Mazindol: Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.Dopamine Uptake Inhibitors: Drugs that block the transport of DOPAMINE into axon terminals or into storage vesicles within terminals. Most of the ADRENERGIC UPTAKE INHIBITORS also inhibit dopamine uptake.Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake.Bupropion: A unicyclic, aminoketone antidepressant. The mechanism of its therapeutic actions is not well understood, but it does appear to block dopamine uptake. The hydrochloride is available as an aid to smoking cessation treatment.Benztropine: A centrally active muscarinic antagonist that has been used in the symptomatic treatment of PARKINSON DISEASE. Benztropine also inhibits the uptake of dopamine.Dopamine: One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.Nomifensine: An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266)Nalorphine: A narcotic antagonist with some agonist properties. It is an antagonist at mu opioid receptors and an agonist at kappa opioid receptors. Given alone it produces a broad spectrum of unpleasant effects and it is considered to be clinically obsolete.Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403)Anabasine: A piperidine botanical insecticide.1-Naphthylamine: A suspected industrial carcinogen (and listed as such by OSHA). Its N-hydroxy metabolite is strongly carcinogenic and mutagenic.Aconitine: A C19 norditerpenoid alkaloid (DITERPENES) from the root of ACONITUM plants. It activates VOLTAGE-GATED SODIUM CHANNELS. It has been used to induce ARRHYTHMIAS in experimental animals and it has antiinflammatory and antineuralgic properties.3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.Methyltyrosines: A group of compounds that are methyl derivatives of the amino acid TYROSINE.alpha-Methyltyrosine: An inhibitor of the enzyme TYROSINE 3-MONOOXYGENASE, and consequently of the synthesis of catecholamines. It is used to control the symptoms of excessive sympathetic stimulation in patients with PHEOCHROMOCYTOMA. (Martindale, The Extra Pharmacopoeia, 30th ed)2-Naphthylamine: A naphthalene derivative with carcinogenic action.Antipsychotic Agents: Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus.Prince Edward Island: An island in the Gulf of St. Lawrence constituting a province of Canada in the eastern part of the country. It is very irregular in shape with many deep inlets. Its capital is Charlottetown. Discovered by the French in 1534 and originally named Ile Saint-Jean, it was renamed in 1799 in honor of Prince Edward, fourth son of George III and future father of Queen Victoria. (From Webster's New Geographical Dictionary, 1988, p981 & Room, Brewer's Dictionary of Names, 1992, p433)Schools, Health Occupations: Schools which offer training in the area of health.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Madurella: A mitosporic fungal genus that causes MYCETOMA in humans. Madurella grisea and M. mycetomatis are the etiological agents.Pyrones: Keto-pyrans.Datura: A plant genus of the family SOLANACEAE. Members contain TROPANES. The common name of trumpet flower is also sometimes used for GELSEMIUM.Estrenes: Unsaturated derivatives of the ESTRANES with methyl groups at carbon-13, with no carbon at carbon-10, and with no more than one carbon at carbon-17. They must contain one or more double bonds.ValeratesTetrazolium Salts: Quaternary salts derived from tetrazoles. They are used in tests to distinguish between reducing sugars and simple aldehydes, for detection of dehydrogenase in tissues, cells, and bacteria, for determination of corticosteroids, and in color photography. (From Mall's Dictionary of Chemistry, 5th ed, p455)Pyrrolidinones: A group of compounds that are derivatives of oxo-pyrrolidines. A member of this group is 2-oxo pyrrolidine, which is an intermediate in the manufacture of polyvinylpyrrolidone. (From Merck Index, 11th ed)Heptanoic Acids: 7-carbon saturated monocarboxylic acids.PyransNaltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.Ergolines: A series of structurally-related alkaloids that contain the ergoline backbone structure.Benzazepines: Compounds with BENZENE fused to AZEPINES.Copyright: It is a form of protection provided by law. In the United States this protection is granted to authors of original works of authorship, including literary, dramatic, musical, artistic, and certain other intellectual works. This protection is available to both published and unpublished works. (from Circular of the United States Copyright Office, 6/30/2008)Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.Quinpirole: A dopamine D2/D3 receptor agonist.Dopamine Antagonists: Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.2,3-Diketogulonic Acid: Metabolite of ASCORBIC ACID and the oxidized form of the lactone DEHYDROASCORBIC ACID.Dictionaries, MedicalDictionaries as Topic: Lists of words, usually in alphabetical order, giving information about form, pronunciation, etymology, grammar, and meaning.Mice, Knockout: Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.Memory, Short-Term: Remembrance of information for a few seconds to hours.Memory: Complex mental function having four distinct phases: (1) memorizing or learning, (2) retention, (3) recall, and (4) recognition. Clinically, it is usually subdivided into immediate, recent, and remote memory.Reagins: Antibodies, especially IGE, that bind to tissue of the same species so that ANTIGENS induce release of HISTAMINE and other vasoactive agents. HYPERSENSITIVITY is the clinical manifestation.Memory Disorders: Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.Oxyquinoline: An antiseptic with mild fungistatic, bacteriostatic, anthelmintic, and amebicidal action. It is also used as a reagent and metal chelator, as a carrier for radio-indium for diagnostic purposes, and its halogenated derivatives are used in addition as topical anti-infective agents and oral antiamebics.Maze Learning: Learning the correct route through a maze to obtain reinforcement. It is used for human or animal populations. (Thesaurus of Psychological Index Terms, 6th ed)Behavior, Animal: The observable response an animal makes to any situation.Space Perception: The awareness of the spatial properties of objects; includes physical space.Spatial Behavior: Reactions of an individual or groups of individuals with relation to the immediate surrounding area including the animate or inanimate objects within that area.Receptors, Adrenergic, beta-2: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.beta-Adrenergic Receptor Kinases: G-protein-coupled receptor kinases that mediate agonist-dependent PHOSPHORYLATION and desensitization of BETA-ADRENERGIC RECEPTORS.Arrestins: Regulatory proteins that down-regulate phosphorylated G-protein membrane receptors, including rod and cone photoreceptors and adrenergic receptors.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Receptors, Adrenergic, beta: One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.Receptors, Adrenergic: Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction.Receptors, Adrenergic, beta-1: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.Convolvulaceae: The morning glory family of flowering plants, of the order Solanales, which includes about 50 genera and at least 1,400 species. Leaves are alternate and flowers are funnel-shaped. Most are twining and erect herbs, with a few woody vines, trees, and shrubs.Internet: A loose confederation of computer communication networks around the world. The networks that make up the Internet are connected through several backbone networks. The Internet grew out of the US Government ARPAnet project and was designed to facilitate information exchange.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.Editorial Policies: The guidelines and policy statements set forth by the editor(s) or editorial board of a publication.Publishing: "The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.Software: Sequential operating programs and data which instruct the functioning of a digital computer.User-Computer Interface: The portion of an interactive computer program that issues messages to and receives commands from a user.Sequence Analysis, RNA: A multistage process that includes cloning, physical mapping, subcloning, sequencing, and information analysis of an RNA SEQUENCE.Information Storage and Retrieval: Organized activities related to the storage, location, search, and retrieval of information.Receptors, Dopamine: Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.Receptors, Dopamine D5: A subtype of dopamine D1 receptors that has higher affinity for DOPAMINE and differentially couples to GTP-BINDING PROTEINS.Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. 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December 1991). "(+/-)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3- benzazepin, a new high-affinity D1 ... 275 (3): 1367-74. PMID 8531104. Barrett AC, Miller JR, Dohrmann JM, Caine SB (2004). "Effects of dopamine indirect agonists and ... 116 (1): 9-18. doi:10.1007/BF02244865. PMID 7862937. Weed MR, Woolverton WL (December 1995). "The reinforcing effects of ... 35 (8): 1466-71. doi:10.1021/jm00086a016. PMID 1533424. Rosenzweig-Lipson S, Hesterberg P, Bergman J (September 1994). " ...
