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Topic: Dopamine antagonist

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	Agonist-antagonist combination to reduce the use of nicotine and other drugs - Patent 5861422
		The method of claim 1 further characterized in that the dopamine receptor activating drug and the antagonist are administered in an amount such that a substantial portion of the receptors which would otherwise be activated by the effects of the abused drug are saturated.
		The method of claim 7 further characterized in that the dopamine receptor activating drug may be present in an amount which would otherwise be toxic in the absence of the antagonist but which toxicity is offset by the presence of the antagonist.
		The method of claim 17 further characterized in that the dopamine receptor activating drug is administered initially and the antagonist is administered by the subject thereafter upon demand for the abused drug by the subject thereby conditioning the subject to a lack of pleasure associated with the abused drug.
	www.freepatentsonline.com /5861422.html (9565 words)

	Dopamine
		The dopamine neurons originating in the VTA send their axons to the prefrontal cortex (an area implicated in attention and working memory) and to the nucleus accumbens (associated with motivational functions).
		Dopamine plays a role in the ability to move, but the nature of its role is unclear.
		Dopamine does not seem to be necessary in order to perform a movement in response to a "strong eliciting stimulus" (e.g., the fire alarm).
	www2.bc.edu /~horvitjo/DA.html (1782 words)

	Biochemical Pharmacology of Midbrain Dopamine Neurons
		Dopamine is released from proximal dendrites in the substantia nigra para compacta of nigrostriatal neurons and from distal dendrites that arborize in the substantia nigra para reticulata.
		Dopamine agonists and antagonists may act on both types of dopamine receptors to elicit biochemical changes in the metabolism of dopamine and alter the functional output of dopaminergic systems (Figure 2).
		While dopamine neurons possessing autoreceptors exhibit dramatic alterations in parameters such as firing rate, dopamine synthesis, and dopamine metabolism in response to acute administration of dopamine antagonists and agonists, mesoprefrontal and mesocingulate dopamine cells are relatively unresponsive both biochemically and electrophysiologically to these agents.
	www.acnp.org /g4/GN401000021/CH021.html (8729 words)

	CISAB \| George V. Rebec - Abstracts
		Although the dopamine response was confined to the brief period of entry into novelty (approximately 8 s duration), a less rapid and more persistent dopamine change (> 20 s duration) occurred in the shell-core transition zone, the so-called shore.
		Phasic inhibition of dopamine uptake in nucleus accumbens induced by intravenous cocaine in freely behaving rats.
		The relatively slow and gradual development of dopamine uptake inhibition, which peaks at times when behaving rats self-inject cocaine, is inconsistent with the suggested role of this mechanism in the acute rewarding (euphoric) effects of self-injected cocaine, but supports its role in the activational and motivational aspects of drug-seeking and drug-taking behavior.
	www.indiana.edu /~animal/research/rebec_abstracts.html (1622 words)

	British Journal of Pharmacology - Real-time analysis of dopamine: antagonist interactions at recombinant human D2long ...
		-adrenergic antagonists in cardiovascular diseases or dopamine antagonists in schizophrenia.
		This was calculated as the surface area between the dopamine and ligand condition for a period of 10 min upon addition of dopamine.
		A similar antagonist profile was also found at the A371K receptor mutant though the efficacy of the blockade was greater as could be expected with a less potent dopamine response at this receptor mutant.
	www.nature.com /bjp/journal/v134/n1/full/0704243a.html (5235 words)

	Dopamine antagonist - Wikipedia, the free encyclopedia
		A dopamine antagonist is a drug which blocks dopamine receptors (of which there are five types in the human body; they are found in the brain, peripheral nervous system, blood vessels, and the kidney).
		Some of these drugs are commonly coupled with a serotonin antagonist and are used as a treatment for certain kinds of psychosis.
		Dopamine antagonists used in psychiatry for psychosis include the atypical antipsychotics clozapine, risperidone, olanzapine, quetiapine, ziprasidone and aripiprazole.
	en.wikipedia.org /wiki/Dopamine_antagonist (147 words)

