当前位置： SCI文献检索 > NEUROPHARMACOLOGY期刊下所有文献 > Use of an inverse agonist radioligand [3H]A-317920 reveals distinct pharmacological profiles of the rat histamine H3 receptor.

Use of an inverse agonist radioligand [3H]A-317920 reveals distinct pharmacological profiles of the rat histamine H3 receptor.

Abstract：

:Selective radioligands for histamine H(3) receptors have been used to characterize H(3) receptor pharmacology by radioligand binding assays and to determine H(3) receptor distribution by tissue autoradiography. Here we report the synthesis and receptor binding characterization of [(3)H]A-317920 (furan-2-carboxylic acid(2-[4-[3-([3,5-(3)H]4-cyclopropanecarbonyl-phenoxy)-propyl]-piperazin-1-yl]-1-methyl-2-oxo-ethyl)-amide), a high affinity inverse agonist radioligand for the rat H(3) receptor. The binding of [(3)H]A-317920 to rat cortical and cloned H(3) receptors revealed fast on- and slower off-rate kinetics with calculated K(d) values in agreement with those determined in saturation binding assays (0.2 nM for both receptors). Further, we compared [(3)H]A-317920 with the agonist [(3)H](N)-alpha-methylhistamine ([(3)H]NalphaMH) as radioligand tools to study receptor pharmacology. Agonists and antagonists displaced [(3)H]NalphaMH with one-site binding characteristics and Hill slopes approached unity. In contrast, although antagonists exhibited one-site binding, [(3)H]A-317920 displacement by agonists was best fit by two-site binding models, and the potencies of the high affinity, GDP-sensitive sites correlated with the potencies defined in [(3)H]NalphaMH binding. Unlike [(125)I]iodoproxyfan, [(3)H]A-317920 exhibits potent and selective binding to rat H(3) receptors with low binding to non-H(3) sites, including cytochrome P450. These findings show that [(3)H]A-317920 is a potent rat H(3) receptor antagonist radioligand and has utility for studying H(3) receptor pharmacology.

journal_name

Neuropharmacology

journal_title

Neuropharmacology

authors

Yao BB,Witte DG,Miller TR,Carr TL,Kang CH,Cassar S,Faghih R,Bennani YL,Surber BW,Hancock AA,Esbenshade TA

doi

10.1016/j.neuropharm.2005.10.008

subject

Has Abstract

pub_date

2006-03-01 00:00:00

pages

468-78

issue

4

eissn

0028-3908

issn

1873-7064

pii

S0028-3908(05)00369-2

journal_volume

50

pub_type

杂志文章

相关文献

NEUROPHARMACOLOGY文献大全
  • The alpha7 nicotinic acetylcholine receptor subtype mediates nicotine protection against NMDA excitotoxicity in primary hippocampal cultures through a Ca(2+) dependent mechanism.

    abstract：:Neuronal nicotinic acetylcholine receptors (nAChR) have been suggested to play a role in a variety of modulatory and regulatory processes, including neuroprotection. Here we have characterized the neuroprotective effects of nicotine against an excitotoxic insult in primary hippocampal cultures. Exposure of hippocampal...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(00)00127-1

    authors： Dajas-Bailador FA,Lima PA,Wonnacott S

    更新日期：2000-10-01 00:00:00

  • Histamine and histamine receptors in Tourette syndrome and other neuropsychiatric conditions.

    abstract：:The potential contributions of dysregulation of the brain's histaminergic modulatory system to neuropsychiatric disease, and the potential of histamine-targeting medications as therapeutic agents, are gradually coming into focus. The H3R receptor, which is expressed primarily in the central nervous system, is a promis...

    journal_title：Neuropharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.neuropharm.2015.08.019

    authors： Rapanelli M,Pittenger C

    更新日期：2016-07-01 00:00:00

  • Toll-like receptor signalling as a cannabinoid target in Multiple Sclerosis.

    abstract：:Toll-like receptors (TLRs) are the sensors of pathogen-associated molecules that trigger tailored innate immune intracellular signalling responses to initiate innate immune reactions. Data from the experimental autoimmune encephalomyelitis (EAE) model indicates that TLR signalling machinery is a pivotal player in the ...