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... phenyl)-1h-pyrazol-3-amine MeSH D03.383.129.539.200 --- epirizole MeSH D03.383.129.539.487 --- indazoles MeSH D03.383.129.539. ... phenyl)-, methyl ester MeSH D03.383.725.210 --- dimethindene MeSH D03.383.725.220 --- 2,2'-dipyridyl MeSH D03.383.725.227 --- ... phenyl)-, methyl ester MeSH D03.383.725.547.950 --- xanthinol niacinate MeSH D03.383.725.565 --- nicotinyl alcohol MeSH D03.383 ... 2,3,4,5-tetrahydro-8-chloro-3-methyl-5-phenyl-1h-3-benzazepin-7-ol MeSH D03.438.079.800 --- 2,3,4,5-tetrahydro-7,8-dihydroxy-1- ...
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"Mesostriatal and Mesolimbic Dopamine Uptake Binding Sites Are Reduced " by G. Chinaglia, Francisco J. Alvarez et al.
It has been suggested that not only mesostriatal but also mesolimbic pathways are involved in the degeneration of dopaminergic neurons in Parkinsons disease. Using quantitative ligand autoradiography we have investigated dopamine transporter sites in basal ganglia of patients affected by Huntingtons chorea, Parkinsons disease and progressive supranuclear palsy. [3H]Mazindol, a ligand for catecholamine uptake, was used in the presence of desipramine to block the binding to norepinephrine uptake sites. Schizophrenic cases were entered in the study to take into account the effects of neuroleptics, commonly administered also to Huntingtons disease patients, on dopamine uptake sites. In control cases ...
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appetite suppressants, drug information, generic and brand names, Benzphetamine, Diethylpropion, Mazindol, Phendimetrazine,...
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The following drugs have DRI action and have been or are used clinically specifically for this property: amineptine, dexmethylphenidate, difemetorex, fencamfamine, lefetamine, levophacetoperane, medifoxamine, mesocarb, methylphenidate, nomifensine, pipradrol, prolintane, and pyrovalerone. The following drugs are or have been used clinically and possess only weak DRI action, which may or may not be clinically-relevant: adrafinil, armodafinil, bupropion, mazindol, modafinil, nefazodone, sertraline, and sibutramine. The following drugs are or have been clinically used but only coincidentally have DRI properties: benzatropine, diphenylpyraline, etybenzatropine, ketamine, nefopam, pethidine ...
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter. - PubMed - NCBI
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In myocardial ischemia, adrenergic terminals undergo ATP depletion, hypoxia, and intracellular pH reduction, causing the accumulation of axoplasmic norepinephrine (NE) and intracellular Na+ [via the Na+-H+ exchanger (NHE)]. This forces the reversal of the Na+- and Cl−-dependent NE transporter (NET), triggering massive carrier-mediated NE release and, thus, arrhythmias. We have now developed a cellular model of carrier-mediated NE release using an LLC-PK1 cell line stably transfected with human NET cDNA (LLC-NET). LLC-NET cells transported [3H]NE and [3H]N-methyl-4-phenylpyridinium ([3H]MPP+) in an inward ...
0059]The role of iron with regard to the central nervous system is often reported in fundamental neurophysiopathology as clinical. Functional intellectual asthenia, chronic fatigue syndrome, or conversely psychomotive instability and irritability may be the consequence of iron deficiency (Lozoff, 1989 Adv Pediatr 1989; 6:331-59). The role of iron in the physiopathology of neurological ailments, and in particular in idiopathic Parkinsons disease, has been known for more than thirty years. The evidence of an increase in iron in particular in certain cerebral structures (e.g. dentate nucleus) in rare neurodegenerative pathologies (e.g. Friedreichs ataxia) is also known. More ...
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Continuous infusion of selective dopamine uptake inhibitors or cocaine produces time-dependent changes in rat locomotor...
Chronic continuous cocaine treatment produces a unique pattern of locomotor activation over time. An initial, progressive increase in locomotion is indicative of sensitization Unlike intermittent cocaine, this increase is subsequently reversed during the continuous exposure, and activity returns to pre-sensitization levels within days. To study the pharmacological mechanisms that underlie this phenomenon, osmotic minipumps containing cocaine or selective uptake inhibitors of dopamine (GBR 12909 or RTI-117), serotonin (fluoxetine), or norepinephrine (nisoxetine) were implanted into rats.
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The monoamine uptake inhibitor BTS 74 398 effectively reversed motor deficits in MPTP-treated primates (Hansard et al., 2004), but investigation into the contribution 5-HT and noradrenaline uptake inhibition made to this effect were confounding (Hansard et al., 2002a). BTS 74 398 was found to be highly potent, but a combination of GBR 12909 with 5-HT uptake inhibition negated all the benefits afforded by the dopamine uptake inhibitor alone. Neither had there been any investigation of the dopamine receptors involved in the response. Against this background, the relative involvement of dopamine, noradrenaline, and ...
The effects of the novel tropanes selective for the serotonin (WF-31 and WF-50) and dopamine (WF-11) transporters were compared with fluoxetine and GBR 12909 in the FST. All of the compounds tested decreased immobility in the FST, albeit to varying degrees. Moreover, administration of the selective serotonin uptake inhibitors WF-31, WF-50 and fluoxetine produced a behavioral pattern qualitatively different from the pattern observed after administration of the dopamine uptake inhibitors WF-11 and GBR 12909. WF-31, WF-50 and fluoxetine increased swimming while not affecting climbing, whereas WF-11 increased climbing and swimming and GBR 12909 increased climbing while not affecting swimming. In addition, the selective dopamine ...
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TY - JOUR. T1 - Characterization of a recombinant human dopamine transporter in multiple cell lines. AU - Eshleman, A. J.. AU - Neve, R. L.. AU - Janowsky, Aaron. AU - Neve, Kim. PY - 1995. Y1 - 1995. N2 - A 3.5-kilobase cDNA encoding the dopamine transporter was isolated from a human substantia nigra cDNA library. Sequence analysis of the coding region of the transporter identified two nucleotide differences between the cDNA and published human dopamine transporter sequences. One of the substitutions changed an amino acid conserved among previously cloned dopamine (DA) and norepinephrine transporters, Arg-344, to a methionine. C6 glioma cells or COS-7 cells transfected with the cDNA (C6-hDAT and Cos7-hDAT ...
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Beta-CIT-FP is a cocaine analog. Beta-CIT-FP is a highly potent and selective dopamine uptake inhibitors and a potent DA, 5-HT, and NE uptake inhibitor.
A number of drugs have been developed and marketed to replace amphetamines as appetite suppressants. These anorectic drugs include benzphetamine (Didrex), diethylproprion (Tenuate, Tepanil), fenfluramine (Pondimin), mazindol (Sanorex, Mazanor), phendimetrazine (Bontril, Prelu-2, Plegine) and phentermine (Ionamin, AdipexP). They produce many of the effects of the amphetamines, but are generally less potent. All are controlled under the CSA because of the similarity of their effects to those of the amphetamines. ...
Abstract This experiment examines the effect of access to a running-wheel on intravenous cocaine self-administration in male and female rats. Rats maintained at 85\% of their free-..
Wei-Lun Sun WL, Zhou L, Nazarian A, Quinones- Jenab V and Jenab S. (2015). Acute cocaine differentially induces PKA phosphorylation substrates in male and female rats. Journal of Addiction Research & Therapy, in press.. Nygard SK, Klambatsen A, Balouch B, Quinones-Jenab V and Jenab S. (2015). Region and context-specific intracellular responses associated with cocaine-induced conditioned place preference expression. Neuroscience 287:1-8.. Nygard SK, Klambatsen A, Hazim R, Eltareb MH, Blank JC, Chang AJ, Quinones-Jenab V and Jenab S. (2013). Sexually dimorphic intracellular responses after cocaine-induced conditioned place preference expressionBrain Res. 1520:121-33.. Quinones-Jenab V and Jenab S. (2012). Influence of sex differences and gonadal hormones on cocaine addiction ILAR J. 53:14-22.. Quinones-Jenab V ...
