Abstract
We aimed to evaluate the effect of ECT on extrastriatal D(2) receptor binding in medicated patients with major depressive disorder (MDD).
Seven patients with a DSM-IV diagnosis of MDD underwent PET scans before and after a series of 6-7 treatments with bilateral ECT. Eleven healthy controls were sca...
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PMID: 20021995
PDF is available here.
Abstract
We examined whether part of this heterogeneity reflects the mixture of distinct cell types present in the striatum, by distinguishing between medium spiny projection neurons (MSNs) and presumed fast-spiking interneurons (FSIs), in freely moving rats. The response of MSNs to both the stimulant amphet...
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PMID: 20090670
PDF is available here.
Abstract
(18)F-Fallypride and (11)C-FLB457 are commonly used PET radioligands for imaging extrastriatal dopamine D(2)/D(3) receptors, but differences in their in vivo kinetics may affect the sensitivity for measuring subtle changes in receptor binding. Focusing on regions of low binding, a direct comparison...
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PMID: 20040928
PDF is available here.
Abstract
These results indicate that activation of dopaminergic D1 and D2 receptors may play a role in mediating the conditioned motivational effects of nicotine-associated cues as measured in the response-reinstatement procedure. These findings suggest that manipulation of dopaminergic neurotransmission at...
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PMID: 20168211
PDF is available here.
Abstract
Cell respiratory activity of protoplasts obtained from the wild type of Neurospora crassa and photoreceptor complex WCC--white collar 1 (wc-1) and white collar 2 (wc-2)--mutants of Neurospora crassa strains was investigated. Respiration inhibition by KCN in the presence of 25 mM succinate was simila...
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PMID: 20586289
PDF is available here.
Abstract
We explored the effects of lorazepam (a single 2.5 mg dose) on cortical and thalamic D(2/3) receptor binding using Positron-Emission Tomography (PET) and the high-affinity D(2/3)-receptor ligand [(11)C]FLB 457 in 12 healthy male volunteers. We used a randomized, double-blind and placebo-controlled s...
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PMID: 19846281
PDF is available here.
Abstract
We have published data showing the effects of the D1-like receptor antagonist, SCH23390 (0.0, 0.01 or 0.02 mg/kg, subcutaneous), on MDMA self-administration, effects of this dose range on the MA dose-response curve were determined. In our previous study, 0.02 mg/kg SCH23390 produced a rightward shif...
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PMID: 19881334
PDF is available here.
Parasitology (95 ( Pt 1))01 2009
Abstract
The cidal properties of some phenolic, halogenated diphenyl, salicylanilide, benzimidazole and diaminophenoxyalkane anthelmintics, against 6-week-old worms of Fasciola hepatica were assessed in vitro. In a conventional fluke culture medium containing RPMI 1640, supplemented with serum with or withou...
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PMID: 3670897
PDF is available here.
Abstract
We evaluated the combined effects of SCH23390-a D(1) receptor antagonist with a D(2) receptor antagonist (eticlopride) on laryngeal neurophysiology, and then tested the separate effects of selective receptor antagonists. Thyroarytenoid (TA) and gastrocnemius (GN) muscle activity was measured at rest...
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PMID: 19535485
PDF is available here.
Abstract
The binding and structural studies of bovine lactoperoxidase with three aromatic ligands, acetylsalicylic acid (ASA), salicylhydoxamic acid (SHA), and benzylhydroxamic acid (BHA) show that all the three compounds bind to lactoperoxidase at the substrate binding site on the distal heme side. The bind...
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PMID: 19465478
PDF is available here.
Abstract
We assessed the effects of the DA releaser amphetamine, as well as receptor selective agonists and antagonists. Amphetamine consistently increased preference for the large/risky lever; an effect that was blocked or attenuated by co-administration of either D(1) (SCH23390) or D(2) (eticlopride) recep...
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PMID: 18668030
PDF is available here.
Abstract
A copper-catalyzed transformation of peptidic thiol esters and boronic acids gives peptidyl ketones and takes place in DMF or DMF/H(2)O at room temperature in air (see scheme). This aerobic reaction only occurs at a thiol ester group capable of coordinating to Cu through its appendage on the sulfur...
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PMID: 19145620
PDF is available here.
Abstract
We have used mutant mice to test whether Rhes (Ras homolog enriched in striatum) is involved in D1 and D2 dopamine receptor-mediated behaviors. Rhes was not necessary for the expression of normal D1/D2 receptor synergism, as measured by apomorphine-induced stereotypy. The stereotypic responses to D1...
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PMID: 18845937
PDF is available here.
Abstract
These results suggest that group II mGluRs may be adapted to interact with dopaminergic neuronal signaling in mediating the sensitized locomotor activity produced by repeated cocaine pre-exposures....
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PMID: 18675831
PDF is available here.
