MDL 72145, an enzyme-activated irreversible inhibitor with selectivity for monoamine oxidase type B.

Abstract:

:MDL 72145, (E)-2-(3',4'-dimethoxyphenyl)-3-fluoroallylamine hydrochloride, was designed and synthesised as a potential enzyme-activated irreversible inhibitor of monoamine oxidase (MAO). In vitro, the compound displayed time-dependent pseudo-first-order irreversible inhibitory characteristics with high selectivity for the B form of rat brain mitochondrial MAO. At 10 degrees C the Ki and tau 50 values for the B enzyme were 40 microM and 1.7 min, respectively, while these same kinetic constants for the A enzyme were 131 microM and 14.5 min, respectively. Selective protection against inactivation of the two forms of MAO by MDL 72145 was obtained by preincubating the enzyme with suitable concentrations of the selective A and B substrates, 5-hydroxytryptamine and benzylamine.

journal_name

J Neurochem

authors

Zreika M,McDonald IA,Bey P,Palfreyman MG

doi

10.1111/j.1471-4159.1984.tb00920.x

subject

Has Abstract

pub_date

1984-08-01 00:00:00

pages

448-54

issue

2

eissn

0022-3042

issn

1471-4159

journal_volume

43

pub_type

杂志文章
  • The α1 subunit of nicotinic acetylcholine receptors in the inner ear: transcriptional regulation by ATOH1 and co-expression with the γ subunit in hair cells.

    abstract::Acetylcholine is a key neurotransmitter of the inner ear efferent system. In this study, we identify two novel nAChR subunits in the inner ear: α1 and γ, encoded by Chrna1 and Chrng, respectively. In situ hybridization shows that the messages of these two subunits are present in vestibular and cochlear hair cells duri...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2007.04980.x

    authors: Scheffer D,Sage C,Plazas PV,Huang M,Wedemeyer C,Zhang DS,Chen ZY,Elgoyhen AB,Corey DP,Pingault V

    更新日期:2007-12-01 00:00:00

  • The discoidin domain receptor 1 gene has a functional A2RE sequence.

    abstract::Discoidin domain receptor 1 (DDR1) is expressed in myelin oligodendrocytes and co-localizes with myelin basic protein (MBP). Alternative splicing of DDR1 generates five isoforms designated DDR1a-e. The MBP mRNA contains an hnRNP A2 response element (A2RE) sequence that is recognized by heterogeneous nuclear ribonucleo...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2011.07580.x

    authors: Roig B,Moyano S,Martorell L,Costas J,Vilella E

    更新日期:2012-02-01 00:00:00

  • ET(A) and ET(B) specific ligands synergistically antagonize endothelin-1 binding to an atypical endothelin receptor in primary rat astrocytes.

    abstract::Using a whole-cell binding procedure with long incubations at low temperature and subsequent acid stripping, we have characterized an atypical endothelin (ET) receptor in primary rat cortical astrocyte cultures. We found the following: (a) no competition for 125I-ET-1 binding by the ET(A) antagonists BQ-123 and LU 135...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1998.70020473.x

    authors: Jensen N,Hasselblatt M,Sirén AL,Schilling L,Schmidt M,Ehrenreich H

    更新日期:1998-02-01 00:00:00

  • Pre- and early postnatal enriched environmental experiences prevent neonatal hypoxia-ischemia late neurodegeneration via metabolic and neuroplastic mechanisms.

    abstract::Prenatal and early postnatal periods are important for brain development and neural function. Neonatal insults such as hypoxia-ischemia (HI) causes prolonged neural and metabolic dysregulation, affecting central nervous system maturation. There is evidence that brain hypometabolism could increase the risk of adult-ons...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/jnc.15221

    authors: Durán-Carabali LE,Kawa Odorcyk F,Greggio S,Teribele Venturin G,Farias Sanches E,Garcia Schu G,Soares Carvalho A,Avila Pedroso T,de Sá Couto-Pereira N,Costa da Costa J,Dalmaz C,Rigon Zimmer E,Netto CA

