for neuronal-released molecules although this issue has been less addressed. Here, we evaluated the role of the excitatory ne...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2008.05428.x

    authors: Romão LF,Sousa Vde O,Neto VM,Gomes FC

    更新日期:2008-07-01 00:00:00

  • Impairment of glucose and glutamate transport and induction of mitochondrial oxidative stress and dysfunction in synaptosomes by amyloid beta-peptide: role of the lipid peroxidation product 4-hydroxynonenal.

    abstract::Deposits of amyloid beta-peptide (A beta), reduced glucose uptake into brain cells, oxidative damage to cellular proteins and lipids, and excitotoxic mechanisms have all been suggested to play roles in the neurodegenerative process in Alzheimer's disease. Synapse loss is closely correlated with cognitive impairments i...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1997.69010273.x

    authors: Keller JN,Pang Z,Geddes JW,Begley JG,Germeyer A,Waeg G,Mattson MP

    更新日期:1997-07-01 00:00:00

  • Increases in cortical glutamate concentrations in transgenic amyotrophic lateral sclerosis mice are attenuated by creatine supplementation.

    abstract::Several lines of evidence implicate excitotoxic mechanisms in the pathogenesis of amyotrophic lateral sclerosis (ALS). Transgenic mice with a superoxide dismutase mutation (G93A) have been utilized as an animal model of familial ALS (FALS). We examined the cortical concentrations of glutamate using in vivo microdialys...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2001.00188.x

    authors: Andreassen OA,Jenkins BG,Dedeoglu A,Ferrante KL,Bogdanov MB,Kaddurah-Daouk R,Beal MF

    更新日期:2001-04-01 00:00:00

  • Phosphorylation of superior cervical ganglion proteins during regeneration.

    abstract::The incorporation of radioactive phosphate into proteins of both normal and regenerating ganglia of the sympathetic nervous system of the rat is reported. The incorporation reactions were carried out in vitro by incubating homogenates of excised ganglia with [gamma-32P]ATP under various conditions. It was found that i...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1989.tb07247.x

    authors: Watterson JG,Good R,Moses E,Hearn MT,Austin L

    更新日期:1989-06-01 00:00:00

  • Barium and calcium stimulate secretion from digitonin-permeabilized bovine adrenal chromaffin cells by similar pathways.

    abstract::We compared the characteristics of secretion stimulated by EGTA-buffered Ba(2+)- and Ca(2+)-containing solutions in digitonin-permeabilized bovine adrenal chromaffin cells. Half-maximal secretion occurred at approximately 100 microM Ba2+ or 1 microM Ca2+. Ba(2+)-stimulated release was not due to release of sequestered...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1992.tb09771.x

    authors: TerBush DR,Holz RW

    更新日期:1992-02-01 00:00:00

  • Molecular, pharmacological, and signaling properties of octopamine receptors from honeybee (Apis mellifera) brain.

    abstract::G protein-coupled receptors are important regulators of cellular signaling processes. Within the large family of rhodopsin-like receptors, those binding to biogenic amines form a discrete subgroup. Activation of biogenic amine receptors leads to transient changes of intracellular Ca²⁺-([Ca²⁺](i)) or 3',5'-cyclic adeno...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/jnc.12619

    authors: Balfanz S,Jordan N,Langenstück T,Breuer J,Bergmeier V,Baumann A

    更新日期:2014-04-01 00:00:00

  • A transient inhibition of mitochondrial ATP synthesis by nitric oxide synthase activation triggered apoptosis in primary cortical neurons.

    abstract::In order to investigate the relationship between nitric oxide-mediated regulation of mitochondrial function and excitotoxicity, the role of mitochondrial ATP synthesis and intracellular redox status on the mode of neuronal cell death was studied. Brief (5 min) glutamate (100 microM) receptor stimulation in primary cor...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2001.00276.x

    authors: Almeida A,Bolaños JP

    更新日期:2001-04-01 00:00:00

  • Matrix metalloproteinase-3 in the central nervous system: a look on the bright side.

    abstract::Matrix metalloproteinases (MMPs) are a large family of proteases involved in many cell-matrix and cell-cell signalling processes through activation, inactivation or release of extracellular matrix (ECM) and non-ECM molecules, such as growth factors and receptors. Uncontrolled MMP activities underlie the pathophysiolog...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章,评审

    doi:10.1111/j.1471-4159.2012.07900.x

    authors: Van Hove I,Lemmens K,Van de Velde S,Verslegers M,Moons L

    更新日期:2012-10-01 00:00:00

  • Metabolism of glycine in primary astroglial cells: synthesis of creatine, serine, and glutathione.