Abstract
We used the radioligands [11C]raclopride and [11C]FLB 457 to determine dopamine D2-receptor binding in 16 human subjects in the morning and evening on the same day. The average difference between morning and evening examinations did not indicate a diurnal effect on D2 receptor availability. However,...
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PMID: 18184446
PDF is available here.
Abstract
Intravenous (iv) cocaine mimics salient somato-sensory stimuli in their ability to induce rapid physiological effects, which appear to involve its action on peripherally located neural elements and fast neural transmission via somato-sensory pathways. To further clarify this mechanism, single-unit r...
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PMID: 18514638
PDF is available here.
Abstract
We describe radiosynthesis of [(11)C]4 and evaluation of its binding characteristics in post-mortem human brain autoradiography and with PET in cynomolgus monkeys. The (11)C labelled 4 was synthesized by using [(11)C]methyltriflate in a methylation reaction with its phenolic precursor with good inco...
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PMID: 18534857
PDF is available here.
Yaya Liu,
Pamela L Donner,
John K Pratt,
Wen W Jiang,
Teresa Ng,
Vijaya Gracias,
Steve Baumeister,
Paul E Wiedeman,
Linda Traphagen,
Usha Warrior,
Clarence Maring,
Warren M Kati,
Stevan W Djuric and
Akhteruzzaman Molla
Abstract
Halosalicylamide derivatives were identified from high-throughput screening as potent inhibitors of HCV NS5B polymerase. The subsequent structure and activity relationship revealed the absolute requirement of the salicylamide moiety for optimum activity. Methylation of either the hydroxyl group or t...
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PMID: 18479921
PDF is available here.
Abstract
We constructed a normal database for the pre- and postsynaptic dopaminergic functions in the living human brain using PET. To measure striatal and extrastriatal dopamine D(1) and D(2) receptor bindings, dopamine transporter binding, and endogenous dopamine synthesis rate, PET scans were performed on...
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PMID: 17962043
PDF is available here.
Abstract
In vitro homogenate assay demonstrated that high SA [(11)C]raclopride (2520-6340 GBq/micromol; 68-171 Ci/micromol) had two-affinity (high and low) binding sites in the striatum and cerebral cortex of rat brain. In the striatum, K(d,high) and B(max,high) values were 0.005+/-0.002 nM and 0.19+/-0.04 f...
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PMID: 18158939
PDF is available here.
Abstract
This study investigated the respiratory properties and the role of the mitochondria isolated from one phosphoenolpyruvate carboxykinase (PCK)-CAM plant, Hoya carnosa, in malate metabolism during CAM phase III. The mitochondria showed high malate dehydrogenase (mMDH) and aspartate amino transferase (...
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PMID: 18403382
PDF is available here.
Abstract
Circadian physiology in the vertebrate retina is regulated by several neurotransmitters. In the lateral eyes of the green iguana the circadian rhythm of melatonin content peaks during the night while the rhythm of dopamine peaks during the day. In the present work, the authors explore the interactio...
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PMID: 18057326
PDF is available here.
Abstract
We examined the effects of various dopamine receptor antagonists on the acquisition and expression of cocaine-induced conditioned suppression in rats. Superimposed on an ongoing baseline of food-reinforced operant responding, a stimulus was paired with response-independent cocaine (3.0 mg/kg, i.v.)...
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PMID: 17628537
PDF is available here.
Abstract
We examined the impact of nicotine treatment on central nervous neurotensin systems by measuring changes in neurotensin tissue content because it has been shown that such changes reflect alterations in release and activity of this peptide system. Male Sprague-Dawley rats received multiple administra...
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PMID: 17689525
PDF is available here.
Abstract
We investigated norepinephrine's (NE) regulation of VTA DA cell excitability by modulation of the hyperpolarization-activated cation current, Ih, with whole cell recordings in rat brain slices. Current clamp recordings show that NE (40 microM) hyperpolarizes spontaneously firing VTA DA cells (11.23+...
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PMID: 17884297
PDF is available here.
Abstract
The acid-base behavior and self-aggregation of salicylhydroxamic (SHA) and p-hydroxybenzohydroxamic acids (PHBHA)have been investigated by UV and 1HNMR spectroscopy, respectively. The acid-base parameters, measured in H2O at 25 degrees C and I=0.1 M, were pK1=7.56, pK2=9.85 for SHA and pK1=8.4, pK2=...
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PMID: 17887699
PDF is available here.
Abstract
We investigated the effects of dopamine agonists on PFC excitatory synaptic transmission with whole-cell recordings from deep-layer pyramidal neurons in brain slices obtained from prepubertal [postnatal day (PD) 28-35] and postpubertal (PD>51) rats. Electrical stimulation of superficial layers elici...
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PMID: 17603809
PDF is available here.