    更新日期:2020-10-23 00:00:00

  • Manipulation of disulfide bonds differentially affects the intracellular transport, sorting, and processing of neuroendocrine secretory proteins.

    abstract::To investigate if the prevention of disulfide bond formation affects the intracellular transport, sorting, and processing of a distinct set of neuroendocrine proteins in the regulated secretory pathway, we have treated Xenopus intermediate pituitaries with the thiol-reducing agent dithiothreitol. Pulse-chase incubatio...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1998.71010402.x

    authors: Van Horssen AM,Van Kuppeveld FJ,Martens GJ

    更新日期:1998-07-01 00:00:00

  • Complex carbohydrate composition of large dense-cored vesicles from sympathetic nerve.

    abstract::Highly purified noradrenergic, large, dense-cored vesicles were isolated from bovine sympathetic nerve endings by sucrose-D2O density gradient centrifugation. Their concentration of glycoprotein hexosamine and sialic acid was 6.6 and 3.9 mumol/100 mg lipid-free dry weight, respectively, values which are similar to tho...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1987.tb02445.x

    authors: Margolis RU,Ledeen RW,Sbaschnig-Agler M,Byrne MC,Klein RL,Douglas BH 2nd,Margolis RK

    更新日期:1987-12-01 00:00:00

  • Nicotinic modulation of [3H]dopamine release from striatal synaptosomes: pharmacological characterisation.

    abstract::Presynaptic nicotinic acetylcholine receptors on striatal nerve terminals modulate the release of dopamine. We have compared the effects of a number of nicotinic agonists and antagonists on a perfused synaptosome preparation preloaded with [3H]dopamine. (-)-Nicotine, acetylcholine, and the nicotinic agonists cytisine ...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1990.tb02341.x

    authors: Rapier C,Lunt GG,Wonnacott S

    更新日期:1990-03-01 00:00:00

  • Microtubule depolymerization inhibits ethanol-induced enhancement of GABAA responses in stably transfected cells.

    abstract::We studied whether microtubule organization is important for actions of ethanol on GABAA ergic responses by testing the effects of microtubule depolymerization on ethanol enhancement of GABA action in mouse L(tk-) cells stably transfected with GABAA receptor alpha 1 beta 1 gamma 2L subunits. The microtubule-disrupting...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1996.66031318.x

    authors: Whatley VJ,Brozowski SJ,Hadingham KL,Whiting PJ,Harris RA

    更新日期:1996-03-01 00:00:00

  • Pivotal roles of alpha-melanocyte-stimulating hormone and the melanocortin 4 receptor in leptin stimulation of prolactin secretion in rats.

    abstract::Leptin, the obese gene product, was reported to stimulate prolactin (PRL) secretion, but the neuroendocrine mechanism underlying this hormonal response is largely unknown. Thus, in this study we examined the involvement of several important PRL regulators in the leptin-induced PRL secretion in male rats. Compared with...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2003.01683.x

    authors: Watanobe H,Schiöth HB,Izumi J

    更新日期:2003-04-01 00:00:00

  • Human amylin induces "apoptotic" pattern of gene expression concomitant with cortical neuronal apoptosis.

    abstract::Amylin forms large beta-pleated neurotoxic oligomers but shows only 38% sequence similarity to A beta. As patterns of gene expression during neuronal apoptosis appear stimulus and cell type specific, we compared the pattern of amylin-induced gene expression in rat cortical neurons with that shown previously to be indu...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1998.71020506.x

    authors: Tucker HM,Rydel RE,Wright S,Estus S

    更新日期:1998-08-01 00:00:00

  • Epigenetic control of early neurodegenerative events in diabetic retinopathy by the histone deacetylase SIRT6.

