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Topic: Dizocilpine


  
  Synaptic potentials in respiratory neurones during evoked phase switching after NMDA receptor blockade in the cat -- ...
After apneusis was induced by dizocilpine, the latency to onset and duration of each PSP were not significantly changed, and changes in their amplitude were inconsistent.
The amplitude of the phase 1 early EPSP was increased by dizocilpine in one cell (Fig.
Dizocilpine depresses the respiratory-related potentials but not the evoked potentials of PI neurones, which might allow afferent inputs from peripheral afferents to terminate inspiration through activation of these neurones.
jp.physoc.org /cgi/content/full/508/2/549   (6512 words)

  
 Dizocilpine - Drug information from Medic8.com
Dizocilpine, also known as MK-801, is a non-competitive NMDA receptor antagonist.
It binds inside the ion channel of the receptor and thus prevents the flow of calcium ions through the channel.
Dizocilpine blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it.
www.medic8.com /medicines/Dizocilpine.html   (378 words)

  
 The Ibogaine Dossier
Dizocilpine (MK-801) is a simpler drug than PCP or ketamine in its actions, but it shares with both the property of blocking in a non-competitive manner the N-methyl-D-aspartate (NMDA) ion- channel.
Behavioral observations and drug-discrimination studies in animals indicate that PCP and dizocilpine are similar in their effects and they both have a neurotoxic effect on neurons in posterior cingulate cortex.
Data from binding studies is consistent with differences between three NMDA receptors in the striatum, thalamus and cerebellum with respect to their preferences for agonist or antagonist binding and the modulation of binding by dizocilpine, cations and polyamines.
www.ibogaine.org /lit-nmda.html   (7184 words)

  
 Med Bull   (Site not responding. Last check: 2007-09-11)
Dizocilpine attenuated lipid peroxidation at 120 minutes, but this was statistically not significant (p=0.204).
In the previous studies, Dizocilpine was proven to improve the motor recovery and reduce the spinal cord edema and tissue damage after AESCI (5,6).
The doses of Dizocilpine (1 mg/kg), that have been used in these studies are the same as the present study.
www.istanbul.edu.tr /istanbultip/mecmua/medmecmua/med-99-1/08.htm   (2064 words)

  
 SSPD Newsletter - Fall 2000- Page 4
In a review of the results from a number of studies, it will first be addressed whether sensitized responding during induction is in fact necessary and sufficient for the subsequent later expression of sensitization.
In this context, the actions of the non-competitive NMDA receptor antagonist dizocilpine on behavioral, cellular and biochemical responses during induction and expression of sensitization will be compared to those of competitive antagonists of NMDA as well as non-NMDA receptors and other manipulations impacting excitatory amino acid transmission.
While the actions of dizocilpine on acute and sensitized drug-induced responding may be complex, the results of the above experiments taken together strongly support a critical need for excitatory amino acid receptor activation in the induction of drug sensitization.
www.sspd.org.uk /newsletters/fall_2000/4.shtml   (672 words)

  
 Characterization of the Dizocilpine Binding Site on the Nicotinic Acetylcholine Receptor -- Arias et al. 59 (5): 1051 ...
I-dizocilpine in the absence or in the presence of CCh was soaked
I-dizocilpine in the absence or in the presence of CCh were excised from
I-dizocilpine (~0.7 nM) and CCh (0.4 mM), in the presence of increasing concentrations of TMB-8 (0.001-200 µM).
molpharm.aspetjournals.org /cgi/content/full/59/5/1051   (6447 words)

  
 Dizocilpine binding to cerebral cortical membranes from developing and ageing mice.   (Site not responding. Last check: 2007-09-11)
Dizocilpine binding to cerebral cortical membranes from developing and ageing mice.
The marked increase in dizocilpine binding sites at the age of 2 weeks coincides with the previously reported transient increase in NMDA binding sites in the cerebral cortex.
The weak potentiation of dizocilpine binding by glutamate and glycine in the immature brain could be a factor which protects neurons during this period from excitotoxicity and increased susceptibility to seizures induced by acidic amino acids.
www.arclab.org /medlineupdates/abstract_8786663.html   (217 words)

  
 Dizocilpine Pretreatment Suppresses the Action of Hypoxia on Hippocampal Epileptic Afterdischarges in Immature Rats   (Site not responding. Last check: 2007-09-11)
Effect of dizocilpine (0.5 mg/kg i.p.) on epileptic afterdischarges elicited by low-frequency electrical stimulation of the dorsal hippocampus was studied in rat pups aged 12 and 18 days.
Dizocilpine potentiated this tendency in 12-day-old rat pups so that it became statistically significant.
Administration of dizocilpine before hypoxia prevented the increase in duration of the first afterdischarge in both age groups.
www.lf2.cuni.cz /iso/physiolres/1999/issue5/iss5cl8.htm   (189 words)

