Compounds with BENZENE fused to AZEPINES.
A selective D1 dopamine receptor agonist used primarily as a research tool.
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.
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.
Drugs that bind to and activate dopamine receptors.
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.
A dopamine D2/D3 receptor agonist.
Cholecalciferols substituted with two hydroxy groups in any position.
Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.
Hydroxy analogs of vitamin D 3; (CHOLECALCIFEROL); including CALCIFEDIOL; CALCITRIOL; and 24,25-DIHYDROXYVITAMIN D 3.
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.
Eighteen carbon fatty acids that comprise the great majority of CASTOR OIL, which is from the seed of RICINUS.
The physiologically active form of vitamin D. It is formed primarily in the kidney by enzymatic hydroxylation of 25-hydroxycholecalciferol (CALCIFEDIOL). Its production is stimulated by low blood calcium levels and parathyroid hormone. Calcitriol increases intestinal absorption of calcium and phosphorus, and in concert with parathyroid hormone increases bone resorption.
A bile salt formed in the liver by conjugation of deoxycholate with taurine, usually as the sodium salt. It is used as a cholagogue and choleretic, also industrially as a fat emulsifier.
The observable response an animal makes to any situation.
(2S-(2 alpha,3 beta(1E,3E,5Z,8Z)))-3-(1,3,5,8-Tetradecatetraenyl)oxiranebutanoic acid. An unstable allylic epoxide, formed from the immediate precursor 5-HPETE via the stereospecific removal of a proton at C-10 and dehydration. Its biological actions are determined primarily by its metabolites, i.e., LEUKOTRIENE B4 and cysteinyl-leukotrienes. Alternatively, leukotriene A4 is converted into LEUKOTRIENE C4 by glutathione-S-transferase or into 5,6-di-HETE by the epoxide-hydrolase. (From Dictionary of Prostaglandins and Related Compounds, 1990)
The relationship between the dose of an administered drug and the response of the organism to the drug.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
A bile salt formed in the liver by conjugation of deoxycholate with glycine, usually as the sodium salt. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and choleretic.
A bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.
A bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.
Enzymes catalyzing the oxidation of arachidonic acid to hydroperoxyarachidonates. These products are then rapidly converted by a peroxidase to hydroxyeicosatetraenoic acids. The positional specificity of the enzyme reaction varies from tissue to tissue. The final lipoxygenase pathway leads to the leukotrienes. EC 1.13.11.- .
Placing of a hydroxyl group on a compound in a position where one did not exist before. (Stedman, 26th ed)
The product of conjugation of cholic acid with taurine. Its sodium salt is the chief ingredient of the bile of carnivorous animals. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as a cholagogue and cholerectic.
Proteins, usually found in the cytoplasm, that specifically bind calcitriol, migrate to the nucleus, and regulate transcription of specific segments of DNA with the participation of D receptor interacting proteins (called DRIP). Vitamin D is converted in the liver and kidney to calcitriol and ultimately acts through these receptors.
The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Chromatography on thin layers of adsorbents rather than in columns. The adsorbent can be alumina, silica gel, silicates, charcoals, or cellulose. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.
Enzymes that catalyze the breakage of a carbon-oxygen bond leading to unsaturated products via the removal of water. EC 4.2.1.
Organic compounds containing both the hydroxyl and carboxyl radicals.
Fractionation of a vaporized sample as a consequence of partition between a mobile gaseous phase and a stationary phase held in a column. Two types are gas-solid chromatography, where the fixed phase is a solid, and gas-liquid, in which the stationary phase is a nonvolatile liquid supported on an inert solid matrix.
A group of 1,2-benzenediols that contain the general formula R-C6H5O2.
An analytical method used in determining the identity of a chemical based on its mass using mass analyzers/mass spectrometers.
The location of the atoms, groups or ions relative to one another in a molecule, as well as the number, type and location of covalent bonds.
