YM-50001: a novel, potent and selective dopamine D4 receptor antagonist.

Abstract:

:We investigated some in vitro pharmacological properties of a novel human dopamine D2-like receptor antagonist, YM-50001 [(R)-5-chloro-4-cyclopropylacarbonylamino-2-methoxy-N-[1-(3-methox ybenzyl)- 3-pyrrolidinyl]benzamide monooxalate]. Receptor binding studies revealed that YM-50001 had a potent affinity for human D4 receptors (Ki = 5.62 nM). YM-50001 displayed weak or negligible affinity for other neurotransmitter receptors including human D2 and D3 receptors. YM-50001 shifted the dopamine response curve on each human D2-like receptor subtype-mediated low-Km GTPase activity to the right. YM-50001 also exhibited good D4 selectivity with respect to D2-like receptor antagonism in the functional assay. These results indicate that YM-50001 is a novel, potent and selective D4 receptor antagonist.

journal_name

Neuroreport

journal_title

Neuroreport

authors

Hidaka K,Tada S,Matsumoto M,Ohmori J,Maeno K,Yamaguchi T

subject

Has Abstract

pub_date

1996-11-04 00:00:00

pages

2543-6

issue

15-17

eissn

0959-4965

issn

1473-558X

journal_volume

7

pub_type

杂志文章
  • Quadrupedal locomotor movements in monkeys (M. Fuscata) on a treadmill: kinematic analyses.

    abstract::Three adult Japanese monkeys (M. fuscata: body weights 4.5-8.5 kg) were trained to walk quadrupedally on a surface of a moving treadmill (walking length and width: 150 cm and 60 cm, treadmill speed: 0.4-1.7 m s-1. At any different constant treadmill velocity, the monkeys exhibited a diagonal pattern of locomotor movem...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199610020-00004

    authors: Mori S,Miyashita E,Nakajima K,Asanome M

    更新日期:1996-10-02 00:00:00

  • Anticipating epileptic seizures in real time by a non-linear analysis of similarity between EEG recordings.

    abstract::In a previous publication we showed that non-linear analysis can extract spatio-temporal changes of brain electrical activity prior to epileptic seizures. Here we describe a new method to analyze this long-term non-stationarity in the EEG by a measure of dynamical similarity between different parts of the time series....

    journal_title:Neuroreport

    pub_type: 临床试验,杂志文章

    doi:10.1097/00001756-199907130-00028

    authors: Le Van Quyen M,Martinerie J,Baulac M,Varela F

    更新日期:1999-07-13 00:00:00

  • High frequency repetitive transcranial magnetic stimulation (rTMS) of the dorsolateral prefrontal cortex in schizophrenic patients.

    abstract::Repetitive transcranial magnetic stimulation (rTMS) has been tried therapeutically in major depression. In order to investigate the therapeutic efficacy of rTMS in psychotic patients, 12 participants (four women, eight men) with schizophrenia according to DSM-IV criteria, aged 25 to 63 years (mean (+/-s.d) 40.4+/-11.0...

    journal_title:Neuroreport

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1097/00001756-200012180-00022

    authors: Rollnik JD,Huber TJ,Mogk H,Siggelkow S,Kropp S,Dengler R,Emrich HM,Schneider U

    更新日期:2000-12-18 00:00:00

  • P2X3 receptor in injured human sensory neurons.

    abstract::The ATP-gated cation channel P2X3 is expressed selectively by rat sensory neurones, and may play a role in nociception by binding ATP released from damaged or inflamed tissues. However, the distribution of this channel in human sensory neurons is not known. Using a specific antibody, we have demonstrated intense P2X3 ...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-200004070-00019

    authors: Yiangou Y,Facer P,Birch R,Sangameswaran L,Eglen R,Anand P

    更新日期:2000-04-07 00:00:00

  • Increases in K+ conductance and Ca2+ influx under high glucose with suppressed Na+/K+-pump activity in rat myelinated nerve fibers.

    abstract::To test the combined effect of high glucose and decreased Na+/K+-pump activity, a condition which closely mimics the diabetic state, on nerve ionic currents, changes in action potential and membrane current induced by high glucose in the presence of ouabain were investigated using voltage clamp analysis in rat single ...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-200008030-00040

    authors: Takigawa T,Yasuda H,Terada M,Maeda K,Haneda M,Kashiwagi A,Kitasato H,Kikkawa R

    更新日期:2000-08-03 00:00:00

  • Absence of M100 source asymmetry in autism associated with language functioning.