  
 Effects of N-methyl-D-aspartate (dizocilpine) and alpha-amino-3-hydroxy-4-isoxazolepropionate (LY215490) receptor ...
Dizocilpine (1-3 mg/kg, i.p.), a non-competitive N-methyl-D-aspartate receptor antagonist, also significantly decreased the urine release (62-82%) and increased residual volume (180-230-fold).
Combined administration of LY215490 (1 mg/kg, i.p.) and dizocilpine (0.3 mg/kg, i.p.) to 10-day-old rats, in doses that individually had no effect on perineal stimulation-evoked voiding, depressed voided volume by 65%.
These results indicate that, in neonatal rats, glutamatergic transmission in the spinal cord has an essential role in reflex micturition induced by perineal stimulation, and that facilitatory interactions between alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate and N-methyl-D-aspartate glutamatergic mechanisms are important for voiding, as noted previously in adult rats.
www.arclab.org /medlineupdates/abstract_10338308.html   (268 words)

  
 APStracts 2:0109N, 1995.
We investigated the involvement of NMDA receptors in the respiratory pattern in an in vitro preparation of adult brainstem compared to in vivo conditions in the guinea pig.
In vivo, combining the NMDA channel blocker dizocilpine (MK-801) administration (3 mg kg-1) with a surgical section of the vagus nerves induced an apneustic type of respiration characterized by long inspiratory "holds" as it was shown in other species.
The duration of periodic inspiratory motor activity recorded from the hypoglossal nerve was unaffected by dizocilpine (1-100 M) or the competitive NMDA antagonist AP5 (100M and 1mM), although respiratory frequency decreased.
www.uth.tmc.edu /apstracts/1995/jn/May/109n.html   (299 words)

  
 University of Iowa Anesthesia Publications
Relative neuroprotective effects of dizocilpine and isoflurane during focal cerebral ischemia in the rat.
Total infarction volumes (mean +/- SD) were less for the dizocilpine group (100 +/- 65 mm3) versus the awake group (182 +/- 36 mm3; P = 0.001).
The glutamate receptor antagonist dizocilpine was effective in reducing cerebral infarction size during persistent conditions of brain normothermia.
www.anesth.uiowa.edu /readabstract.asp?PMID=0009661549   (315 words)

  
 The involvement of adenosine receptors in the effect of dizocilpine on mice in the elevated plus-maze.
The involvement of adenosine receptors in the effect of dizocilpine on mice in the elevated plus-maze.
The anxiolytic effect of dizocilpine was accompanied by an increase in locomotor activity.
It is concluded that at least part of the anxiolytic and locomotor stimulant properties of dizocilpine may be explained by the release of endogenous adenosine acting at A1, but not A2 receptors.
www.aegis.com /pubs/medline/1998/jan/m9813588.html   (332 words)

  
 Chromatographia online -Supplement 59 abstracts
Dizocilpine is pharmacologically related to ketamine and phencyclidine; as such, it has the potential to affect behavior and performance in horses, with particular efficacy at lower concentrations.
No unchanged dizocilpine was identified in unhydrolysed urine, and the presence of hydroxymethyl and carboxydizocilpine glucuronide metabolites were supported by observation of m/z 414®238 and 428®235 transitions.
The goal of this research was to identify a target analyte for dizocilpine in post-administration equine urine, so that work may begin on development of a forensically validated qualitative method for this target analyte.
www.chromatographia.de /daten/supplement_59_abstracts.htm   (3014 words)

  
 CCK-induced inhibition of presympathetic vasomotor neurons: dependence on subdiaphragmatic vagal afferents and central ...
B: after administration of dizocilpine, the effect of CCK on the discharge of the RVLM neuron is blocked.
B: after administration of dizocilpine, the effect of PBG on the discharge of the RVLM neuron is blocked.
B: after administration of dizocilpine, the effect of PE on the discharge of the RVLM neuron is markedly reduced.
ajpregu.physiology.org /cgi/content/full/287/4/R809   (3982 words)

  
 Erowid.org: Erowid Reference 969 : Chlormethiazole and dizocilpine block the behavioural, but not the neurotoxic ...
A dose of dizocilpine of 0.12 mumol/kg or chlormethiazole at a dose of 150 mumol/kg prevented seizures for 30 min.
This loss was not prevented by administration of either dizocilpine (4.5 mumol/kg intraperitoneally) or chlormethiazole (300 mumol/kg intraperitoneally) given 5 min.
It is proposed that chlormethiazole and dizocilpine may protect against 5,7-dihydroxytryptamine-induced seizures because of their anticonvulsant activity, but that they do not prevent the neurotoxic effects of the compound.
www.erowid.org /references/refs_view.php?ID=969   (223 words)