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The maximal effects achieved by the dopamine agonists alone were also not related to the lack of GABA enhancement. For example, when given alone across a wide range of doses, methamphetamine produced significant but minimal amounts of gnawing (maximal score ,100). Amfonelic acid, on the other hand, produced greater maximal increases in gnawing (∼400) (Tirelli and Witkin, 1995). Nevertheless, THIP enhanced gnawing of both methamphetamine and amfonelic acid. Of the compounds that were not enhanced by THIP, a range of maximal effects have been demonstrated under the present testing conditions. Maximal gnawing scores for WIN ...
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We reviewed 20 English-language weight-reduction studies, reported between 1967 and March 1993, of the effect of | or = 6 mo of pharmacologic therapy on weight loss and its maintenance to determine the clinical benefits of extended treatment, propose treatment guidelines, and identify future research needs. Pharmacologic agents included phentermine, mazindol, fenfluramine, dexfenfluramine, and fluoxetine. Study designs varied with respect to blinding, use of a single agent vs a combination, dosing, length of therapy, patient selection, adjunctive therapy, and visit frequency. At endpoint, weight loss varied from study to study but a plateauing of weight loss or weight regain was observed after approximately ...
... (Letter Report, 06/07/96, GAO/HEHS-96-80).. Pursuant to a congressional request, GAO reviewed the extent to which federally funded cocaine treatment therapies have proven successful and additional research initiatives that are needed to increase knowledge of cocaine treatment effectiveness.. GAO found that: (1) cocaine treatment research is still in its early stages; (2) preliminary study results have shown that relapse prevention, community reinforcement and contingency management, and neurobehavioral therapy may produce prolonged periods of abstinence among cocaine users; (3) relapse prevention programs have the highest abstinence rates, followed by community ...
Our group is trying to understand neurological mechanisms which underlie sex differences in responses to stressors, such as pain and drugs of abuse. To understand these questions we are using an integrated approach combining molecular, cellular, physiological and behavioral techniques such as in situ histochemistry, RNA solution hybridization, RT-PCR, immunocytochemistry, radioimmunoassay, and behavioral monitoring. Over the past five years at Hunter, we have demonstrated fundamental sex differences in cocaine-induced behavioral effects. For example, female rats have exaggerated behavioral responses and increased corticosterone release after acute and ...
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Ethylphenidate (EPH) is a psychostimulant and a close analog of methylphenidate. Ethylphenidate acts as both a dopamine reuptake inhibitor and norepinephrine reuptake inhibitor, meaning it effectively boosts the levels of the norepinephrine and dopamine neurotransmitters in the brain, by binding to, and partially blocking the transporter proteins that normally remove those monoamines from the synaptic cleft. However, considering the close similarities between ethylphenidate and methylphenidate and the fact that ...
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ROCKVILLE, MD -- (Marketwire) -- 11/09/12 -- MarketResearch.com has announced the addition of the new report "The Future of Heart Health Food and Drinks," to their collection of market reports. Cardiovascular disorders such as elevated blood cholesterol levels, hypertension, and impaired blood circulation represent a major public health issue and are the number one cause of mortality globally. The WHO estimates that 29% of all global deaths in 2004 were due to cardiovascular diseases. This report examines the emerging market for food and drink products that target heart health. ...
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ENDOGENOUS DOPAMINE FACILITATES STRIATAL IN VIVO ACETYLCHOLINE-RELEASE BY ACTING ON D(1)-RECEPTORS LOCALIZED IN THE STRIATUM |...
Intrastriatal application of the D1 antagonist SCH 23390 by two procedures, reverse dialysis (20-mu-M) and local injection (0.45 nmol per striatum), elicited a reduction in acetylcholine (ACh) release superimposable on that induced by systemic administration. The novel selective D1 antagonist SCH 39166 produced a similar decreasing effect on striatal ACh release on local injection (0.45 nmol per striatum). On the other hand, local application of SCH 23390 into the frontal cortices (0.45 nmol per side) failed to alter striatal ACh overflow, indicating that the drug does not diffuse out of its injection site to any significant extent. The dopamine release inducer d-amphetamine (2 mg/kg s.c.) and ...
Axsome Therapeutics Initiates Phase 2/3 Trial of AXS-05 for Alzheimer's Disease Agitation Nasdaq:AXSM
Agitation reported in nearly 50% of patients with Alzheimers disease FDA Fast Track designation previously received for AXS-05 for Alzheimers disease agitation. Second indication for AXS-05 in late-stage clinical trials. NEW YORK, July 17, 2017 (GLOBE NEWSWIRE) -- Axsome Therapeutics, Inc. (NASDAQ:AXSM), a clinical-stage biopharmaceutical company developing novel therapies for the management of central nervous system (CNS) disorders, enrolled the first patient in the ADVANCE-1 (Addressing Dementia Via Agitation-Centered Evaluation 1) study, a Phase 2/3 trial evaluating the efficacy and safety of AXS-05 for the treatment of Alzheimers disease (AD) agitation. AXS-05 is a combination of dextromethorphan (an NMDA receptor antagonist, sigma-1 receptor agonist, ...
PR04.MZ 8-(4-fluoro-but-2-ynyl)-3-p-tolyl-8-aza-bicyclo[3.2.1]octane-2-carboxylic acid methyl ester (1) and LBT999 8-((E)-4-fluoro-but-2-enyl)-3b-p-tolyl-8-aza-bicyclo[3.2.1]octane-2beta-carboxylic acid methyl ester (2) are selective dopamine reuptake inhibitors, derived from cocaine. Compounds 1 and 2 were labelled with fluorine-18 at their terminally fluorinated N-substituents employing microwave enhanced direct nucleophilic fluorination. K[(18)F]F(-) Kryptofix 222 cryptate, tetrabutyl ammonium [(18)F]fluoride and caesium [(18)F]fluoride ...
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senior study author Dr. Eric Nestler of New York Citys Mount Sinai School of Medicine said in a statement.. Nestler and colleagues combined highly sensitive genetic isolation and screening techniques to study regulation of gene transcription in the brains of mice repeatedly receiving cocaine. The researchers also found a previously unrecognized family of genes -- called the sirtuins -- involved in cocaine addiction. Chronic cocaine administration was linked with an increase in sirtuin gene transcription while increased sirtuin activity was associated the rewarding effects of cocaine being augmented, while pharmacological inhibition of sirtuins reduced the rewarding effects of cocaine and the motivation to ...
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The only medication Ive taken comparable to Reboxetine in its specificity is desipramine and even that if I recall was as an augmentation for Prozac. But neither reboxetine by itself or desipramine plus Prozac in the long term helped much. Although I got by with plain old Prozac for several years.. If it is stimulation you are looking for I recommend Provigil. For a while there they didnt know how it worked but I was looking at the wiki for it today and I guess they have discovered it is a dopamine reuptake inhibitor. Its stimulating but not like Ritalin or Amphetamine, more mild, but good for attention and energy in general. Regarding ketamine, here in the US ketamine is ...
The only medication Ive taken comparable to Reboxetine in its specificity is desipramine and even that if I recall was as an augmentation for Prozac. But neither reboxetine by itself or desipramine plus Prozac in the long term helped much. Although I got by with plain old Prozac for several years.. If it is stimulation you are looking for I recommend Provigil. For a while there they didnt know how it worked but I was looking at the wiki for it today and I guess they have discovered it is a dopamine reuptake inhibitor. Its stimulating but not like Ritalin or Amphetamine, more mild, but good for attention and energy in general. Regarding ketamine, here in the US ketamine is ...
Patent US6399826 - Salts of sibutramine metabolites, methods of making sibutramine metabolites ... - Google Patents
Methods of making and using racemic and optically pure metabolites of sibutramine, and pharmaceutically acceptable salts, solvates, and clathrates thereof, are disclosed. Pharmaceutical compositions and dosage forms are also disclosed which comprise a dopamine reuptake inhibitor, such as a racemic or optically pure sibutramine metabolite, and optionally an additional pharmacologically active compound.
Does anyone have any information or speculation on what receptors Catuabine D might activate (found in the herb Catuaba) http://www.erowid.org/experiences/exp.php?ID=45399 It looks like it should be a dopamine reuptake inhibitor but I think that might be wishful thinking.