An epimer of chenodeoxycholic acid. It is a mammalian bile acid found first in the bear and is apparently either a precursor or a product of chenodeoxycholate. Its administration changes the composition of bile and may dissolve gallstones. It is used as a cholagogue and choleretic.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
The 3 alpha,7 alpha,12 alpha-trihydroxy-5 beta-cholanic acid family of bile acids in man, usually conjugated with glycine or taurine. They act as detergents to solubilize fats for intestinal absorption, are reabsorbed by the small intestine, and are used as cholagogues and choleretics.
A microanalytical technique combining mass spectrometry and gas chromatography for the qualitative as well as quantitative determinations of compounds.
An essential branched-chain aliphatic amino acid found in many proteins. It is an isomer of LEUCINE. It is important in hemoglobin synthesis and regulation of blood sugar and energy levels.
An emulsifying agent produced in the LIVER and secreted into the DUODENUM. Its composition includes BILE ACIDS AND SALTS; CHOLESTEROL; and ELECTROLYTES. It aids DIGESTION of fats in the duodenum.
An enzyme of the oxidoreductase class primarily found in PLANTS. It catalyzes reactions between linoleate and other fatty acids and oxygen to form hydroperoxy-fatty acid derivatives.
The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
Uptake of substances through the lining of the INTESTINES.
The rate dynamics in chemical or physical systems.
Ethers that are linked to a benzene ring structure.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
Widely distributed enzymes that carry out oxidation-reduction reactions in which one atom of the oxygen molecule is incorporated into the organic substrate; the other oxygen atom is reduced and combined with hydrogen ions to form water. They are also known as monooxygenases or hydroxylases. These reactions require two substrates as reductants for each of the two oxygen atoms. There are different classes of monooxygenases depending on the type of hydrogen-providing cosubstrate (COENZYMES) required in the mixed-function oxidation.
A nutritional condition produced by a deficiency of VITAMIN D in the diet, insufficient production of vitamin D in the skin, inadequate absorption of vitamin D from the diet, or abnormal conversion of vitamin D to its bioactive metabolites. It is manifested clinically as RICKETS in children and OSTEOMALACIA in adults. (From Cecil Textbook of Medicine, 19th ed, p1406)
A conditionally essential nutrient, important during mammalian development. It is present in milk but is isolated mostly from ox bile and strongly conjugates bile acids.
The portion of the GASTROINTESTINAL TRACT between the PYLORUS of the STOMACH and the ILEOCECAL VALVE of the LARGE INTESTINE. It is divisible into three portions: the DUODENUM, the JEJUNUM, and the ILEUM.
A chemical reaction in which an electron is transferred from one molecule to another. The electron-donating molecule is the reducing agent or reductant; the electron-accepting molecule is the oxidizing agent or oxidant. Reducing and oxidizing agents function as conjugate reductant-oxidant pairs or redox pairs (Lehninger, Principles of Biochemistry, 1982, p471).
The movement of materials across cell membranes and epithelial layers against an electrochemical gradient, requiring the expenditure of metabolic energy.
A vitamin that includes both CHOLECALCIFEROLS and ERGOCALCIFEROLS, which have the common effect of preventing or curing RICKETS in animals. It can also be viewed as a hormone since it can be formed in SKIN by action of ULTRAVIOLET RAYS upon the precursors, 7-dehydrocholesterol and ERGOSTEROL, and acts on VITAMIN D RECEPTORS to regulate CALCIUM in opposition to PARATHYROID HORMONE.
A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.
Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Organic, monobasic acids derived from hydrocarbons by the equivalent of oxidation of a methyl group to an alcohol, aldehyde, and then acid. Fatty acids are saturated and unsaturated (FATTY ACIDS, UNSATURATED). (Grant & Hackh's Chemical Dictionary, 5th ed)
The restriction of a characteristic behavior, anatomical structure or physical system, such as immune response; metabolic response, or gene or gene variant to the members of one species. It refers to that property which differentiates one species from another but it is also used for phylogenetic levels higher or lower than the species.