    journal_title：Neuropharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.neuropharm.2016.04.009

    authors： Fitzpatrick JK,Downer EJ

    更新日期：2017-02-01 00:00:00

  • Ultrasonic vocalizations as a tool in studying emotional states in rodent models of social behavior and brain disease.

    abstract：:Rodents emit ultrasonic vocalizations (USVs) to communicate the presence of positive or negative emotional states and to coordinate social interactions. On this basis, USVs are increasingly being used as a behavioral readout in rodent studies of affect, motivation and social behavior. Notably, several investigations h...

    journal_title：Neuropharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.neuropharm.2018.11.008

    authors： Simola N,Granon S

    更新日期：2019-11-15 00:00:00

  • Fluoride-stimulated adenylate cyclase activity in rat brain following chronic treatment with psychotropic drugs.

    abstract：:Chronic treatment with imipramine and reserpine increased fluoride-stimulated activity of adenylate cyclase in homogenates of cerebral cortex and "limbic" forebrain of the rat. Concomitant treatment with lithium counteracted this effect, while lithium alone had no effect on the activity of adenylate cyclase. ...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/0028-3908(84)90253-3

    authors： Andersen PH,Klysner R,Geisler A

    更新日期：1984-04-01 00:00:00

  • Neuroprotective activity of the potent and selective mGlu1a metabotropic glutamate receptor antagonist, (+)-2-methyl-4 carboxyphenylglycine (LY367385): comparison with LY357366, a broader spectrum antagonist with equal affinity for mGlu1a and mGlu5 recept

    abstract：:(+)-2-Methyl-4-carboxyphenylglycine (LY367385), a potent and selective antagonist of mGlu1a metabotropic glutamate receptors, was neuroprotective in the following in vitro and in vivo models of excitotoxic death: (i) mixed cultures of murine cortical cells transiently exposed to N-methyl-D-aspartate (NMDA); (ii) rats ...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(98)00159-2

    authors： Bruno V,Battaglia G,Kingston A,O'Neill MJ,Catania MV,Di Grezia R,Nicoletti F

    更新日期：1999-02-01 00:00:00

  • Effect of desipramine, phenoxybenzamine and yohimbine on beta-adrenoceptors and cyclic AMP production in the rat brain.

    abstract：:In rat brain, the number of beta-adrenoceptors and activity of noradrenaline-dependent adenylate cyclase were examined after treatment with desipramine (7.5 mg kg-1 day-1) for three days alone or in combination with the alpha 2-adrenoceptor antagonist, yohimbine (2 mg kg-1 12 hr-1), or with phenoxybenzamine (7.5 mg kg...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/0028-3908(84)90077-7

    authors： Campbell IC,McKernan RM,Smokcum RW,Stephenson JD,Weeramanthri TB

    更新日期：1984-12-01 00:00:00

  • In vivo assessment of release and metabolism of dopamine in the ventrolateral striatum of awake rats following administration of dopamine D1 and D2 receptor agonists and antagonists.

    abstract：:The ability of specific dopamine (DA) receptor agonists and antagonists to modify the release and metabolism of DA in the ventrolateral striatum of awake rats was assessed using in vivo microdialysis. The specific DA D2 receptor antagonist, raclopride (0.1, 0.5 and 2.0 mg/kg, i.p.), dose-dependently increased release ...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/0028-3908(91)90022-4

    authors： See RE,Sorg BA,Chapman MA,Kalivas PW

    更新日期：1991-12-01 00:00:00

  • Fractional occupancy of synaptic binding sites and the molecular plasticity of inhibitory synapses.

    abstract：:The postsynaptic density (PSD) at inhibitory synapses is a complex molecular assembly that serves as a platform for the interaction of neurotransmitter receptors, scaffold and adapter proteins, cytoskeletal elements and signalling molecules. The stability of the PSD depends on a multiplicity of interactions linking in...

    journal_title：Neuropharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.neuropharm.2019.01.008

    authors： Specht CG

    更新日期：2020-06-01 00:00:00

  • Reduction of the amplitude of preovulatory LH and FSH surges and of the amplitude of the in vitro GnRH-induced LH release by substance P. Reversal of the effect by RP 67580.