Primary Structure of the Human Platelet Serotonin Uptake Site: Identity with the Brain Serotonin Transporter - Lesch - 1993 -...
Abstract: A cDNA encoding the human platelet serotonin (5-HT) uptake site was isolated and sequenced using the PCR. The cDNA represents a ˜3.1-kb mRNA transcript and contains an open reading frame encoding a hydrophobic polypeptide of 630 amino acids with 12 membrane-spanning segments, a calculated molecular mass of 70,320 Da, and an estimated isoelectrical point of 5.84. The human platelet 5-HT uptake site is identical with the human brain 5-HT transporter and ˜92% homologous to the rat protein. Hydropathicity analysis indicates 12 membrane-spanning segments with two putative glycosylation sites within the second extracellular loop. ...
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All contents Copyright 1999-2017 Genius Central and Moses Kountry Health Foods. All rights reserved. This internet site is hosted by Genius Central, a Web site service provider to natural health stores nationwide. Genius Central and Moses Kountry Health Foods have no means of independently evaluating the safety or functionality of the products offered by their suppliers and affiliates and thus can neither endorse nor recommend products. Information presented is of a general nature for educational and informational purposes only. Statements about products and health conditions have not been evaluated by the US Food and Drug Administration. Products and information presented ...
All contents Copyright 1999-2018 Genius Central and Moses Kountry Health Foods. All rights reserved. This internet site is hosted by Genius Central, a Web site service provider to natural health stores nationwide. Genius Central and Moses Kountry Health Foods have no means of independently evaluating the safety or functionality of the products offered by their suppliers and affiliates and thus can neither endorse nor recommend products. Information presented is of a general nature for educational and informational purposes only. Statements about products and health conditions have not been evaluated by the US Food and Drug Administration. Products and information presented ...
All contents Copyright 1999-2017 Genius Central and Sawall Health Foods. All rights reserved. This internet site is hosted by Genius Central, a Web site service provider to natural health stores nationwide. Genius Central and Sawall Health Foods have no means of independently evaluating the safety or functionality of the products offered by their suppliers and affiliates and thus can neither endorse nor recommend products. Information presented is of a general nature for educational and informational purposes only. Statements about products and health conditions have not been evaluated by the US Food and Drug Administration. Products and information presented ...
Submitted by Annie White on March 2, 2011 Soy is everywhere, from plastics to cosmetics and saturates the food supply in everything from infant formula to prison food to health food. It s inexpensive to grow, and the U.S., with the help of Monsanto, is pumping it out at a dizzying and unfortunately, sickening rate. We produced nearly a hundred million metric tons in 2009. Between 90 and 95 percent of those soybeans were genetically modified which means they were designed to withstand heavy doses of RoundUp Ready that would kill a normal plant. Humans are not Monsanto genetically modified plants; repeated doses of RoundUp Ready in the diet is not ...
The Monitors healthy living festival. McAllen, TX - February 28, 2017. Theres a common misconception that healthy food isnt as tasty or appealing as more fatty and calorie-laden fare. Unfortunately this misunderstanding has resulted in the Rio Grande Valley being named one the nations most obese region, with a very high rate of diabetes.. AIM Media Texas is concerned about the well-being of the region and has taken the lead in promoting healthier living and better eating habits. As such, AIM Media Texas, in conjunction with The Monitor, is producing Por Vida Health & Food ...
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A: The fact that Altoids were being sold in health food stores was important to Debras success. She didnt have to convince the stores to sell a breath mint. She only had to show how she was different. Selling a healthy breath mint in health food stores is a way to get in the flow and this is easier than swimming up stream. The health food stores define themselves by the product mix and pride themselves in making statements like: processed white sugar is bad. Debra is a health food expert and was ...
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Chacko, V and Joseph, B and Mohanty, SP and Jacob, Thomas (1986) Management of Spinal Cord Injury in a General Hospital in Rural India. Paraplegia, 24. pp. 330-335. ISSN 1362-4393 Chacko, Verghese and Joseph, Benjamin and Seetharam, B (1986) Perthes Disease in South India. Clinical Orthopaedics and Related Research (209). pp. 95-99. Jha, S K and Thimmappa, B H S and Mathur, P (1986) A Convenient Synthesis of Fe(CO)2(η2-S2CNMe2)2 and Fe(η2-S2CNMe2)2 from the Monodentate Dithiocarbamato Derivative, [(η5-C5H5)(CO)3W(η1-SCSNMe2)] and Fe2(CO)9. Polyhedron , 5 (12). pp. 2123-2125. ISSN 0277-5387 Nalini, K and Aroor, AR and Kumar, KB and Rao, ...
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In many ways the saying by Hippocrates is true today: "Let thy food be thy medicine and let thy medicine be thy food."This principle can be applied to your eye health. No vision improvement program is complete without the proper nutritional foundation to support better eye health. So, if your taste buds are craving a break from traditional foods good for eyes, here are some foods you never knew that can improve and promote better eyesight.. Beets: When it comes to eye health foods, Beets are good for your eyes as they consist of Lutein and Zeaxanthin, beneficial nutrients that promote the ...
The Daily Mail (4/27, Johnston) reports that "some of the most popular health foods" may negatively affect dental health. The acid content in green smoothies, for example, may damage enamel, while nutrient-rich beetroot may contribute to teeth staining. The article provides several "tooth-friendly" alternatives, recommending whole fruits and vegetables, nuts in moderation, and cheese.. Meanwhile, a second article in the Daily Mail (4/27) states, "People make a number of simple mistakes" that can harm teeth, such as chewing ice cubes, eating dried fruits, using a toothbrush ...
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Posts in the Nutritional Supplements Category at The Health Food Outlaw. Three Important Facts About Nutritional Supplements. In fact, many individuals just waste their money purchasing nutritional supplements. Of course, this is clearly because when they swallow them, they are obviously not fully absorbed. Thus in order for you to be very healthy, you should consume those optimum nutrients which are synergistically balanced and also possess bioavailability.. First of all, lets mention bioavailability. Well, when individuals take nutrients which are in capsule or pill form, such nutrients obviously do not readily break down ...
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Vitamin and mineral B2 is definitely important nutrient which is without difficulty absorbed by way of the body. This is probably the recommended nutritional vitamins pertaining to weight training since it must be used within a variety of cellular techniques in the human body. Vitamin B2 is important intended for flavoproteins, which are needed for metabolism, along with flesh and mobile repair. Each and every personal in the human body employs health food B2 to create vigor, in order to metabolize extra fat, essential fatty acids, suscrose, in addition to protein. It is important towards functionality skin color various other B nutritional vitamins, ...