Abstract
Many therapeutic agents had been used for the treatment of diabetes mellitus before insulin was discovered and several hundred plants have shown some extent of antidiabetic activity. This study tries to explore which agents were most widely used in Europe in the pre-insulin era. According to the sci...
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PMID: 17944329
PDF is available here.
Abstract
There was no difference in the binding of [(11)C]FLB 457 between the two groups. [(11)C]raclopride binding was reduced in the dorsal striatum of people taking antidepressants suggesting either that D(2/3) expression was reduced, or that dopamine release was increased, compared to untreated controls....
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PMID: 17197036
PDF is available here.
Abstract
We studied the use of a 4-fluid nozzle spray drier as a new one-step method for preparing drug-containing microparticles to enhance the dissolution and absorption of poorly water-soluble drugs. We employed ethenzamide (EZ) and flurbiprofen (FP) as poorly water-soluble drugs and lactose (LAC) and man...
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PMID: 17582644
PDF is available here.
Abstract
Results suggest that quinpirole reduced T (50) via an action at D(2) receptors. D(1)-like and D(2)-like receptors may mediate behaviourally similar but pharmacologically distinct effects on timing behaviour....
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PMID: 17484066
PDF is available here.
Abstract
We analyzed the susceptibility of Arabidopsis mutants with defects in salicylic acid (SA) and jasmonic acid (JA)/ethylene (ET) signaling to infection by Cauliflower mosaic virus (CaMV). Mutants cpr1-1 and cpr5-2, in which SA-dependent defense signaling is activated constitutively, were substantially...
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PMID: 17555274
PDF is available here.
Abstract
Blockade of dopamine D2 receptors remains a common feature of all antipsychotics. It has been hypothesized that the extrastriatal (cortical, thalamic) dopamine D2 receptors may be more critical to antipsychotic response than the striatal dopamine D2 receptors. This is the first double-blind controlle...
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PMID: 17077809
PDF is available here.
Abstract
These results suggest that while the D2 receptors within the VTA regulate EtOH-motivated behaviors, this is modulated by GABAergic input from the mesolimbic forebrain, specifically from the BST and NAcc....
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PMID: 17451754
PDF is available here.
Abstract
Aspergillus fumigatus possesses a branched mitochondrial electron transport chain, with both cyanide-sensitive and -insensitive oxygen-consumption activities. Mitochondrial reactive oxygen species mediate signaling for alternative oxidase (AOX) expression. A 1173 bp-long Afaox gene encoding a 40 kDa...
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PMID: 17425662
PDF is available here.
Abstract
Activation of the D(1) and D(2) classes of dopamine receptor in the striatum synergistically promotes motor stereotypy. The mechanism of D(1)/D(2) receptor interaction remains unclear. To investigate the involvement of electrical synaptic transmission in this phenomenon, genetic inactivation of the...
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PMID: 17318881
PDF is available here.
Abstract
We demonstrated that a nanoprobe-based assay is a cost-effective, rapid, and accurate platform for robotic screening of small molecules....
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PMID: 17402709
PDF is available here.
Abstract
Activation of NO synthesis by phasic DA transmission is down-regulated via a DA D2 receptor-dependent mechanism. DA D(2) receptor activation opposes DA D(1) receptor activation of NO synthesis at a site postsynaptic to the DA terminal. Further studies examining NO-DA dynamics may have potential to r...
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PMID: 17206493
PDF is available here.
Abstract
Eticlopride into either the Acb core or shell did not affect premature responding, a measure for inhibitory response control, but increased reaction time and errors of omission. In contrast, SCH 23390 into both regions reduced premature responding, slightly improved attentional performance in the co...
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PMID: 16972104
PDF is available here.
Abstract
We examined brain, muscle and skin temperatures together with conventional locomotion during selective interruption of DA transmission induced by a mixture of D1 and D2 antagonists (SCH-23390 and eticlopride at 0.2 mg/kg, s.c.) and its selective activation by apomorphine (APO; 0.05 and 0.25 mg/kg, i...
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PMID: 17196751
PDF is available here.
Abstract
We hypothesized that asymmetry in dopamine neurotransmission declines during normal aging. In order to test this hypothesis, we measured dopamine D2/3 receptor availability with [18F]desmethoxyfallypride-PET (DMFP) in putamen and caudate nucleus (NC) of 21 healthy, right-handed males (24-60 years; 3...
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PMID: 17174574
PDF is available here.
Abstract
The very high-affinity position emission tomography (PET) radioligand [(11)C]FLB 457 was developed in order to study extrastriatal tissues, where the density of dopamine D(2)/D(3) receptors is one to two orders of magnitude lower than in the striatum. The present study investigated the validity of u...
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PMID: 16736043
PDF is available here.