    abstract：:The effects of Substance P (SP) and of a specific nonpeptide antagonist of the NK1 receptor (RP 67580) on preovulatory gonadotropin surges and on the in vitro GnRH induced LH surge were investigated in cycling female rats. A subcutaneous injection of SP (0.5 mg/kg body weight) at 12.00 h on the proestrous day signific...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(96)00124-4

    authors： Duval P,Lenoir V,Garret C,Kerdelhue B

    更新日期：1996-01-01 00:00:00

  • Serotonin depletion in the dorsal and ventral hippocampus: effects on locomotor hyperactivity, prepulse inhibition and learning and memory.

    abstract：:We present an overview of our studies on the differential role of serotonergic projections from the median raphe nucleus (MRN) and dorsal raphe nucleus (DRN) in behavioural animal models with relevance to schizophrenia. Stereotaxic microinjection of the serotonin neurotoxin 5,7-dihydroxytryptamine (5,7-DHT) into the M...

    journal_title：Neuropharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.neuropharm.2008.06.035

    authors： Adams W,Kusljic S,van den Buuse M

    更新日期：2008-11-01 00:00:00

  • Effects of nimodipine on extracellular dopamine levels in the rat nucleus accumbens in ethanol withdrawal.

    abstract：:Withdrawal from chronic ethanol intoxication is associated with a reduction of dopamine neurotransmission. However, the mechanisms of dopamine depletion, a putative neurochemical correlate of the dysphoric symptomatology, are not yet understood. To assess the role of L-type calcium channels in the inhibition of the do...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(99)00039-8

    authors： Rossetti ZL,Isola D,De Vry J,Fadda F

    更新日期：1999-09-01 00:00:00

  • KCC2 membrane diffusion tunes neuronal chloride homeostasis.

    abstract：:Neuronal Cl- homeostasis is regulated by the activity of two cation chloride co-transporters (CCCs), the K+-Cl- cotransporter KCC2 and the Na+-K+-Cl- cotransporter NKCC1, which are primarily extruding and importing chloride in neurons, respectively. Several neurological and psychiatric disorders including epilepsy, ne...

    journal_title：Neuropharmacology

    pub_type： 杂志文章,评审

    doi：10.1016/j.neuropharm.2019.03.014

    authors： Côme E,Marques X,Poncer JC,Lévi S

    更新日期：2020-06-01 00:00:00

  • Spontaneous activity, singly bound states and the impact of alpha1Phe64 mutation on GABAAR gating in the novel kinetic model based on the single-channel recordings.

    abstract：:GABAA receptor is the primary mediator of inhibition in the adult mammalian brain. Our recent studies revealed that a classic gating scheme for GABAAR needed to be updated with an intermediate step (flipping) and that the α1Phe64 mutation at the GABA binding site affects this transition. However, description of flippi...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/j.neuropharm.2017.11.030

    authors： Kisiel M,Jatczak M,Brodzki M,Mozrzymas JW

    更新日期：2018-03-15 00:00:00

  • GABAergic drugs, morphine and morphine tolerance: a study in relation to nociception and gastrointestinal transit in mice.

    abstract：:Agonists and antagonists of gamma-aminobutyric acid, i.e. GABAergic drugs, such as muscimol, baclofen or bicuculline, alone or in combination, exhibited analgesic effects per se and enhanced the analgesia induced by morphine. The analgesic effects of GABAergic drugs were unaffected by administration of naloxone in a d...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/0028-3908(83)90101-6

    authors： Sivam SP,Ho IK

    更新日期：1983-06-01 00:00:00

  • Oxytocin and a C-terminal derivative (Z-prolyl-D-leucine) attenuate tolerance to and dependence on morphine and interact with dopaminergic neurotransmission in the mouse brain.

    abstract：:The effects of oxytocin (OXT) and of dipeptides derived from the C-terminal portion of oxytocin (Z-prolyl-leucine and Z-prolyl-D-leucine) on the development of acute and chronic tolerance to, and dependence on morphine were tested in the mouse. Oxytocin and the dipeptides attenuated the development of acute and chroni...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/0028-3908(85)90026-7

    authors： Kovács GL,Horváth Z,Sarnyai Z,Faludi M,Telegdy G

    更新日期：1985-05-01 00:00:00

  • Role of sensory deficits in motor impairments after injury to primary motor cortex.