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R)-(+)-6-Chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine - Alfa Chemistry
R)-(+)-6-Chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine/AFI253446150 can be provided in Alfa Chemistry. We ... Tel:1-201-478-8534. 1-516-662-5404. Fax: 1-516-927-0118. Address: Suite 212, Waverly Plaza, 755 Waverly Avenue, Holtsville, NY ... Tel:1-201-478-8534. 1-516-662-5404. Fax: 1-516-927-0118. Address: Suite 212, Waverly Plaza, 755 Waverly Avenue, Holtsville, NY ... Home > Product > Heterocyclic Organic Compounds > (R)-(+)-6-Chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine ...http://www.alfa-chemistry.com/cas_253446-15-0.htm
8-hydroxy-2-(di-n-propylamino)tetralin). DA. dopamine. DS. discriminative stimulus. NE. norepinephrine. FR. fixed ratio. FRF. ... 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)-piperazine). HDL. high-dose lever. MW. molecular weight. NE. norepinephrine. ... 6-chloro-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine. VTA. ventral tegmental area. ... In all, the results confirm reports that monoamine reuptake blockers enhance the DS effects of cocaine and indicate that 5-HT ...http://jpet.aspetjournals.org/content/284/3/1015
Preconditioning ip injection of the D1/D5 agonist SKF-3 | Open-i
Mentions: Experiment 1 was designed as a pilot study with only 4 gerbils per group for an initial assessment of the role of ... Mentions: Experiment 1 was designed as a pilot study with only 4 gerbils per group for an initial assessment of the role of ... Gerbils were randomly assigned to 1 of 2 groups, A and B, and trained on the FM discrimination task once per day for a total of ... Gerbils were randomly assigned to 1 of 2 groups, A and B, and trained on the FM discrimination task once per day for a total of ...https://openi.nlm.nih.gov/detailedresult.php?img=PMC2567422_cercorbhn026f01_lw&req=4
6-Br-APB - The Full Wiki
Benzazepines: 6-Br-APB • Fenoldopam • SKF-38,393 • SKF-77,434 • SKF-81,297 • SKF-82,958 • SKF-83,959; Ergot-derivatives: ... 6-Br-APB is a synthetic compound that acts as a selective dopamine receptor D1 agonist, with the (R) enantiomer being a ... 2-Fluoroamphetamine • 2-OH-PEA • 2-Phenyl-3-aminobutane • 2-Phenyl-3-methylaminobutane • 2,3-MDA • 3-Fluoroamphetamine • 3- ... 3α-Bis-(4-fluorophenyl)methoxytropane • 3-CPMT • 3-Pseudotropyl-4-fluorobenzoate • Altropane (IACFT) • Brasofensine • CFT (WIN ...http://www.thefullwiki.org/6-Br-APB
1987) [3H]GBR 12935 binding in vivo in mouse brain: Labelling of a piperazine acceptor site. Eur J Pharmacol 144:1-6. ... 6-chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine. THIP. Gaboxadol HCl. WIN 35428. (−)-2-β- ... 1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl)-piperazine. RU 24213. N-n-propyl-N-phenylethyl-1-phenylethylamine. SCH 23390. R ... 1980) Aryl 1,4-dialk(en)ylpiperazines as selective and very potent inhibitors of dopamine uptake. Eur J Med Chem 15:363-370. ...http://jpet.aspetjournals.org/content/284/1/116
Neurochemical evidence of dopamine release by lateral olivocochlear efferents and its presynaptic modulation in guinea-pig...
Piribedil (a D3/D2/D1 agonist), a drug under investigation, known to prevent acoustic trauma or ischaemia-induced hearing loss ... D2 agonists and antagonists failed to modulate the release of dopamine, indicating the lack of negative feedback modulation of ... Our results suggest that the release of dopamine was subjected to modulation by a D1 receptor agonist and an antagonist. In ... The effect of both drugs on stimulation-evoked release could be prevented by SKF-83566 (a selective D1 antagonist). However, ...https://hungary.pure.elsevier.com/en/publications/neurochemical-evidence-of-dopamine-release-by-lateral-olivocochle
F. S., 2018, In : HIV Clinical Trials. 19, 4, p. 158-162 5 p.. Research output: Contribution to journal › Article ... Dopamine inhibits human CD8+ Treg function through D1-like dopaminergic receptors. Nasi, G., Ahmed, T., Rasini, E., Fenoglio, D ... Inflammatory effects of atazanavir/ritonavir versus darunavir/ritonavir in treatment naïve, HIV-1-infected patients. Dentone, C ... Jan 1 2019, In : Journal of virus eradication. 5, 1, p. 47-49 3 p.. Research output: Contribution to journal › Article ...https://moh-it.pure.elsevier.com/en/persons/daniela-fenoglio
Research Interests for Edward D. Levin
Benzazepines, Benzodiazepines, Binding Sites, Binding, Competitive, Biogenic Monoamines, Birth Weight, Blinking, Blood Pressure ... Phenyl Ethers, Phosphinic Acids, Phosphites, Photic Stimulation, Phylogeny, Physical Exertion, Physical Stimulation, ... 4 (July, 2005), pp. 447-453 , [doi] [abs]. *Addy, NA; Pocivavsek, A; Levin, ED, Reversal of clozapine effects on ... 2 (April, 2005), pp. 132-142 , [doi] [abs]. *Levin, ED; Pizarro, K; Pang, WG; Harrison, J; Ramsdell, JS, Persisting ...http://fds.duke.edu/db/aas/pn/faculty/edlevin/research.html
Hypertension sub-cluster 20
1. This study compared the effect of a non-peptide angiotensin II receptor antagonist and a series of clonidine analogues on ... Melatonin and 5-methoxytryptophol were approximately equipotent and a dose of 150 micromol/kg brought about a reduction of ... 1. Effects of the alpha2-adrenoceptor agonist dexmedetomidine on vasoconstrictor and heart rate (HR) responses to acute central ... METHODS AND RESULTS: In 11 healthy subjects (7 men, age 27+/-2 years, body mass index 23.1+/-0.7 kg/m2), we compared the ... ...http://www.biomedsearch.com/cluster/89/Hypertension/sub-20-p6.html
BHSE Centers - Scholarly Works - Arizona State University
Mustard, J. A., Pham, P. M. & Smith, B., Apr 2010, In : Journal of Insect Physiology. 56, 4, p. 422-430 9 p.. Research output: ... Warren, J. P., Santello, M. & Helms Tillery, S., Oct 2010, In : Experimental Brain Research. 206, 4, p. 419-426 8 p.. Research ... Johnston, J. A., Bobich, L. R. & Santello, M., Apr 2010, In : Neuroscience Letters. 474, 2, p. 104-108 5 p.. Research output: ... Brower, J. B., Targovnik, J. H., Caplan, M. & Massia, S., 2010, In : Cytoskeleton. 67, 3, p. 135-141 7 p.. Research output: ...https://asu.pure.elsevier.com/en/organisations/bhse-centers-2/publications/?page=9
Effect of GBR12909 on affective behavior: Distinguishing motivational behavior from antidepressant-like and addiction-like...
Y1 - 2013/4/5. N2 - Rationale: It was recently demonstrated that the priming stimulation effect (PSE) in the runway model of ... 1, 05.04.2013, p. 313-321.. Research output: Contribution to journal › Article ... 2013 Apr 5;243(1):313-321. https://doi.org/10.1016/j.bbr.2012.10.051 ... Behavioural Brain Research, 243(1), 313-321. https://doi.org/10.1016/j.bbr.2012.10.051 ...https://okayama.pure.elsevier.com/en/publications/effect-of-gbr12909-on-affective-behavior-distinguishing-motivatio
Ethanol facilitates glutamatergic transmission to dopamine neurons in the ventral tegmental area<...