    abstract::Diabetic retinopathy (DR) is one of the common complications associated with diabetes mellitus and the leading cause of blindness worldwide. Recent research has demonstrated that DR is not only a microvascular disease but may be a result of neurodegenerative processes. Moreover, glucose-induced neuron and glial cell d...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/jnc.14243

    authors: Zorrilla-Zubilete MA,Yeste A,Quintana FJ,Toiber D,Mostoslavsky R,Silberman DM

    更新日期:2018-01-01 00:00:00

  • Characterization of mature rat oligodendrocytes: a proteomic approach.

    abstract::Oligodendrocytes are glial cells responsible for the synthesis and maintenance of myelin in the central nervous system (CNS). Oligodendrocytes are vulnerable to damage occurring in a variety of neurological diseases. Understanding oligodendrocyte biology is crucial for the dissemination of de- and remyelination mechan...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2007.04575.x

    authors: Dumont D,Noben JP,Moreels M,Vanderlocht J,Hellings N,Vandenabeele F,Lambrichts I,Stinissen P,Robben J

    更新日期:2007-07-01 00:00:00

  • A UDP-sugar pyrophosphatase is developmentally regulated in the rat retina.

    abstract::Rat retina tissue contains relatively high amounts of GD3 in relation to ganglio-series gangliosides even in the adult stages. This was attributed in part to an activity ratio between the enzyme that converts GM3 to GD3 [sialytransferase II (ST-II)] and the enzyme that converts GM3 to GM2 [N-acetylgalactosaminyltransf...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1995.64031274.x

    authors: Martina JA,Daniotti JL,Maccioni HJ

    更新日期:1995-03-01 00:00:00

  • The role of MAC1 in diesel exhaust particle-induced microglial activation and loss of dopaminergic neuron function.

    abstract::Increasing reports support that air pollution causes neuroinflammation and is linked to central nervous system (CNS) disease/damage. Diesel exhaust particles (DEP) are a major component of urban air pollution, which has been linked to microglial activation and Parkinson's disease-like pathology. To begin to address ho...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/jnc.12231

    authors: Levesque S,Taetzsch T,Lull ME,Johnson JA,McGraw C,Block ML

    更新日期:2013-06-01 00:00:00

  • Characterization of two chromaffin cell populations isolated from bovine adrenal medulla.

    abstract::Cultures of chromaffin cells isolated from the bovine adrenal medulla have been extremely useful for investigating secretory mechanisms, but such cultures used up to the present time represent mixed populations of adrenergic and noradrenergic cells. This report describes how, with slight modifications to standard proc...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1991.tb03761.x

    authors: Moro MA,Garcia AG,Langley OK

    更新日期:1991-08-01 00:00:00

  • Involvement of the AT1 receptor subtype in the effects of angiotensin IV and LVV-haemorphin 7 on hippocampal neurotransmitter levels and spatial working memory.

    abstract::Intracerebroventricular (i.c.v.) administration of angiotensin IV (Ang IV) or Leu-Val-Val-haemorphin 7 (LVV-H7) improves memory performance in normal rats and reverses memory deficits in rat models for cognitive impairment. These memory effects were believed to be mediated via the putative 'AT4 receptor'. However, thi...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2009.06547.x

    authors: De Bundel D,Demaegdt H,Lahoutte T,Caveliers V,Kersemans K,Ceulemans AG,Vauquelin G,Clinckers R,Vanderheyden P,Michotte Y,Smolders I

    更新日期:2010-03-01 00:00:00

  • GM3 alpha2,8-sialyltransferase (GD3 synthase): protein characterization and sub-golgi location in CHO-K1 cells.

    abstract::GD3 synthase (Sial-T2) is a key enzyme of ganglioside synthesis that, in concert with GM2 synthase (GalNAc-T), regulates the ratio of a- and b-pathway gangliosides. In this work, we study the sub-Golgi location of an epitope-tagged version of chicken Sial-T2 transfected to CHO-K1 cells. The expressed protein was enzym...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2000.0741711.x

    authors: Daniotti JL,Martina JA,Giraudo CG,Zurita AR,Maccioni HJ

    更新日期:2000-04-01 00:00:00

  • Phorbol ester-induced upregulation of angiotensin II receptors in neuronal cultures is potentiated by a calcium ionophore.