    abstract::The metabolism of [2-13C]glycine in astroglia-rich primary cultures obtained from brains of neonatal Wistar rats was investigated using 13C NMR spectroscopy. After a 24-h incubation of the cells in a medium containing glucose, glutamate, cysteine, and [2-13C]glycine, cell extracts and incubation media were analyzed fo...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1998.70020835.x

    authors: Dringen R,Verleysdonk S,Hamprecht B,Willker W,Leibfritz D,Brand A

    更新日期:1998-02-01 00:00:00

  • Fractalkine-induced activation of the phosphatidylinositol-3 kinase pathway attentuates microglial activation in vivo and in vitro.

    abstract::Several neurodegenerative disorders are associated with evidence of inflammation, one feature of which is increased activation of microglia, the most likely cellular source of inflammatory cytokines like interleukin-1beta. It is now recognized that interaction of microglia with other cells contributes to maintenance o...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2009.06253.x

    authors: Lyons A,Lynch AM,Downer EJ,Hanley R,O'Sullivan JB,Smith A,Lynch MA

    更新日期:2009-09-01 00:00:00

  • Bone morphogenetic protein down-regulation of neuronal pituitary adenylate cyclase-activating polypeptide and reciprocal effects on vasoactive intestinal peptide expression.

    abstract::Among bone morphogenetic proteins (BMPs), the decapentaplegic (Dpp; BMP2, BMP4) and glass bottom boat (Gbb/60A; BMP5, BMP6, BMP7) subgroups have well-described functions guiding autonomic and sensory neuronal development, fiber formation and neurophenotypic identities. Evaluation of rat superior cervical ganglia (SCG)...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2006.04293.x

    authors: Pavelock KA,Girard BM,Schutz KC,Braas KM,May V

    更新日期:2007-02-01 00:00:00

  • Cellular prion protein coupling to TACE-dependent TNF-alpha shedding controls neurotransmitter catabolism in neuronal cells.

    abstract::Despite considerable efforts to unravel the role of cellular prion protein (PrP(C)) in neuronal functions, the mechanisms by which PrP(C) takes part in the homeostasis of a defined neuronal phenotype remain poorly characterized. By taking advantage of a neuroectodermal cell line (1C11) endowed with the capacity to dif...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2009.06176.x

    authors: Pradines E,Loubet D,Mouillet-Richard S,Manivet P,Launay JM,Kellermann O,Schneider B

    更新日期:2009-08-01 00:00:00

  • Apoptosis inducing factor mediates caspase-independent 1-methyl-4-phenylpyridinium toxicity in dopaminergic cells.

    abstract::Parkinson's disease is a debilitating neurodegenerative disease characterized by loss of midbrain dopaminergic neurons. These neurons are particularly sensitive to the neurotoxin 1-methyl-4-phenylpyridinium (MPP+), the active metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), which causes parkinsonian ...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2005.03329.x

    authors: Chu CT,Zhu JH,Cao G,Signore A,Wang S,Chen J

    更新日期:2005-09-01 00:00:00

  • Glycine is taken up through GLYT1 and GLYT2 transporters into mouse spinal cord axon terminals and causes vesicular and carrier-mediated release of its proposed co-transmitter GABA.

    abstract::Glycine and GABA are likely co-transmitters in the spinal cord. Their possible interactions in presynaptic terminals have, however, not been investigated. We studied the effects of glycine on GABA release using superfused mouse spinal cord synaptosomes. Glycine concentration dependently elicited [(3)H]GABA release whi...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2001.00159.x

    authors: Raiteri L,Raiteri M,Bonanno G

    更新日期:2001-03-01 00:00:00

  • Cross-seeding of wild-type and hereditary variant-type amyloid beta-proteins in the presence of gangliosides.

    abstract::We investigated the molecular mechanism underlying the ganglioside-induced initiation of the assembly of wild and hereditary variant-type amyloid beta-proteins, including Arctic-, Dutch-, and Flemish-type amyloid beta-proteins. We monitored the assembly of amyloid beta-protein by thioflavin-T assay, western blotting a...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2005.03444.x

    authors: Yamamoto N,Matsuzaki K,Yanagisawa K

    更新日期:2005-11-01 00:00:00