    abstract：:After a focal ischemic lesion in the hand representation of the primary motor cortex in squirrel monkeys, manual skill was mildly and transiently impaired on a reach-and-retrieval task. Performance was significantly poorer during weeks 1 and 3 post-lesion, but was normal by week 4. An unusual behavioral event was also...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(99)00254-3

    authors： Nudo RJ,Friel KM,Delia SW

    更新日期：2000-03-03 00:00:00

  • Behavioral syndrome induced by allylnitrile, crotononitrile or 2-pentenenitrile in rats.

    abstract：:A single oral administration of allylnitrile, crotononitrile or 2-pentenenitrile in rats induced behavioral abnormalities, such as head-twitching, head weaving, hindlimb abduction, backward pedaling and pivoting. The head-twitching, which was most consistently observed, was suppressed by serotonin (5-HT) antagonists, ...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/0028-3908(91)90123-s

    authors： Tanii H,Hayashi M,Hashimoto K

    更新日期：1991-08-01 00:00:00

  • Modulation of neurotransmitter release by P2X and P2Y receptors in the rat spinal cord.

    abstract：:In this study, the P2 receptor-mediated modulation of [3H]glutamate and [3H]noradrenaline release were examined in rat spinal cord slices. Adenosine 5'-triphosphate (ATP), adenosine 5'-diphosphate (ADP), and 2-methylthioadenosine 5'-diphosphate (2-MeSADP) decreased the electrical stimulation-evoked [3H]glutamate efflu...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/j.neuropharm.2007.10.013

    authors： Heinrich A,Kittel A,Csölle C,Sylvester Vizi E,Sperlágh B

    更新日期：2008-02-01 00:00:00

  • Alpha6-containing nicotinic acetylcholine receptor is a highly sensitive target of alcohol.

    abstract：:Alcohol use disorder (AUD) is a serious public health problem that results in tremendous social, legal and medical costs to society. Unlike other addictive drugs, there is no specific molecular target for ethanol (EtOH). Here, we report a novel molecular target that mediates EtOH effects at concentrations below those ...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/j.neuropharm.2019.01.021

    authors： Gao F,Chen D,Ma X,Sudweeks S,Yorgason JT,Gao M,Turner D,Eaton JB,McIntosh JM,Lukas RJ,Whiteaker P,Chang Y,Steffensen SC,Wu J

    更新日期：2019-05-01 00:00:00

  • Sex differences in corticotropin releasing factor peptide regulation of inhibitory control and excitability in central amygdala corticotropin releasing factor receptor 1-neurons.

    abstract：:The central amygdala (CeA) is a critical regulator of emotional behavior that has been implicated in psychiatric illnesses, including anxiety disorders and addiction. The CeA corticotropin releasing factor receptor 1 (CRF1) system has been implicated in alcohol use disorder (AUD) and mood disorders, and has been shown...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/j.neuropharm.2020.108296

    authors： Agoglia AE,Tella J,Herman MA

    更新日期：2020-12-01 00:00:00

  • The metabotropic glutamate receptor 5 radioligand [11C]AZD9272 identifies unique binding sites in primate brain.

    abstract：:The metabotropic glutamate receptor 5 (mGluR5) is a target for drug development and for imaging studies of the glutamate system in neurological and psychiatric disorders. [11C]AZD9272 is a selective mGluR5 PET radioligand that is structurally different from hitherto applied mGluR5 radioligands. In the present investig...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/j.neuropharm.2018.03.039

    authors： Varnäs K,Juréus A,Finnema SJ,Johnström P,Raboisson P,Amini N,Takano A,Stepanov V,Halldin C,Farde L

    更新日期：2018-06-01 00:00:00

  • The effects of tetraethylammonium during twitch and tetanic stimulation of the phrenic nerve diaphragm preparation in the rat.

    abstract：:Tetraethylammonium (TEA) (2.6 x 10(-3) M) potentiated the twitches of the indirectly- or directly-stimulated phrenic nerve diaphragm of the rat at 37 degrees C by prolonging the action potential of the sarcolemma, due to an inhibition of the repolarizing K+ current. With indirect stimulation, TEA caused a use-dependen...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/0028-3908(89)90137-8

    authors： Røed A

    更新日期：1989-06-01 00:00:00

  • P2 receptor modulation and cytotoxic function in cultured CNS neurons.