    abstract::Various clinical populations display atypical volume asymmetry of language structures and also the auditory M100 source. Although such atypical volume asymmetries have also been observed in autism, M100 source asymmetries have not yet been investigated. We examined M100 asymmetry in autism and its relationship with la...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/WNR.0b013e32832e0ca7

    authors: Schmidt GL,Rey MM,Oram Cardy JE,Roberts TP

    更新日期:2009-07-15 00:00:00

  • Ethanol consumption and reward depend on norepinephrine in the prefrontal cortex.

    abstract::We studied the involvement of norepinephrine in the medial prefrontal cortex in the rewarding/reinforcing effects of ethanol. We evaluated the effects of norepinephrine selective depletion in the medial prefrontal cortex of C57/BL6J inbred mice that are commonly used in molecular studies and are highly susceptible to ...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/01.wnr.0000239964.83566.75

    authors: Ventura R,De Carolis D,Alcaro A,Puglisi-Allegra S

    更新日期:2006-11-27 00:00:00

  • Transgenic over-expression of galanin in injured primary sensory neurons.

    abstract::The 29 amino acid neuropeptide galanin is normally expressed in < 5% of sensory neurons in the adult dorsal root ganglia. After nerve transection (axotomy), the galanin content of the dorsal root ganglia rises 120-fold and the peptide is then expressed in > 50% of neurons. Published data suggest that galanin plays a r...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-200211150-00028

    authors: Bacon A,Holmes FE,Small CJ,Ghatei M,Mahoney S,Bloom S,Wynick D

    更新日期:2002-11-15 00:00:00

  • Visually induced gamma-band responses to coherent and incoherent motion: a replication study.

    abstract::The present study was based on earlier findings that the observation of a coherently moving long bar induced gamma-band activity in humans. The power in the EEG-gamma-band was reduced during the presentation of two incoherently moving short bars. The present study demonstrates the replicability of this cortical activi...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199707280-00031

    authors: Müller MM,Junghöfer M,Elbert T,Rochstroh B

    更新日期:1997-07-28 00:00:00

  • MK-801 prevents microglial reaction in rat hippocampus after forebrain ischemia.

    abstract::Delayed neuronal death induced by transient forebrain ischemia in the rat hippocampus is preceded by a prominent microglial reaction which begins within minutes after the ischemic injury. In the present study we have examined the effect of the non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist MK-801 on m...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199202000-00006

    authors: Streit WJ,Morioka T,Kalehua AN

    更新日期:1992-02-01 00:00:00

  • Interaction between the intracellular Ca2+ stores in rat dissociated hippocampal neurones.

    abstract::The interaction between the Ca(2+)-activated K+ currents (IK(Ca)) induced by acetylcholine (ACh), 1-aminocyclopentane-1S,3R-dicarboxylic acid (1S,3R)-ACPD) and caffeine in rat hippocampal CA1 neurones was investigated to examine the functional independence between IP3- and Ca(2+)-sensitive Ca2+ stores. Pretreatment wi...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199605310-00020

    authors: Imanishi T,Yamanaka H,Rhee JS,Akaike N

    更新日期:1996-05-31 00:00:00

  • The role of Ca2+ channels in the repetitive firing of striatal projection neurons.

    abstract::Blockade of L-type Ca2+ channels results in a decrease in firing frequency of neostriatal neurons. In contrast, N- and P/Q-types of Ca2+ channel cooperate to tune firing pattern, since both of these channel types have to be blocked to enhance firing frequency. Parameters of the intensity-frequency plot were differenti...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-200307010-00013

    authors: Pérez-Garci E,Bargas J,Galarraga E

    更新日期:2003-07-01 00:00:00

  • TGF-beta1-conditioned glial cell-derived dendritic cells inhibit expansion of MBP-reactive T cells in vitro.

    abstract::Resident microglial cells contribute to activation and expansion of T cells under inflammatory conditions within the CNS. However, there is no evidence how interactions between microglia and T cells affect CNS inflammation. We evaluated the effect of glial cell-derived dendritic cells (GC-DC) in expanding and eliminat...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-200201210-00012

    authors: Xu LY,Yang JS,Xiao BG

    更新日期:2002-01-21 00:00:00

  • Calbindin-D28K, parvalbumin and calretinin in primate lower motor neurons.