  
 Ibogaine Treatment Clinics
The method of claim 4, wherein the drug is selected from the group consisting of di(2-tolyl)guanidine, rimcazole, haloperidol, and thioridazine, and salts, isomers, and analogs thereof which suppress activity at sigma receptors and which are effective in preventing a neurotoxic dose of dizocilpine maleate from causing vacuole formation in posterior cingulate-retrosplenial neurons.
Dizocilpine is the most selective and effective non-competitive NMDA antagonist ever discovered; it is powerful and highly selective at the PCP binding site.
The maleate salt of dizocilpine is commercially available to researchers under the name MK-801, and MK-801 has been investigated extensively for use as an antiepileptic and for preventing damage due to cerebral ischemia.
www.ibogaineclinics.com /patents/06_Preventing_neuronal_degeneration_in_Alzheimer's_disease.html   (18027 words)

  
 Glufosinate ammonium induces convulsion through N-methyl-D-aspartate receptors in mice Neuroscience Letters 304 (2001) ...   (Site not responding. Last check: 2007-09-11)
Because of the structural similarities between glufosinate and glutamate, the convulsion induced by glufosinate ammonium may be ascribed to glutamate receptor activation.
Dizocilpine was coadministrated (0.3 mg/kg, i.p.) with glufosinate ammonium (n = 10-1 1 in each group) in mice.
Dizocilpine significantly prolonged the onset of convulsion caused by glufosinate ammonium at the dose of 80 and 100 mg/kg (Fig.
www.mindfully.org /Pesticide/Glufosinate-Ammonium-Convulsion.htm   (1616 words)

  
 The Anorexia File: Drug Therapy
These data raise the possibility that a disturbance of serotonin activity may create a vulnerability for the expression of a cluster of symptoms that are common to both AN and BN and that nutritional factors may affect SSRI response in depression, obsessive-compulsive disorder, or other conditions characterized by disturbances in serotonergic pathways.
The effect of intracerebroventricular administration of dizocilpine on feeding behaviour and adrenal corticrotropic hormone (ACTH)-induced anorexia in elevated plus maze was examined.
Dizocilpine (10, 20 and 40 nmol/rat, i.c.v.) showed a dose-dependent increase in food intake in 16 h food deprived rats.
ssl.adgrafix.com /users/lifestag/anorexia/drugs.html   (6210 words)

  
 APStracts 5:0053R, 1998.   (Site not responding. Last check: 2007-09-11)
In vagotomized, anesthetized rats (n=16) cardiorespiratory responses to hypoxia (8% O2, 30-90 s) were recorded before and after dizocilpine (10 (g-1 mg/kg, i.v.), and NMDA receptors were mapped with [3H]dizocilpine (n=6).
Dizocilpine elicited a dose-related effect on PHFD, blocking PHFD at high doses.
Resting arterial blood pressure and breathing frequency decreased with high doses of dizocilpine, but the respiratory response to hypoxia remained intact.
www.uth.tmc.edu /apstracts/1998/regulatory/February/53R.html   (240 words)

  
 Inspiration-promoting vagal reflex under NMDA receptor blockade in anaesthetized rabbits -- Takano and Kato 516 (2): ...
After dizocilpine administration, stimulation in the range of 0-80 Hz produced values significantly different from control, but stimulation in the 100-160 Hz range produced values that were not significantly different from control (Mann-Whitney U test).
The central end of a vagus nerve was stimulated at frequencies of 0·5-160 Hz to observe effects on spontaneous rhythmic discharge of the phrenic nerve in five vagotomized animals (Fig.
To confirm that the threshold of PSR afferent fibres was not affected by dizocilpine, we tested different stimulation intensities (0·1-5·0 V) before and after dizocilpine administration.
jp.physoc.org /cgi/content/full/516/2/571   (7720 words)

  
 The SPD Network - Summary of SPD Scientific Work Group
When nicotine and dizocilpine are both administered, there is a decreasing effect on PPI as the dose of dizocilpine increases (65-75 % PPI with no dizocilpine; 60% PPI with 25 mg/kg dizocilpine; 40-50% PPI with 50mg/kg dizocilpine; 0-20%PPI with 100 mg/kg dizocilpine).
However, when clozapine is added to nicotine and dizocilpine, the % PPI increases significantly in relation to the dose of clozopine administered.
With tactile startle there is also a dose effect of dizocilpine on the intensity of response (increasing dizocilpine relates to decreased startle).
www.spdnetwork.org /swg/summary   (3700 words)