    abstract::Previous studies have suggested that protein kinase C is important in the regulation of angiotensin II receptors in neuronal cultures, because the C-kinase agonists, phorbol esters, are able to increase the number of these receptors. In the present study, we have further investigated the role of protein kinase C in an...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1988.tb04849.x

    authors: Sumners C,Rueth SM,Myers LM,Kalberg CJ,Crews FT,Raizada MK

    更新日期:1988-07-01 00:00:00

  • Amyloid Abeta1-40 preconditions non-apoptotic signals in vivo and protects fetal rat brain from intrauterine ischemic stress.

    abstract::Abstract The dualistic activities of the amyloid beta (Abeta) peptide as a pro-oxidant and ubiquitous constituent of amyloid deposits in Alzheimer's disease plaques and as an antioxidant of purported physiological function has been suggested but the mechanisms are far from being understood. In this report we measure s...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2004.02778.x

    authors: Kuperstein F,Brand A,Yavin E

    更新日期:2004-11-01 00:00:00

  • Regulatory effects of D2 receptors in the ventral tegmental area on the mesocorticolimbic dopaminergic pathway.

    abstract::To investigate the regulatory effects of somatodendritic D2 receptors on the terminal's extracellular dopamine (DA) concentration, a D2 antagonist (eticlopride) was infused directly into the ventral tegmental area via a microdialysis probe in chloral hydrate-anesthetized rats. Extracellular DA changes in both the nucl...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.2000.0742576.x

    authors: Chen NN,Pan WH

    更新日期:2000-06-01 00:00:00

  • In vivo production and release of acetylcholine from primary fibroblasts genetically modified to express choline acetyltransferase.

    abstract::Primary rat fibroblasts genetically modified to express Drosophila choline acetyltransferase (dChAT) synthesize and release acetylcholine (ACh) in vitro. The ACh produced from the transduced fibroblasts was found to be enhanced by increasing amounts of choline chloride in the culture media. These dChAT-expressing cell...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1993.tb13625.x

    authors: Fisher LJ,Schinstine M,Salvaterra P,Dekker AJ,Thal L,Gage FH

    更新日期:1993-10-01 00:00:00

  • Adult neurogenesis and its role in brain injury and psychiatric diseases.

    abstract::In the adult mammalian brain, neural stem cells (NSCs) reside in two neurogenic regions, the walls of the lateral ventricles, and the subgranular zone of the hippocampus, which generate new neurons for the olfactory bulb and dentate gyrus, respectively. These adult NSCs retain their self-renewal ability and capacity t...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章,评审

    doi:10.1111/jnc.14557

    authors: Hayashi Y,Jinnou H,Sawamoto K,Hitoshi S

    更新日期:2018-12-01 00:00:00

  • Direct and continuous detection of ATP secretion from primary monolayer cultures of bovine adrenal chromaffin cells.

    abstract::A method was developed for direct and continuous detection of secretion of ATP from primary monolayer cultures of bovine adrenal chromaffin cells. ATP, which is costored with catecholamines within adrenal chromaffin cells, was released into the incubation medium, where it reacted with firefly luciferin-luciferase prod...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1987.tb10019.x

    authors: White TD,Bourke JE,Livett BG

    更新日期:1987-10-01 00:00:00

  • L-3,4-dihydroxyphenylalanine-induced dopamine release in the striatum of intact and 6-hydroxydopamine-treated rats: differential effects of monoamine oxidase A and B inhibitors.