Abstract
We conclude that MP in doses within the therapeutic range for the treatment of attention deficit hyperactivity disorder causes increases in dopamine concentrations in extrastriatal regions and that [(11)C]FLB 457 PET may be a useful tool for the assessment of change in dopamine concentration in thes...
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PMID: 16685253
PDF is available here.
Abstract
The combination of multicommutation and flow-through multioptosensing is presented in this work as a powerful strategy for the routine analysis of active principles in pharmaceuticals. By coupling methodologies, the selectivity and sensitivity of optosensors is maintained, while the use of the multi...
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PMID: 16978822
PDF is available here.
Abstract
These results indicate that the role and regulation of AOX in light are determined by the developmental stage of plant photosynthetic apparatus....
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PMID: 17408956
PDF is available here.
Harry L HL June,
Katrina L KL Foster,
William J A WJ Eiler,
Joshua J Goergen,
Jason B JB Cook,
Nathan N Johnson,
Boikai B Mensah-Zoe,
Jothan O JO Simmons,
Harry L HL June,
Wenyuan W Yin,
James M JM Cook and
Gregg E GE Homanics
Abstract
We determined if the alcohol-induced stimulant effects were regulated via dopaminergic (DA) or benzodiazepine (BDZ)-dependent mechanisms. To accomplish this, we investigated the capacity of DA (eticlopride, SCH 23390) and BDZ (flumazenil, betaCCt) receptor antagonists to attenuate the alcohol-induce...
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PMID: 16710315
PDF is available here.
Abstract
We have explored the ability of endogenous dopamine, present in slices containing the prefrontal cortex, to influence excitatory synaptic transmission. We found that 10 microM amphetamine, which releases and blocks the reuptake of dopamine from dopaminergic nerve terminals, significantly depressed e...
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PMID: 16895728
PDF is available here.
Abstract
We designed three novel compounds, ACB41, ACD15, and ACD16, and investigated their effects on trypanosome alternative oxidase (TAO) enzymatic activity, parasite respiration, and parasite growth in vitro. All three compounds contain a 2-hydroxybenzoic acid moiety, analogous to that present in SHAM, a...
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PMID: 17126803
PDF is available here.
Abstract
The potential for various small molecule organic crystals to undergo complete mechanically induced disordering is investigated. A model is proposed, which considers changes in free energy required for lattice incorporation of a critical dislocation density. Application requires knowledge of a few ph...
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PMID: 16924685
PDF is available here.
Abstract
We examined the interaction between arcuate nucleus dopaminergic cells and accumbal beta-endorphin, during cocaine exposure. Using microdialysis, we found that blockade of arcuate dopamine-2 receptors with a selective antagonist significantly attenuated cocaine-induced increases of beta-endorphin le...
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PMID: 17001283
PDF is available here.
Abstract
We used PET measurements on regional D2 dopamine and 5-HT1A serotonin receptor binding in man to compare binding potential (BP) estimates of six different parametric imaging approaches to the traditional Logan ROI-based approach which was used as a "gold standard". The parametric imaging approaches...
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PMID: 16859930
PDF is available here.
Abstract
We examined the effects of iontophoretic DA and amphetamine on SNr neurons in awake, unrestrained rats. DA had no consistent effects on SNr cells but amphetamine, known to induce DA release, dose-dependently inhibited most of them. This effect was blocked by SCH23390, a selective D1 receptor blocker...
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PMID: 16987223
PDF is available here.
Abstract
Differences in the mesolimbic dopamine (DA) pathway that regulates alcohol preference may also increase sensitivity to the reinforcing effects of other drugs of abuse. In the present study, the curve-shift (rate-frequency) paradigm was used to quantify the interaction of amphetamine with the rewardi...
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PMID: 16893279
PDF is available here.
Abstract
A series of azole-fused salicylamides were prepared as analogues of antimycin and assayed for activity at complex III of the mitochondrial respiratory chain. The activity of these compounds approached that of antimycin in inhibitory potency and some showed growth reduction of Septoria nodorum in vit...
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PMID: 16854082
PDF is available here.
Abstract
We examined how acute dopamine receptor blockade (SCH23390 and eticlopride) affects impulse activity of substantia nigra pars reticulata neurons and their response to iontophoretic gamma-amino-n-butyric acid in awake, unrestrained rats. No changes in discharge rate were found during complete dopamin...
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PMID: 16791106
PDF is available here.
Abstract
We have previously shown that Fawn-Hooded (FH) rats reared in isolation display an anxiety-like phenotype and an enhanced acquisition of ethanol seeking behaviour. Furthermore, antalarmin, a selective corticotrophin-releasing factor type 1 (CRF1) receptor antagonist, reduces isolation-induced acquis...
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PMID: 16820021
PDF is available here.
Abstract
NNMS improved heart physiology after reperfusion following 4 hours of hypothermic ischemia....
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PMID: 16797274
PDF is available here.