	The Role of Dopamine Receptors in Schizophrenia
		A study was conducted in which presynaptic dopamine function (measured by the uptake of fluorodopa) was observed by PET in the brains of seven schizophrenic patients and eight healthy people (controls).
		In addition, D1 binding of dopamine was found to be lower in schizophrenic patients as compared to healthy subjects of the same age.
		The increase in dopamine synthesis lasts one to two weeks of medication from the start of therapy, which is the same time required for the medication to become effective.
	wwwchem.csustan.edu /chem44x0/SJBR/Mann.htm (1264 words)

	Dopamine Antagonists & Increased Risk
		Laurie Barclay, MD Dec. 27, 2002 — Women using antipsychotic dopamine antagonists had a 16% increased risk of developing breast cancer, according to results of a retrospective study published in the December issue of the Archives of General Psychiatry.
		Use of antipsychotic dopamine antagonists was linked to increased risk of breast cancer (adjusted hazard ratio, 1.16; 95% confidence interval, 1.07-1.26) but not of colon cancer.
		The authors note that even if their preliminary results are verified, there is less than a 14% chance that a dopamine antagonist user who develops breast cancer did so on the basis of her antipsychotic drug use.
	www.annieappleseedproject.org /dopaninris.html (456 words)

	[No title] (Site not responding. Last check: 2007-09-08)
		The function of the dopamine receptors is to bind to dopamine that was secreted from the presynaptic nerve cells, thus triggering changes in the metabolic activity of the post synaptic nerve cells.
		Dopamine, histamine and Norepinephrine are known to be involved in increasing arousal.
		These reduced dopamine levels, which may be responsible for the negative symptoms of schizophrenia, appear to lead to increased levels of dopamine in secondary dopaminergic systems.
	sulcus.berkeley.edu /mcb/165_001/papers/manuscripts/_286.html (3056 words)

	Dopamine (Site not responding. Last check: 2007-09-08)
		Dopamine also is synthesized by neurons in the ventral tegmental area, which projects to the prefrontal cortex and the basal forebrain, including the nucleus accumbens.
		Dopamine receptors are involved in neurological disorders such as Parkinson's disease and schizophrenia.
		Dopamine is very basic and probably exists in the protonated form in solution rendering it inaccessable to the brain.
	www.neurosci.pharm.utoledo.edu /MBC3320/dopamine.htm (870 words)

	Glutamate Transmission in the Nucleus Accumbens Mediates Relapse in Cocaine Addiction -- Cornish and Kalivas 20 (15): ... (Site not responding. Last check: 2007-09-08)
		Elevated dopamine transmission in the nucleus accumbens is thought to be a primary mediator of addiction to cocaine.
		cocaine or saline, or intra-accumbens coadministration of dopamine.
		by dopamine in the nucleus accumbens was antagonized by CNQX.
	www.jneurosci.org /cgi/content/full/20/15/RC89 (3715 words)

	BioMed Central \| Full text \| Dibenzazecine compounds with a novel dopamine/5HT2Areceptor profile and 3D-QSAR analysis
		Dopamine is an important neurotransmitter in the mammalian CNS which has influence on physiological, behavioural and neuroendocrine functions, mediated through receptors on the cell surface.
		Dopamine receptors are clinically important drug targets for the treatment of disorders such as Parkinson's disease and schizophrenia [3].
		Antagonistic activity was tested by pre-incubation of test compounds for 30 min at 37°C and 5% CO prior to the addition of agonist (hD
	www.biomedcentral.com /1471-2210/6/11 (6354 words)

	Understanding Addiction
		Dopamine affects brain processes that control movement, emotional response, and ability to experience pleasure and pain.
		In contrast to dopamine agonists, dopamine antagonists are drugs that bind but don't stimulate dopamine receptors.
		Dopamine antagonists are traditionally used to treat schizophrenia and related mental disorders.
	www.utexas.edu /research/asrec/dopamine.html (1051 words)