    abstract::Administration of L-DOPA (50 mg/kg) elicits a significant increase in extracellular dopamine in striata of rats treated with the catecholaminergic neurotoxin 6-hydroxydopamine but not in striata of intact rats. To assess the role of dopaminergic nerve terminals in determining the effects of exogenous L-DOPA on extrace...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1046/j.1471-4159.1994.63010108.x

    authors: Wachtel SR,Abercrombie ED

    更新日期:1994-07-01 00:00:00

  • The non-peptidic δ-opioid receptor agonist Tan-67 mediates neuroprotection post-ischemically and is associated with altered amyloid precursor protein expression, maturation and processing in mice.

    abstract::Tan-67 is a selective non-peptidic δ-opioid receptor (DOR) agonist that confers neuroprotection against cerebral ischemia/reperfusion (I/R)-caused neuronal injury in pre-treated animals. In this study, we examined whether post-ischemic administration of Tan-67 in stroke mice is also neuroprotective and whether the tre...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/jnc.14265

    authors: Min JW,Liu Y,Wang D,Qiao F,Wang H

    更新日期:2018-02-01 00:00:00

  • Chemical compositions of brain and myelin in two patients with multiple sulphatase deficiency (a variant form of metachromatic leukodystrophy).

    abstract::The lipid composition of the brain, including myelin, was studied in detail in two cases with a variant form of metachromatic leukodystrophy (multiple sulphatase deficiency type). In the white matter, the sulphatide concentration was 3-4 times higher than the normal level in both cases. There was a significant accumul...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1976.tb00310.x

    authors: Eto Y,Meier C,Herschkowitz NN

    更新日期:1976-11-01 00:00:00

  • Cellular distribution of gangliosides in the developing mouse cerebellum: analysis using the staggerer mutant.

    abstract::The distribution of cerebellar gangliosides was studied in staggerer (sg/sg) mutant mice, where the majority of granule cells die after completing their migration across the molecular layer. In addition, the external granule cell layer in sg/sg mice persists longer than in normal mice. Moreover, in the sg/sg cerebellu...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1984.tb12856.x

    authors: Seyfried TN,Bernard DJ,Yu RK

    更新日期:1984-10-01 00:00:00

  • Activation of the extracellular signal-regulated kinase pathway contributes to the behavioral deficit of fragile x-syndrome.

    abstract::Fragile X syndrome (FXS) is a developmental disorder caused by the loss of Fragile X Mental Retardation 1 (FMR1) gene function because of a CGG repeat expansion (> 200 repeats) in the gene. The molecular mechanism(s) linking loss of FMR1 function to the molecular pathology and cognitive/behavioral disability remain un...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.2012.07722.x

    authors: Wang X,Snape M,Klann E,Stone JG,Singh A,Petersen RB,Castellani RJ,Casadesus G,Smith MA,Zhu X

    更新日期:2012-05-01 00:00:00

  • Kinetic effects of terbium ions on muscarinic acetylcholine receptors of murine neuroblastoma cells.

    abstract::Preincubation of murine neuroblastoma cells (clone N1E-115) with terbium chloride resulted in a significant potentiation of carbachol-mediated increase in cyclic GMP formation. This effect was accompanied by a shift of the peak response from 30 s to 120 s and a 6-fold decrease in carbachol concentration producing half...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1984.tb02760.x

    authors: El-Fakahany EE,Pfenning M,Richelson E

    更新日期:1984-03-01 00:00:00

  • Iron deficiency alters discrete proteins in rat caudate nucleus and nucleus accumbens.

    abstract::Young rats (21 days old) made nutritionally iron deficient, by feeding them a semisynthetic diet containing skimmed milk for 5 weeks, had significantly lowered hemoglobin levels (5.2 +/- 4 g/100 ml). The nonheme iron content in caudate nucleus was decreased by 47%. The behavioral response of iron-deficient rats to apo...

    journal_title:Journal of neurochemistry

    pub_type: 杂志文章

    doi:10.1111/j.1471-4159.1986.tb00681.x

    authors: Youdim MB,Sills MA,Heydorn WE,Creed GJ,Jacobowitz DM

    更新日期:1986-09-01 00:00:00