    abstract::It has been suggested that lower motor neurons containing calcium-binding proteins (CBP) may be resistant to degeneration in motor neuron disease. The testing of this hypothesis is hampered by lack of comprehensive information regarding the presence of CBPs in motor neurons. To address this shortcoming, we investigate...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-200403010-00012

    authors: Fahandejsaadi A,Leung E,Rahaii R,Bu J,Geula C

    更新日期:2004-03-01 00:00:00

  • Schwann cells in rat vascular autonomic nerves activated via purinergic receptors.

    abstract::Schwann cells at the somatic neuromuscular junction possess adenosine receptors that when activated by the release of endogenous transmitter modulate quantal transmitter release. Recently, purinergic receptors have been shown to exist on Schwann cells of axon varicosities in visceral smooth muscle where they are activ...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/01.wnr.0000209001.09987.77

    authors: Lin YQ,Bennett MR

    更新日期:2006-04-03 00:00:00

  • Attracting attention to the illusory location of a sound: reflexive crossmodal orienting and ventriloquism.

    abstract::Sound localization can be affected by vision; in the ventriloquism effect, sounds that are hard to localize within hearing become mislocalized toward the location of concurrent visual events. Here we tested whether spatial attention is drawn to the illusory location of a ventriloquized sound. The study exploited our p...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-200006260-00049

    authors: Spence C,Driver J

    更新日期:2000-06-26 00:00:00

  • Event-related potential N270 correlates of brand extension.

    abstract::The aim of this study is to investigate the neural mechanism of extending a brand in a specific product category to other product categories. Facing two sequential stimuli in pairs consisting of beverage brand names (stimulus 1) and product names (stimulus 2) in other categories, 16 participants were asked to indicate...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/WNR.0b013e3281667d59

    authors: Ma Q,Wang X,Dai S,Shu L

    更新日期:2007-07-02 00:00:00

  • Grating and plaid chrominance motion influences the suppressed ocular following response.

    abstract::Involuntary eye movements to foveal stimulation were measured in a monkey while it performed a fixation task. Second-order plaid motion generated higher velocities of eye movements than did first-order gratings, yet the latency of the early following response was no different for grating or plaid motion. Nevertheless,...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199902050-00032

    authors: Guo K,Benson PJ

    更新日期:1999-02-05 00:00:00

  • Auditory sensory memory in 2-year-old children: an event-related potential study.

    abstract::Auditory sensory memory is assumed to play an important role in cognitive development, but little is known about it in young children. The aim of this study was to estimate the duration of auditory sensory memory in 2-year-old children. We recorded the mismatch negativity in response to tone stimuli presented with dif...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/WNR.0b013e3282f97867

    authors: Glass E,Sachse S,von Suchodoletz W

    更新日期:2008-03-26 00:00:00

  • Double-pulse stimulation dissociates intrathalamic and cortical high-frequency (>400Hz) SEP components in man.

    abstract::Human somatosensory evoked potentials (SEP) contain high-frequency (600 Hz) wavelet bursts possibly reflecting repetitive population spikes in thalamocortical axons and/or postsynaptic responses. To dissociate thalamic and cortical burst components the recovery of intrathalamic SEP (derived from electrodes implanted f...

    journal_title:Neuroreport

    pub_type: 临床试验,杂志文章

    doi:10.1097/00001756-200004270-00030

    authors: Klostermann F,Funk T,Vesper J,Siedenberg R,Curio G

    更新日期:2000-04-27 00:00:00

  • Movement-related neuromagnetic fields and performances of single trial classifications.

    abstract::In order to clarify whether neurophysiological profiles affect the performance of brain machine interfaces (BMI), we examined the relationships between amplitudes of movement-related cortical fields (MRCFs) and decoding performances during movement. Neuromagnetic activities were recorded in nine healthy participants d...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/WNR.0b013e32834d935a

    authors: Sugata H,Goto T,Hirata M,Yanagisawa T,Shayne M,Matsushita K,Yoshimine T,Yorifuji S

    更新日期:2012-01-04 00:00:00

  • Persistence of CA1 hippocampal LTP after selective cholinergic denervation.

    abstract::The possible role of endogenous cholinergic innervation in hippocampal plasticity is controversial. We studied the role of acetylcholine (ACh) in short- and long-term potentiation (STP and LTP), using the cholinergic neurotoxin 192 IgG-saporin. It was still possible to induce STP the LTP in the CA1 field following com...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199603220-00024

    authors: Jouvenceau A,Billard JM,Lamour Y,Dutar P

    更新日期:1996-03-22 00:00:00

  • Sexual receptivity is reduced in the female mu-opioid receptor knockout mouse.