	Altered Nucleus Accumbens Circuitry Mediates Pain-Induced Antinociception in Morphine-Tolerant Rats -- Schmidt et al. ... (Site not responding. Last check: 2007-09-08)
		the dopamine receptor antagonist flupentixol or the opioid receptor
		Altier N, Stewart J (1998) Dopamine receptor antagonists in the nucleus accumbens attenuate analgesia induced by ventral tegmental area substance P or morphine and by nucleus accumbens amphetamine.
		Altier N, Stewart J (1999) The role of dopamine in the nucleus accumbens in analgesia.
	www.jneurosci.org /cgi/content/full/22/15/6773 (4345 words)

	lavid
		prevents the binding of dopamine to its receptor in the synaptic cleft, which is the space between brain cells (neurons) where neurotransmitters modulate communication within the brain.
		The initial use of haloperidol in stuttering was not based on its mechanism of action, as the association of dopamine and stuttering was not known at the time.
		Prolactin induces lactation and ovulation, and its release from the pituitary gland is inhibited by dopamine.
	www.mnsu.edu /comdis/isad8/papers/lavid8.html (1926 words)

	Dopamine and Serotonin (5-HT) in Migraine
		Peroutka asks whether it is the increase in dopamine that triggers and maintains a migraine attack.
		In 1977, Hughes reported that 10 mg metoclopramide, a dopamine antagonist, relieved the nausea and headache in 3 of 4 patients having an acute attack (Med J Aust 1977; 2:580).
		Modulating brain dopamine and 5-HT in migraineurs mirrors the approach used in treating hypertension with blood pressure and cholesterol lowering agents.
	www.meds.com /conrad/aash/peroutka.html (464 words)

	[No title]
		Inhibiting the re-uptake of dopamine (cocaine, bupropion, methylphenidate, amineptine)
		Furthermore, it is possible that focusing on the role of dopamine in abuse-potential could aid in the removal of that potential from various drugs.
		Antidepressants that affect dopamine transmission (as opposed to just serotonin and norepinephrine) are arguably better for some patients and may contribute to faster remission.
	www.unc.edu /~novick/bupropion2.html (1321 words)

	April 5, 2001-Vol32n26: Hull sets standard for research in field
		In the next set of experiments, Hull and colleagues administered a dopamine antagonist-a drug that blocks dopamine receptors-which was known to decrease the number of dopamine receptors in adult rats when given prenatally, and to increase dopamine receptors when given postnatally.
		To her surprise, the dopamine antagonist made male rats less male no matter when it was administered, and testosterone levels weren't affected.
		Using microdialysis, Hull was able to show that dopamine must be released in the male rat's MPOA for copulation to occur and must continue for the animal to ejaculate-the test of a "successful" copulation.
	www.buffalo.edu /reporter/vol32/vol32n26/n3.html (1510 words)

	L-646,462, a cyproheptadine-related antagonist of dopamine and serotonin with selectivity for peripheral systems - ...
		The selectivity of L-646,462 for peripheral serotonin (5-HT) receptors in rats was determined by measuring its effectiveness in blocking 5-HT-induced paw edema (peripheral response) and 5-hydroxytryptophan-induced head twitch (central response); a ratio of 114 was obtained.
		L-646,462 is, therefore, selective in vivo, preferentially blocking dopamine and 5-HT receptors located outside the blood-brain barrier.
		L-646,462, a cyproheptadine-related antagonist of dopamine and serotonin with selectivity for peripheral systems.
	www.rti.org /abstract.cfm?pubid=2708 (308 words)

	FuturePundit: Dopamine D2 Receptor Blocker Cures Cocaine Addiction In Rats
		As a result, their brain cells made more dopamine, which meant cocaine was not needed to increase dopamine levels and the addiction was cured.
		Dopamine production and nerve cell endings capable of releasing dopamine were increased when the D2 receptor was blocked by the drug.
		Dopamine is released by specialised nerve endings in the brain called terminals.
	www.futurepundit.com /archives/002615.html (2029 words)