The principal sterol of all higher animals, distributed in body tissues, especially the brain and spinal cord, and in animal fats and oils.
A dual inhibitor of both cyclooxygenase and lipoxygenase pathways. It exerts an anti-inflammatory effect by inhibiting the formation of prostaglandins and leukotrienes. The drug also enhances pulmonary hypoxic vasoconstriction and has a protective effect after myocardial ischemia.
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.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
A dihydropyridine derivative, which, in contrast to NIFEDIPINE, functions as a calcium channel agonist. The compound facilitates Ca2+ influx through partially activated voltage-dependent Ca2+ channels, thereby causing vasoconstrictor and positive inotropic effects. It is used primarily as a research tool.
Elements of limited time intervals, contributing to particular results or situations.
Derivatives of phenylacetic acid. Included under this heading are a variety of acid forms, salts, esters, and amides that contain the benzeneacetic acid structure. Note that this class of compounds should not be confused with derivatives of phenyl acetate, which contain the PHENOL ester of ACETIC ACID.
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). " ...
... 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 D03.383.725.547.950 - xanthinol niacinate MeSH D03.383.725.565 - nicotinyl alcohol MeSH D03.383. ... phenyl)-, methyl ester MeSH D03.383.725.210 - dimethindene MeSH D03.383.725.220 - 2,2'-dipyridyl MeSH D03.383.725.227 - ... 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- ...
Some of the benzazepines have high intrinsic activity whereas others do not. In 2015 the first positive allosteric modulator ... 1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human ... 12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline: synthesis, resolution, and preliminary pharmacological characterization of a new ... Benzazepine derivatives SCH-23,390 - 100-fold selectivity for D1 over D5 Ecopipam (SCH-39,166) - a selective D1/D5 antagonist ...
2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine*2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine ... "2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine" is a descriptor in the National Library of Medicines controlled ... Below are the most recent publications written about "2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine" by people in ... This graph shows the total number of publications written about "2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine" by ...
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 ...
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 ...
... the present study describes a common change in synaptic regulation of dopamine cells in the ventral tegmental area 1 week … ... DOI: 10.1016/s0896-6273(00)80082-3 Abstract The mesolimbic system is known to play a role in self-administration of opioids and ... 1 The Vollum Institute, Oregon Health Sciences University L474, Portland, 97201, USA. ... the present study describes a common change in synaptic regulation of dopamine cells in the ventral tegmental area 1 week after ...
Benzazepines / pharmacology * Centrifugation, Density Gradient * Dopamine / pharmacology* * Dopamine Agents / pharmacology * ... Inhibition of Na+,K(+)-ATPase in rat renal proximal tubules by dopamine involved DA-1 receptor activation Naunyn Schmiedebergs ... Incubation with fenoldopam (10(-5) to 10(-8) mol/l) in the presence of SK&F 89124 (10(-6) mol/l) inhibited Na+,K(+)-ATPase ... We found that, in the lower concentration range (10(-5) to 10(-7) mol/l), dopamine-induced inhibition of Na+,K(+)-ATPase ...
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 ...
0 (Benzazepines); 0 (Isotonic Solutions); 0 (Receptors, Dopamine D1); 0 (Receptors, Vasopressin); 0 (SCH 23390); 0 ( ... 1h after the training phase (consolidation design); retention performance was tested 24h post-training. We found that ... 2,3,4,5-Tetra-Hidro-7,8-Di-Hidroxi-1-Fenil-1H-3-Benzazepina/farmacologia. Dopamina/metabolismo. Neostriado/efeitos dos f rmacos ... 0 (Vasoconstrictor Agents); 50VV3VW0TI (Atenolol); 56-59-7 (Felypressin); YKH834O4BH (Epinephrine). [Em] M s de entrada:. 1507 ...