    abstract：:In this study we investigate the presence, modulation and biological function of P2 receptors and extracellular ATP in cultured cerebellar granule neurons. As we demonstrate by RT-PCR and western blotting, both P2X and P2Y receptor subtypes are expressed and furthermore regulated as a function of neuronal maturation. ...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(01)00197-6

    authors： Amadio S,D'Ambrosi N,Cavaliere F,Murra B,Sancesario G,Bernardi G,Burnstock G,Volonté C

    更新日期：2002-03-01 00:00:00

  • Inhibition of catechol-O-methyltransferase in the cynomolgus monkey by opicapone after acute and repeated administration.

    abstract：INTRODUCTION:The aim of the study was to clarify the dose response for inhibition of catechol-O-methyltransferase (COMT) by opicapone, a third generation COMT inhibitor, after acute and repeated administration to the cynomolgus monkey with pharmacokinetic evaluation at the higher dose. METHODS:Three cynomolgus monkeys...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/j.neuropharm.2018.10.001

    authors： Kitajima T,Mizote S,Bonifácio MJ,Umemura T,Yoneda K,Moser P,Soares-da-Silva P,Tanaka M

    更新日期：2018-12-01 00:00:00

  • Morphine conditioned reward is inhibited by MPEP, the mGluR5 antagonist.

    abstract：:In the present study we examined the effect of MPEP [2-methyl-6-(phenylethynyl)-pyridine] a potent, selective and systemically active metabotropic glutamate receptor (mGluR) type I (subtype mGluR5) antagonist on conditioned morphine reward in mice. In an unbiased version of conditioned place preference (CPP) paradigm,...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(02)00309-x

    authors： Popik P,Wróbel M

    更新日期：2002-12-01 00:00:00

  • Electrophysiological characterisation of the human N-type Ca2+ channel II: activation and inactivation by physiological patterns of activity.

    abstract：:In a cell line (C2D7) stably expressing the human N-type calcium channel encoded by the subunits alpha1B-a, beta1b, alpha2bdelta, we have analysed the Ca2+ currents produced by a range of action potential-like voltage protocols (APVPs). Such protocols consistently produced robust inward currents that could be eliminat...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(97)00153-6

    authors： McNaughton NC,Bleakman D,Randall AD

    更新日期：1998-01-01 00:00:00

  • Cerebrospinal fluid diazepam binding inhibitor in depressed patients and normal controls.

    abstract：:Diazepam binding inhibitor (DBI) is a neuromodulatory peptide for gamma-aminobutyric acid (GABA) neurotransmission. Levels of DBI in cerebrospinal fluid (CSF) were found to be elevated in depressed patients, when compared to age- and sex-matched normal controls. Levels of the peptide, corticotropin-releasing hormone (...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/s0028-3908(11)80014-6

    authors： Roy A

    更新日期：1991-12-01 00:00:00

  • Serotonin turnover rate, [3H]paroxetine binding sites, and 5-HT1A receptors in the hippocampus of rats subchronically treated with clonazepam.

    abstract：:Selective central benzodiazepine agonists, such as clonazepam, are known to modify serotonin and 5-hydroxyindoleacetic content in the brain. In order to further study the effect of this benzodiazepine on serotonin turnover rate, rats received clonazepam, 10 mg/kg for 10 days, and the concentrations of serotonin and 5-...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/0028-3908(95)00103-d

    authors： Lima L,Trejo E,Urbina M

    更新日期：1995-10-01 00:00:00

  • Contrasting sex-dependent adaptations to synaptic physiology and membrane properties of prefrontal cortex interneuron subtypes in a mouse model of binge drinking.

    abstract：:Alcohol use disorder (AUD) affects all sexes, however women who develop AUD may be particularly susceptible to cravings and other components of the disease. While many brain regions are involved in AUD etiology, proper prefrontal cortex (PFC) function is particularly important for top-down craving management and the m...

    journal_title：Neuropharmacology

    pub_type： 杂志文章

    doi：10.1016/j.neuropharm.2020.108126

    authors： Joffe ME,Winder DG,Conn PJ

    更新日期：2020-11-01 00:00:00