Y1 - 2009/1. N2 - The cellular mechanisms underlying alcohol addiction are poorly understood. In several brain areas, ethanol ... The effects of ethanol are mimicked by SKF 38393, a dopamine D1 receptor agonist, and by GBR 12935, a dopamine reuptake ... Finally, 6, 7-dinitroquinoxaline-2, 3-dione (DNQX), an AMPA receptor antagonist, attenuates ethanol-induced excitation of VTA ... Finally, 6, 7-dinitroquinoxaline-2, 3-dione (DNQX), an AMPA receptor antagonist, attenuates ethanol-induced excitation of VTA ...https://asu.pure.elsevier.com/en/publications/ethanol-facilitates-glutamatergic-transmission-to-dopamine-neuron
6-Br-APB - Wikipedia
December 1991). "(+/-)-3-Allyl-6-bromo-7,8-dihydroxy-1-phenyl-2,3,4,5-tetrahydro-1H-3- benzazepin, a new high-affinity D1 ... 275 (3): 1367-74. PMID 8531104. Barrett AC, Miller JR, Dohrmann JM, Caine SB (2004). "Effects of dopamine indirect agonists and ... 116 (1): 9-18. doi:10.1007/BF02244865. PMID 7862937. Weed MR, Woolverton WL (December 1995). "The reinforcing effects of ... 35 (8): 1466-71. doi:10.1021/jm00086a016. PMID 1533424. Rosenzweig-Lipson S, Hesterberg P, Bergman J (September 1994). " ...https://en.wikipedia.org/wiki/6-Br-APB
List of MeSH codes (D03) - Wikipedia
... phenyl)-1h-pyrazol-3-amine MeSH D03.383.129.539.200 --- epirizole MeSH D03.383.129.539.487 --- indazoles MeSH D03.383.129.539. ... phenyl)-, methyl ester MeSH D03.383.725.210 --- dimethindene MeSH D03.383.725.220 --- 2,2-dipyridyl MeSH D03.383.725.227 --- ... phenyl)-, methyl ester MeSH D03.383.725.547.950 --- xanthinol niacinate MeSH D03.383.725.565 --- nicotinyl alcohol MeSH D03.383 ... 2,3,4,5-tetrahydro-8-chloro-3-methyl-5-phenyl-1h-3-benzazepin-7-ol MeSH D03.438.079.800 --- 2,3,4,5-tetrahydro-7,8-dihydroxy-1- ...https://en.wikipedia.org/wiki/List_of_MeSH_codes_(D03)
European Journal of Pharmacology (v.497, #2) | www.chemweb.com
3 H] A-369508 binds with high affinity to the major human dopamine D4 receptor variants D4.2, D4.4 and D4.7 (K d=1.7, 4, and ... In a recent study, racemic 3-(N,N-dimethylamino)butyl-N,N-dimethylcarbamate () was shown to be a potent agonist at neuronal ... 3 H] A-369508 binds to a single, high affinity site on membranes containing the human dopamine D4.4 receptor. When compared to ... 3 H] A-369508 is a useful tool to define the localization and physiological role of dopamine D4 receptors in central nervous ...https://chemweb.com/articles/00142999/04970002
PHARMACOLOGICAL EVIDENCE FOR THE SUBCLASSIFICATION OF CENTRAL DOPAMINE RECEPTORS IN THE RAT, British Journal of Pharmacology |...
... phenyl‐1H‐3‐benzazepine HCl (SK & F 38393) whether injected intracerebrally or peripherally, induced contralateral rotation but ... dihydroxy‐1,2,3,4‐tetrahydronaphthalene (A‐5, 6 DTN, A‐6, 7 DTN) and N,N dipropyl A‐5, 6DTN induced both responses. In contrast ... tetrahydro‐7,8‐dihydroxy‐1‐phenyl‐1H‐3‐benzazepine HCl (SK & F 38393) whether injected intracerebrally or peripherally, induced ... dihydroxy‐1,2,3,4‐tetrahydronaphthalene (A‐5, 6 DTN, A‐6, 7 DTN) and N,N dipropyl A‐5, 6DTN induced both responses. In contrast ...https://www.deepdyve.com/lp/wiley/pharmacological-evidence-for-the-subclassification-of-central-dopamine-kv7Z7BuEvw?impressionId=5c917e092923b&i_medium=docview&i_campaign=references&i_source=references
NAVER Academic > Search...
1998 M Walton et al. Molecular Brain Research cited 8 times Animals, Brain Chemistry, Brain Injuries, genetics, CCAAT-Enhancer- ... 11 Beta-hydroxysteroid dehydrogenase type 2 in the postnatal and adult rat brain.. 1998 A C Robson et al. Molecular Brain ... 1998 A Salminen et al. Molecular Brain Research cited 7 times Animals, Apoptosis, drug effects, Cells, Cultured, Cerebellum, ... 1998 S V van de Witte et al. Molecular Brain Research cited 5 times ...https://academic.naver.com/search.naver?field=3&query=Molecular+Brain+Research+61%EA%B6%8C+1-2%ED%98%B8
Patent USRE40667 - [R-(R*R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl-3-phenyl-4 ... - Google Patents
1H-pyrrole-1-heptanoic acid or (2R-trans)-5-(4-fluoro-phenyl)-2-(1-methylethyl-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H ... 1H-pyrrole-3-carboxamide; and pharmaceutically acceptable salts thereof. ... R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-((1-methylethyl)-3-phenyl-4-[(phenylamino)-carbonyl)]- ... 6-tetrahydro-2H-pyran-2-ones. US4319039. 11 Aug 1980. 9 Mar 1982. Merck & Co., Inc.. Preparation of ammonium salt of ...http://www.google.co.uk/patents/USRE40667
Dopamine-enhancing Medications to Accelerate Emergence from General Anesthesia | Anesthesiology | ASA Publications
The data of Taylor et al .5 and that of others now highlight the importance of DA in arousal. These findings have direct ... D-1 agonist, SKF 38393, but not a D-2 agonist, produces a cholinergically mediated analeptic effect in rabbits. Pharmacol ... In this issue of ANESTHESIOLOGY, Taylor et al .5 report that the dopamine-1 receptor (D1R) agonist 6-chloro-7,8-dihydroxy-3- ... In the previous study, Horita et al .7 also provide evidence that the dopaminergic effects (driven by D1R but presumably ...http://anesthesiology.pubs.asahq.org/article.aspx?articleid=2034687
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Receptors, Dopamine D2/drug effects Substances Benzazepines Dopamine Agonists. Pairing naltrexone with SKF-38393 produced ... Quinpirole Naltrexone 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine Haloperidol Grant Support DA04194/DA/NIDA NIH ... 1994 Sep;49(1 197-204. Hobbs DJ 1, Koch JE, Bodnar RJ. Author information 1Department of Psychology, Queens College, CUNY, ... Both SKF-38393 (5-10 mg/kg) and SCH-23390 (100-200 micrograms/kg) significantly and dose dependently reduced deprivation- ...http://naltrexoneinfo.com/naltrexone-dopamine-agonist/
Block by apomorphine of acetylcholine receptor channels expressed in Xenopus oocytes<...
1H)-3-benzazepine-7,8-diol; dopamine D1 receptor agonist; 3 and 30 μM), quinpirole (dopamine D2 receptor agonist; 30 μM), ... 1H)-3-benzazepine-7,8-diol; dopamine D1 receptor agonist; 3 and 30 μM), quinpirole (dopamine D2 receptor agonist; 30 μM), ... 1H)-3-benzazepine-7,8-diol; dopamine D1 receptor agonist; 3 and 30 μM), quinpirole (dopamine D2 receptor agonist; 30 μM), ... 1H)-3-benzazepine-7,8-diol; dopamine D1 receptor agonist; 3 and 30 μM), quinpirole (dopamine D2 receptor agonist; 30 μM), ...https://kyushu-u.pure.elsevier.com/en/publications/block-by-apomorphine-of-acetylcholine-receptor-channels-expressed
Interaction between the NMDA competitive antagonist CPP and the dopaminergic system in one-trial inhibitory avoidance in C57BL...
Mele A1, Castellano C, Cestari V, Oliverio A.. Author information. 1. Dipartimento di Genetica e Biologia Molecolare, ... Neurobiol Learn Mem. 1995 Mar;63(2):143-8.. Interaction between the NMDA competitive antagonist CPP and the dopaminergic system ... Furthermore, subchronic blockade of dopamine receptor through a 10-day daily treatment with 4 mg/kg of haloperidol induced an ...https://www.ncbi.nlm.nih.gov/pubmed/7663887?dopt=Abstract
Skf-38393,N-allyl-,hydrobromide d1dopamine agonist - Alfa Chemistry
Tel:1-201-478-8534. 1-516-662-5404. Fax: 1-516-927-0118. Address: 2200 Smithtown Avenue, Room 1 Ronkonkoma, NY 11779-7329 USA ... Tel:1-201-478-8534. 1-516-662-5404. Fax: 1-516-927-0118. Address: 2200 Smithtown Avenue, Room 1 Ronkonkoma, NY 11779-7329 USA ... Skf-38393,N-allyl-,hydrobromide d1dopamine agonist , CAS Number: 300561-58-4. ... 8-Dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide, 1-phenyl-3-prop-2-en-1-yl-2,3,4,5-tetrahydro-1H- ...http://www.alfa-chemistry.com/cas_300561-58-4.htm
What does 2,3-diketogulonic acid mean?
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Dopamine D1-Dependent Trafficking of Striatal N-Methyl-D-aspartate Glutamate Receptors Requires Fyn Protein Tyrosine Kinase but...