    abstract::Activation of mu-opioid receptors is critical to steroid regulation of female sexual behavior, lordosis, in rodents. Estrogen treatment activates mu-opioid receptors in the medial preoptic area inhibiting lordosis, but ultimately appears important for progesterone facilitation of lordosis. We investigated the role of ...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/01.wnr.0000181585.49130.93

    authors: Sinchak K,Shahedi K,Dewing P,Micevych P

    更新日期:2005-10-17 00:00:00

  • Cell density and exogenous CNTF affect CNTF mRNA levels in glial cell cultures.

    abstract::Regulation of CNTF mRNA was investigated in primary cortical astrocytes cultured from newborn rats and in C6 glioma cells. Northern blot analysis indicated that semi-confluent astrocyte cell cultures. CNTF added to confluent astrocyte cultures down-regulated CNTF message in a dose-dependent fashion. In contrast, when ...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199410000-00026

    authors: Meyer V,Unsicker K

    更新日期:1994-10-03 00:00:00

  • Persistence of somatic and dendritic growth associated processes and induction of dendritic sprouting in motoneurones after neonatal axotomy in the rat.

    abstract::The effect of neonatal axotomy on the maturation of motoneurone somadendritic morphology was studied in identified motoneurones innervating the ankle dorsiflexor muscles tibialis anterior (TA) and extensor digitorum longus (EDL) of the rat by intracellular injection of Lucifer Yellow and confocal microscopy. At birth,...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199805110-00051

    authors: Dekkers J,Navarrete R

    更新日期:1998-05-11 00:00:00

  • Ketamine differentially restores diverse alterations of neuroligins in brain regions in a rat model of neuropathic pain-induced depression.

    abstract::Depression is present in a large proportion of patients suffering from chronic pain, and yet the underlying mechanisms remain to be elucidated. Neuroligins (NLs), as a family of cell-adhesion proteins, are involved in synaptic formation and have been linked to various neuropsychiatric disorders. Here, we studied the a...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/WNR.0000000000001045

    authors: Pan W,Zhang GF,Li HH,Ji MH,Zhou ZQ,Li KY,Yang JJ

    更新日期:2018-07-04 00:00:00

  • 1-Aminocyclopropane-carboxylic acid reduces NMDA-induced hippocampal neurodegeneration in vivo.

    abstract::The effect of systemic treatment with 1-aminocyclopro-panecarboxylic acid (ACPC), a partial agonist at the glycine site of the NMDA receptor, on convulsions and neurodegeneration induced by intrahippocampal injection of NMDA was investigated in mice. Five days after intrahippocampal NMDA infusion, 80-100% pyramidal ce...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199601310-00005

    authors: Zapata A,Capdevila JL,Viu E,Trullas R

    更新日期:1996-01-31 00:00:00

  • Brain potentials as objective indexes of auditory pitch extraction from harmonics.

    abstract::Complex tones such as vowels expressed by the human voice vary both in fundamental pitch (harmonic periodicity) and spectrum shape (vowel type). Three different pitches and spectra were combined into nine auditory stimuli. Latencies of cerebral evoked potential components decreased significantly as pitch increased, wh...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199603220-00014

    authors: Ragot R,Lepaul-Ercole R

    更新日期:1996-03-22 00:00:00

  • Cells with a familial Alzheimer's disease mutation produce authentic beta-peptide.

    abstract::Cells overexpressing the beta-amyloid precursor protein possessing a mutation found in familial Alzheimer's disease overproduce beta-amyloid peptide (A beta). Because these findings were based on immunological identification, we have chemically characterized the peptides produced. Purified A beta fragments from the co...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/00001756-199308000-00011

    authors: Dovey HF,Suomensaari-Chrysler S,Lieberburg I,Sinha S,Keim PS

    更新日期:1993-08-01 00:00:00

  • Moyamoya patients exhibit higher brain temperatures than normal controls.

    abstract::The balance between heat production (metabolism) and heat removal (blood flow) helps in keeping the temperature of the brain constant. In patients with moyamoya disease, this balance may be disturbed. The purpose of this study was to assess the thermal pathophysiology of the brain in patients with moyamoya disease. Th...

    journal_title:Neuroreport

    pub_type: 杂志文章

    doi:10.1097/WNR.0b013e32833d6b7a

    authors: Yamada K,Sakai K,Akazawa K,Yuen S,Sugimoto N,Sasajima H,Mineura K,Nishimura T

    更新日期:2010-09-15 00:00:00