1H]-3-benzazepine (0.3-3.0 mg/kg) produced either no effect or promoted hyperactivity. Thirty minutes after administration of a ... D2, but Not D1 Dopamine Receptor Agonists Potentiate Cannabinoid-Induced Sedation in Nonhuman Primates , Justin P. Meschler, ... D2, but Not D1 Dopamine Receptor Agonists Potentiate Cannabinoid-Induced Sedation in Nonhuman Primates , Justin P. Meschler, ... D2, but Not D1 Dopamine Receptor Agonists Potentiate Cannabinoid-Induced Sedation in Nonhuman Primates , Justin P. Meschler, ...
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,[1] 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 ...
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 ...
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 ... ...
6-dihydroxy-3-phenyl-1H-2-benzopyran hydrochloride (A-68930), like SKF-38393, produced a dose-dependent, D1-selective increase ... Administration of the selective D1-dopamine receptor agonist 2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine (SKF- ... The full D1-dopamine agonist l,(R,S)1-aminomethyl-3,4-dihydro-5, ...
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). " ...
... 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 D03.383.725.547.950 - xanthinol niacinate MeSH D03.383.725.565 - nicotinyl alcohol MeSH D03.383. ... phenyl)-, methyl ester MeSH D03.383.725.210 - dimethindene MeSH D03.383.725.220 - 2,2-dipyridyl MeSH D03.383.725.227 - ... 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- ...
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 [15971025], [doi] [abs]. *Addy, NA; Pocivavsek, A; Levin, ED, Reversal of clozapine effects on ... 2 (April, 2005), pp. 132-142 [15829222], [doi] [abs]. *Levin, ED; Pizarro, K; Pang, WG; Harrison, J; Ramsdell, JS, Persisting ...
11b-tetrahydro-1H-naph[1,2,3-de]isoquinoline: A potent full dopamine D1 agonist containing a rigid β-phenyldopamine ... 9-Dihydroxy-1,2,3,11b-tetrahydrochromeno[4,3,2,-de]isoquinoline (dinoxyline), a high affinity and potent agonist at all ... benzazepine, 6,7-Dihydroxy-1,2,3,4,8,12b-hexahydroanthr[10,4a,4-cd]azepine, and 10-(Aminomethyl)-9,10-dihydro-1,2- ... D1 dopamine receptors. Huang, X., Lawler, C. P., Lewis, M. M., Nichols, D. E. & Mailman, R. B., Jan 1 2001, In : International ...
... phenyl1H3benzazepine HCl (SK & F 38393) whether injected intracerebrally or peripherally, induced contralateral rotation but ... dihydroxy1,2,3,4‐tetrahydronaphthalene (A‐5, 6 DTN, A‐6, 7 DTN) and N,N dipropyl A‐5, 6DTN induced both responses. In contrast ... tetrahydro7,8dihydroxy1phenyl1H3benzazepine HCl (SK & F 38393) whether injected intracerebrally or peripherally, induced ... dihydroxy1,2,3,4‐tetrahydronaphthalene (A‐5, 6 DTN, A‐6, 7 DTN) and N,N dipropyl A‐5, 6DTN induced both responses. In contrast ...
Fingerprint Dive into the research topics of Stimulation of dopamine D2/D3 but not D1 receptors in the central amygdala decreases cocaine-seeking behavior. Together they form a unique fingerprint. ...
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 ...
Fingerprint Dive into the research topics of D1-D2 interaction in feedback control of midbrain dopamine neurons. Together they form a unique fingerprint. ...
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, ...
Ueda, A., Yamamoto, M. & Hirose, N., Apr 1 2011, In : Polar Science. 5, 1, p. 1-10 10 p.. Research output: Contribution to ... Nakanishi, H., Jan 1 1994, In : Physical Review E. 49, 6, p. 5412-5419 8 p.. Research output: Contribution to journal › Article ... Kira, J. I., Dec 1 2010, In : Clinical Neurology. 50, 11, p. 788-793 6 p.. Research output: Contribution to journal › Article ... Inomata, N., Shibata, H., Okuyama, E. & Yamazaki, T., Jan 1 1995, In : Genetics. 141, 1, p. 237-244 8 p.. Research output: ...