6-chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4, 5-tetra-hydro-1H-benzazepine] produced redistribution of NMDA receptors from ... a potent and selective inhibitor of protein phosphatase-1, or the protein tyrosine kinase Fyn. In striatal tissue from DARPP-32 ...http://scholars.uab.edu/display/pub726829
ReceptorsPharmacologyAntagonistEthylReceptor agonistAgonistsAgonistInhibitors1995Brain ResearchAtropineStimulationApomorphineAcidHaloperidolContrast1999PharmacologicalPotenciesRacloprideSelectiveJournalEffectsGeneBinds1994DosageSignalCompoundsDrugResearchGlutamateNeuroscienceCellsRegulationProteinTimes
- Furthermore, negative feedback on the stimulation-evoked release of dopamine via D 2 dopamine receptors has been excluded. (elsevier.com)
- In addition, it is concluded that D 2 receptors are not involved in the modulation of dopamine release. (elsevier.com)
- Using knockout mice, we have found that β2-containinc nicotinic receptors appear to be more important for the initiation of nicotine self-administration during the first few weeks, whereas α7 nicotinic receptors appear to be more important for the long-term consumption of nicotine over a period of 5 months. (duke.edu)
- The EPSCs were mediated by glutamate α-amino-3-hydroxy-5- methylisoxazole-4-propionic acid (AMPA) receptors. (elsevier.com)
- We therefore conclude that, acting via presynaptic D 1 receptors, ethanol at low concentrations increases glutamate release in the VTA, thus raising somatodendritic dopamine release, which further activates the presynaptic D 1 receptors. (elsevier.com)
- 5 The results provide evidence that contralateral rotation induced by dopamine receptor agonists is mediated by two different classes of dopamine receptors and that these receptors differ from those mediating the stereotypy response. (deepdyve.com)
- In a recent study, racemic 3-( N , N- dimethylamino)butyl- N , N -dimethylcarbamate () was shown to be a potent agonist at neuronal nicotinic acetylcholine receptors with a high selectivity for nicotinic over muscarinic acetylcholine receptors [Mol. (chemweb.com)
- Somatic application of GABA induced currents which were partially suppressed by (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid (TPMPA), a specific antagonist of GABA C receptors. (chemweb.com)
- Tritiation of the dopamine D 4 receptor selective agonist A-369508 ([2-[4-(2-cyanophenyl)-1-piperazinyl]- N -(3-methylphenyl) acetamide) has provided a radioligand for the characterization of dopamine D 4 receptors. (chemweb.com)
- It also binds to the rat dopamine D 4 receptor, ( K d =4.4 nM), implying similar binding affinity across human and rat receptors. (chemweb.com)
- 3 H ] A-369508 is a useful tool to define the localization and physiological role of dopamine D 4 receptors in central nervous system and can facilitate measuring accurate affinities ( K i ) for structure/activity relationship studies designed to identify dopamine D 4 receptor selective agonists. (chemweb.com)
- Receptors, Dopamine D2/drug effects Substances Benzazepines Dopamine Agonists. (naltrexoneinfo.com)
- In striatal tissue from DARPP-32-depleted mice, basal tyrosine and serine phosphorylation of striatal NMDA receptor subunits NR1, NR2A, and NR2B was normal, and activation of dopamine D1 receptors with the agonist SKF-82958 [(±)-6-chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4, 5-tetra-hydro-1H-benzazepine] produced redistribution of NMDA receptors from vesicular compartments (P3 and LP2) to synaptosomal membranes (LP1). (uab.edu)
- The dopamine D 1 receptor belongs to the superfamily of heptahelical receptors that modulate the activity of effectors such as adenylate cyclase by activation of specific heterotrimeric GTP-binding proteins (G proteins). (aspetjournals.org)
- The Journal of Pharmacology and Experimental Therapeutics 275 (3): 1367-74. (thefullwiki.org)
- Gov't, P.H.S. MeSH Terms 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine/pharmacology Animals Benzazepines/pharmacology Dopamine Agonists/pharmacology Dopamine Antagonists/pharmacology. (naltrexoneinfo.com)
- European Journal of Pharmacology: Molecular Pharmacology , 269 (3), 375-379. (elsevier.com)
- Nakazawa, K, Akiyama, T & Inoue, K 1994, ' Block by apomorphine of acetylcholine receptor channels expressed in Xenopus oocytes ', European Journal of Pharmacology: Molecular Pharmacology , vol. 269, no. 3, pp. 375-379. (elsevier.com)
- However, pretreatment with the alpha -1 adrenergic antagonist prazosin failed to alter completely the ability of desipramine to enhance the DS effects of the low training dose of cocaine, but did produce dose-related decreases in the cocaine-enhancing effects of the beta adrenergic antagonist propranolol (10 mg/kg i.p. (aspetjournals.org)
- Positive modulation of dopamine release has been shown by a D 1 dopamine receptor agonist, an antagonist and piribedil. (elsevier.com)
- The effect of both drugs on stimulation-evoked release could be prevented by SKF-83566 (a selective D 1 antagonist). (elsevier.com)
- Our results suggest that the release of dopamine was subjected to modulation by a D 1 receptor agonist and an antagonist. (elsevier.com)
- Fiduxosin is an alpha(1)-adrenoceptor antagonist with higher affinity for alpha(1A)-adrenoceptors and for alpha(1D)-adrenoceptors than for alpha(1B)-adrenoceptors. (biomedsearch.com)
- The effects of ethanol are mimicked by SKF 38393, a dopamine D 1 receptor agonist, and by GBR 12935, a dopamine reuptake inhibitor, and they are blocked by SKF 83566, a D 1 antagonist, or by reserpine, which depletes dopamine stores. (elsevier.com)
- When compared to the D 2 -like antagonist [ 3 H ] spiperone, competition binding for agonists like dopamine and apomorphine were 2-10-fold more potent with [ 3 H ] A-369508, while the antagonists clozapine, haloperidol and L-745870 bind with similar affinity to both ligands. (chemweb.com)
- 7 investigated the effects of a D1R agonist (1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol) and a D2R antagonist (raclopride) on duration of phenobarbital anesthesia in rats (administered only 20 min after induction with 40 mg/kg intraperitoneal phenobarbital to reduce pharmacokinetic effects on emergence). (asahq.org)
- 7 reported that the D2R antagonist raclopride and atropine also reversed the effect of the D1R agonist. (asahq.org)
- We then assessed the contribution of the basal ganglia motor loops to these impairments, using open field testing and analysis of drug-induced locomotor responses to the psychostimulant cocaine, the benzazepine D 1 receptor agonists SKF83822 and SKF83959, and the NMDA receptor antagonist MK-801. (frontiersin.org)
- D 1 -EGFP was similar to the untagged D 1 receptor in terms of affinity for agonist and antagonist ligands, coupling to G proteins, and stimulation of cyclic AMP accumulation. (aspetjournals.org)
- 3. A compound of claim 1 which is (2R-trans)-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide. (google.co.uk)
- Trans-( )-5-(4-fluorophenyl)-2-(1-methylethyl)-N,4-diphenyl-1-[2-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamides are among compounds of U.S. Pat. (google.co.uk)
- Pretreatment with the protein kinase A inhibitor H-89 ( N -[2-( p -bromocinnamylamino)ethyl]-5-isoquinolinesulfonamide) or substitution of Ala for Thr268 reduced agonist-stimulated phosphorylation of the receptor and resulted in diminished trafficking of the receptor to the perinuclear region of the cell. (aspetjournals.org)
- Here, we report that the D1/D5 dopamine receptor agonist SKF-38393 substantially improved gerbils' FM discrimination learning when administered systemically or locally into the auditory cortex shortly before, shortly after, or 1 day before conditioning. (nih.gov)
- The dopamine D1 receptor agonist (+/-)-6-chloro-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide (SKF 82958) produced effects comparable to cocaine. (biomedsearch.com)
- This sensitivity was enhanced when we evoked the currents by the GABA C receptor agonist cis -4-aminocrotonic acid (CACA). (chemweb.com)