	Schizophrenia.com - New Schizophrenia Medications
		Asenapine is a serotonin and dopamine (5HT/D2) antagonist, part of a class of atypical antipsychotics that have typically been more effective than medications that act only at D2 receptors.
		For example, clozapine, risperadone, and olanzapine all have serotonin-dopamine antagonist properties, and these drugs are popular for their low incidence of side effects (particularly EPS side effects) and their efficacy against both positive and negative symptoms.
		It is expected that partial dopamine agonist action will have beneficial effects for positive, negative, and cognitive symptoms, while the serotonergic agonist action will help alleviate some side effects and possibly combat depression and anxiety that can accompany schizophrenia treatment.
	www.schizophrenia.com /newmeds2004.html (2219 words)

	NIDA - Publications - NIDA Notes - Vol. 18, No. 1 - Research Findings
		After taking a chemical compound that blocks release of dopamine to the brain's pleasure center, smokers lit up sooner and smoked more cigarettes than they did after taking a compound that stimulates dopamine release.
		Smokers who received haloperidol, a dopamine antagonist, smoked more cigarettes during a 5-hour period and took more puffs per cigarette than did smokers who received bromocriptine, which enhances dopamine's effects.
		Nicotine triggers the release of dopamine in the brain, and the pleasurable sensations that result are thought to be a driving force in establishing addiction.
	www.drugabuse.gov /NIDA_notes/NNVol18N1/Manipulating.html (662 words)

	Functional characterization of basolateral and luminal dopamine receptors in rabbit CCD -- Saito et al. 281 (1): 114 -- ... (Site not responding. Last check: 2007-09-08)
		Domperidone, a specific in vitro dopamine antagonist, devoid of in vivo central dopaminergic activity.
		Evidence that intrarenal dopamine acts as a paracrine substance at the renal tubule.
		Dopamine inhibits AVP-dependent Na+ transport and water permeability in rat CCD via a D4-like receptor.
	ajprenal.physiology.org /cgi/content/full/281/1/F114 (3087 words)

	SELECTIVE ACTIVATION OF DOPAMINE RECEPTOR SUBPOPULATIONS
		While this hypothesis is proposed to generalize to all G-protein coupled receptor systems, I propose to test and refine this hypothesis by studying D2-like dopamine (DA) receptors.
		Surprisingly, however, these same drugs have little or no effect on D2 receptors known (or presumed) to be coupled to potassium (K+) channels (e.g., they do not inhibit dopamine cell firing or dopamine release, and they induce only weak activation of K+ channels in pituitary lactotrophs).
		The development of drugs (such as the hexahydrobenzo[a]phenathridines) with functional selectivity may lead to dramatically improved pharmacotherapies by providing opportunities for targeting a subset of receptor-linked events, thus avoiding the undesirable side effects due to widespread activation or blockade of receptor functions.
	www.med.unc.edu /wrkunits/1dean/research/Mailman243.html (414 words)

	UB Reporter: Researchers aligning opposing camps
		Functionalists have held to the dopamine antagonist theory: that the neurotransmitter dopamine is malfunctioning, causing the disease's characteristic delusions and hallucinations.
		The mouse displays the structural and neurochemical changes in dopamine neurons similar to those seen in PET scans of human patients with schizophrenia.
		The investigators found that both the dopamine-producing regions in the brain and the new cells within those regions were smaller than normal, prompting the neurons to overcompensate and overproduce dopamine.
	www.buffalo.edu /reporter/vol38/vol38n6/articles/SchizoMouse.html (500 words)

	Domperidone, a new dopamine antagonist -- Champion et al. 135 (5): 457 -- Canadian Medical Association Journal (Site not responding. Last check: 2007-09-08)
		Domperidone, a new dopamine antagonist -- Champion et al.
		Domperidone is a dopamine antagonist that has recently been released in
		antagonist, it does not readily enter the central nervous system.
	www.cmaj.ca /cgi/content/abstract/135/5/457 (146 words)

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