  
 The SPD Network - Summary of SPD Scientific Work Group
When nicotine and dizocilpine are both administered, there is a decreasing effect on PPI as the dose of dizocilpine increases (65-75 % PPI with no dizocilpine; 60% PPI with 25 mg/kg dizocilpine; 40-50% PPI with 50mg/kg dizocilpine; 0-20%PPI with 100 mg/kg dizocilpine).
However, when clozapine is added to nicotine and dizocilpine, the % PPI increases significantly in relation to the dose of clozopine administered.
With tactile startle there is also a dose effect of dizocilpine on the intensity of response (increasing dizocilpine relates to decreased startle).
www.sinetwork.org /swg/summary   (3700 words)

  
 From the Cover: Glutamate antagonists limit tumor growth -- Rzeski et al. 98 (11): 6372 -- Proceedings of the National ...
Cells were exposed to either culture medium alone (control), dizocilpine (1-250 µM), or GYKI52466 (1-250 µM) for 96 h, and viability was measured photometrically by means of the MTT assay.
)dizocilpine, ketamine, or memantine in concentrations ranging from 1 to 500 µM for 96 h, and viability was measured photometrically by means of the MTT assay.
The effect of cyclophosphamide and thiotepa on viability of TE671 and SKNAS cells was enhanced by dizocilpine (100 µM) and GYKI52466 (100 µM).
www.pnas.org /cgi/content/full/98/11/6372   (3966 words)

  
 Membrane potentials of respiratory neurones during dizocilpine-induced apneusis in adult cats.   (Site not responding. Last check: 2007-09-11)
In the vagotomized cat, blockade of NMDA receptors by dizocilpine (MK-801) produces an apneustic pattern of respiration characterized by a large increase in the duration of inspiration.
In I neurones, dizocilpine decreased the ramp depolarization and an 82% increase in input resistance was observed during inspiration.
The hyperpolarization of PI neurones during early inspiration was reduced in amplitude by dizocilpine and input resistance was increased by 75% during inspiration, indicating that dizocilpine reduced the activity of the presynaptic inhibitory early-inspiratory (eI) neurones.
www.ionchannels.org /showabstract.php?pmid=8887787   (364 words)

  
 1998 - 2000 Allyn & Bacon Award Winner Abstracts - Psi Chi
Two groups of male Sprague Dawley rats were trained to lever-press for either a contingent 2% sucrose/10% ethanol or a 3% sucrose solution for 30 min per day using a 2-lever procedure under a fixed ratio 2 (FR2) schedule of reinforcement.
There was a significant main effect of drugs, but there were no differences between the ethanol and sucrose groups, nor any differences between active and inactive lever presses.
The data suggest that it is unlikely that the NMDA antagonist effects of ethanol contribute to reinstatement of ethanol self-administration behavior.
psichi.threehd.com /awards/winners/abstracts/allbac2.asp   (1007 words)

  
 Article Figures and Tables
Photomicrographs obtained in a representative rat from the compression + dizocilpine maleate group.
Dizocilpine maleate pretreatment improved the survival of SGCs.
Squares and vertical bars indicate the mean and one standard deviation, respectively, in each group.
www.thejns-net.org /jns/issues/v93n1/fig_tab/n0930090_f3.html   (227 words)

  
 A role for NMDA receptors in posthypoxic frequency decline in the rat -- Coles et al. 274 (6): 1546 -- AJP - ...
Dizocilpine had a dose-related effect on the respiratory response to hypoxia.
of dizocilpine, baseline inspiratory duration increased and increased
Before dizocilpine (A), after vehicle (B), and after low dose of dizocilpine (C), peak and posthypoxic breathing frequencies were not significantly correlated (r = 0.30, 0.24, and 0.40 and P = 0.26, 0.58, and 0.34, respectively).
ajpregu.physiology.org /cgi/content/full/274/6/R1546   (4491 words)

  
 Method
Effects of a benzodiazepine, chlordiazepoxide,  a non-competitive NMDA receptor antagonist, dizocilpine (MK-801),  and an opiate agonist, morphine, were assessed.
Preclinical studies with nonhuman subjects that model the complex cognitive demands evident in humans are of considerable importance for the development of suitable treatments with such compounds and also have the potential of increasing understanding of the neurobiology of learning and memory processes.
For example, Keith and Galizio found that a non-competitive NMDA antagonist, dizocilpine (DZP), impaired acquisition in a dose-dependent manner, but the same doses that increased acquisition escape latencies also produced clear evidence of impairment in the performance component.
people.uncw.edu /galizio/rapfiles/BNversion.htm   (4568 words)

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