- [ 2 ] (R)-6-Br-APB and similar D 1 -selective full agonists like SKF-81297 and SKF-82958 produce characteristic anorectic effects, stereotyped behaviour and self-administration in animals, with a similar but not identical profile to that of dopaminergic stimulant drugs such as amphetamine. (thefullwiki.org)
- D 2 agonists and antagonists failed to modulate the release of dopamine, indicating the lack of negative feedback modulation of dopamine release. (elsevier.com)
- MARRIOTT, A.S. 1982-09-01 00:00:00 1 The relative potencies of dopamine receptor agonists in causing stereotypy in rats when injected into the olfactory tubercles, and contralateral rotation when injected unilaterally into the caudate nucleus of rats with lesions of the nigro‐striatal dopamine pathway, were determined. (deepdyve.com)
- 6-Br-APB is a synthetic compound that acts as a selective dopamine receptor D 1 agonist, [ 1 ] with the (R) enantiomer being a potent full agonist , while the (S) enantiomer retains its D 1 selectivity but is a weak partial agonist . (thefullwiki.org)
- SKF-38393 (a selective D 1 agonist) increased both the resting and electrically evoked release of dopamine. (elsevier.com)
- Piribedil (a D 3 /D 2 /D 1 agonist), a drug under investigation, known to prevent acoustic trauma or ischaemia-induced hearing loss, had a similar and concentration-dependent increasing effect on both resting and evoked release of dopamine. (elsevier.com)
- PURPOSE: Clonidine, an alpha(2)-adrenergic agonist, raises blood pressure in patients with autonomic failure, in whom failure of reflex neurogenic venoconstriction leads to severe orthostatic hypotension. (biomedsearch.com)
- Agonist activity determined by inhibition of forskolin-induced cAMP in Chinese hamster ovary cells transfected with the human dopamine D 4.4 receptor (EC 50 =7.5 nM, intrinsic activity=0.71) indicates that A-369508 is a potent agonist at the human dopamine D 4 receptor. (chemweb.com)
- 5 report that the dopamine-1 receptor (D1R) agonist 6-chloro-7,8-dihydroxy-3-allyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrobromide but not the D2R agonist quinpirole reduces the time to emergence from isoflurane anesthesia in rats by 85% compared with placebo. (asahq.org)
- 5 showed decreases in the time from emergence of anesthesia in the rats treated with the D2R agonist quinpirole (from 330 to 189 s) and had their sample (n = 6) been larger, this effect may have been significant. (asahq.org)
- The aim of this study was to use pharmacological inhibition of protein kinase A and mutation of potential protein kinase A phosphorylation sites to determine the role of protein kinase A-catalyzed phosphorylation of the dopamine D 1 receptor in agonist-stimulated desensitization and internalization of the receptor. (aspetjournals.org)
- Electrical stimulation of the cochlear tissue produced a significant and reproducible release of [ 3 H]dopamine, which could be blocked by tetrodotoxin (1 μM) and cadmium (100 μM), proving that axonal activity releases dopamine and its dependence on Ca 2+ influx verifies its neuronal origin. (elsevier.com)
- Nomifensine, a high-affinity dopamine uptake blocker, prevented the tissue from taking up [ 3 H]dopamine from the bathing solution, also indicating the neural origin of dopamine released in response to stimulation. (elsevier.com)
- 3 Contralateral rotation and stereotypy induced by apomorphine or N,N dipropyl A‐5, 6 DTN were inhibited by haloperidol, pimozide and fluphenazine but these drugs failed to inhibit rotation induced by SK & F 38393. (deepdyve.com)
- When channels were expressed with a combination of α 3 and β 4 subunits, acetylcholine activated an inward current, and apomorphine suppressed the current in a concentration-dependent manner with an IC 50 value of about 3 μM. (elsevier.com)
- The inhibition by apomorphine of the acetylcholine-activated current was also apparent when α 3 subunit was combined with β 2 subunit instead of β 4 subunit, or β 4 subunit was combined with α 2 or α 4 subunit instead of α 3 subunit to express channels. (elsevier.com)
- When channels were expressed with a combination of α3 and β4 subunits, acetylcholine activated an inward current, and apomorphine suppressed the current in a concentration-dependent manner with an IC50 value of about 3 μM. (elsevier.com)
- 2. A compound of claim 1 which is [R-(R*R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid. (google.co.uk)
- What does 2,3-diketogulonic acid mean? (definitions.net)
- Here are all the possible meanings and translations of the word 2,3-diketogulonic acid . (definitions.net)
- Are we missing a good definition for 2,3-diketogulonic acid ? (definitions.net)
- What rhymes with 2,3-diketogulonic acid ? (definitions.net)
- Quinpirole Naltrexone 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine Haloperidol Grant Support DA04194/DA/NIDA NIH HHS/United States DA07135/DA/NIDA NIH HHS/United States LinkOut - more resources). (naltrexoneinfo.com)
- Furthermore, subchronic blockade of dopamine receptor through a 10-day daily treatment with 4 mg/kg of haloperidol induced an adaptation of both the dopaminergic and the glutamatergic system. (nih.gov)
- All the monoamine reuptake blockers produced high-dose-appropriate responding in a dose-related manner when combined with a low dose of cocaine, but compounds from other pharmacological classes (benztropine, caffeine, diazepam, or 8-hydroxy-2-(di-n-propylamino)tetralin) did not enhance the DS effects of cocaine. (aspetjournals.org)
- Here we present the synthesis and pharmacological characterization of a series of analogs of , where the methyl group at C-3 has been replaced by different alkyl substituents. (chemweb.com)
- To unravel the signaling pathways underlying this trafficking, we studied mice with targeted disruptions of either the gene that encodes the dopamine- and cAMP-regulated phosphoprotein (DARPP-32), a potent and selective inhibitor of protein phosphatase-1, or the protein tyrosine kinase Fyn. (uab.edu)
- In all, the results confirm reports that monoamine reuptake blockers enhance the DS effects of cocaine and indicate that 5-HT and DA can effectively modulate the DS effects of cocaine, but suggest that NE interactions may be relatively less important in the rat. (aspetjournals.org)
- 4 The molecular mechanisms for these effects are still incompletely understood. (asahq.org)
- Phenylethanolamine N-methyltransferase gene expression: synergistic activation by Egr-1, AP-2 and the glucocorticoid receptor. (naver.com)
- 5. The DNA construct as claimed in claim 1, further comprising at least one selectable marker gene, said at least one selectable marker gene being disposed within said construct so as not to disrupt expression of said DNA segment and encoding a protein conferring resistance to a selection agent. (google.com)
- 6. The DNA construct as claimed in claim 5, wherein said selectable marker gene confers resistance to a selection agent selected from the group consisting of hygromycin, neomycin, ampicillin, spectinomycin, and streptomycin. (google.com)
- c) a 3' polyadenylation signal sequence, operably linked to said DNA segment. (google.com)
- 4. The DNA construct as claimed in claim 1, wherein said 3' polyadenylation signal sequence is selected from the group consisting of bovine growth hormone polyadenylation signal sequences and thymidine kinase polyadenylation signal sequences. (google.com)
- Second, a better understanding of the neuronal mechanisms by which DA increases the emergence from anesthesia will also help in the management of patients with DA abnormalities as may be the case for patients with Parkinson disease, schizophrenic patients treated with depot neuroleptics (long-acting dopamine-2 receptor [D2R] antagonists) and drug abusers. (asahq.org)
- To facilitate purification and imaging of the D 1 receptor, we attached a polyhistidine tag to the amino terminus and enhanced green fluorescent protein to the carboxyl terminus of the receptor (D 1 -EGFP). (aspetjournals.org)
- We conclude that protein kinase A-dependent phosphorylation of the D 1 receptor on Thr268 regulates a late step in the sorting of the receptor to the perinuclear region of the cell, but that phosphorylation of Thr268 is not required for receptor sequestration or maximal desensitization of cyclic AMP accumulation. (aspetjournals.org)