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 ...
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 ...
Xu, J., Xie, X., Chen, H., Zou, J., Xue, Y., Ye, N., Shi, P. Y. & Zhou, J., Jun 1 2020, In: Bioorganic and Medicinal Chemistry ... Deer, R. R., Akhverdiyeva, L., Kuo, Y. F. & Volpi, E., Jul 2020, In: Clinical Nutrition. 39, 7, p. 2233-2237 5 p.. Research ... Defever, K., Platz, E. A., Lopez, D. S. & Mondul, A. M., Sep 1 2020, In: Cancer Causes and Control. 31, 9, p. 851-860 10 p.. ... Langsjoen, R. M., Muruato, A. E., Kunkel, S. R., Jaworski, E. & Routh, A., Jul 1 2020, In: mBio. 11, 4, p. 1-20 20 p., e00731- ...
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: ...
Pacheco, L. D., Saad, A. F. & Saade, G., Jul 2020, In: Obstetrics and gynecology. 136, 1, p. 42-45 4 p.. Research output: ... OKeefe, M. E., Jan 1 2020, In: Nursing forum. 55, 1, p. 3 1 p.. Research output: Contribution to journal › Letter › peer- ... Langsjoen, R. M., Muruato, A. E., Kunkel, S. R., Jaworski, E. & Routh, A., Jul 1 2020, In: mBio. 11, 4, p. 1-20 20 p., e00731- ... Prasad, A. N., Ronk, A. J., Widen, S. G., Wood, T. G., Basler, C. F. & Bukreyev, A., Mar 1 2020, In: Journal of virology. 94, 6 ...
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 ...
1H-3-Benzazepine-7,8-diol, 2,3,4,5-tetrahydro-1-phenyl-. R-SK&F 38393. RSK&F 38393. SK&F 38393. SK&F-38393. SK&F38393. SKF ... Benzazepines (1966-1989). Dopaminergic Agents (1989). Public MeSH Note:. 2005; see SK&F-38393 1989-2004. ... 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine - Preferred Concept UI. M0362415. ... 5-Tetrahidro-7,8-dihidroxi-1-fenil-1H-3-benzazepina Descriptor Portuguese: 2,3,4,5-Tetra-Hidro-7,8-Di-Hidroxi-1-Fenil-1H-3- ...
Fingerprint Dive into the research topics of Activation of post-synaptic dopamine D receptors promotes the release of tissue plasminogen activator in the nucleus accumbens via PKA signaling.. Together they form a unique fingerprint. ...
  • 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)
  • 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)
  • 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)
  • 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)
  • In rats with a unilateral lesion of the dopaminergic nigrostriatal pathway with 6-hydroxydopamine, blockade of N-methyl-D-aspartate receptors by MK-801 strongly potentiated the turning behavior induced by D-1 receptor stimulation. (elsevier.com)
  • However, the results do suggest that chronic APD treatment alters the interaction between D 1 - and D 2 -neostriatal receptors. (elsevier.com)
  • Molecular genetic studies have also focused on hypothesized associations between various DA related genes and ADHD, with mixed evidence regarding DAT1 and somewhat stronger results with respect to DA receptors DRD4 and DRD5 [ 3 ]. (biomedcentral.com)
  • These receptors are crucial modulators of the motor and cognitive functions mediated by the frontal-striatal circuitry [ 5 , 6 ], functions which are impaired in patients with ADHD. (biomedcentral.com)
  • The present study was to investigate the role of dopamine D1 receptors and its relationship with glutamate , N-methyl-D-aspartic acid ( NMDA ) receptor and α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid ( AMPA ) receptor in depression induced by chronic unpredictable mild stress (CUMS). (bvsalud.org)
  • 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)
  • Receptors, Dopamine D2/drug effects Substances Benzazepines Dopamine Agonists. (naltrexoneinfo.com)
  • Recent evidence suggests that the blockade of cannabinoid CB(1) receptors might be beneficial to alleviate motor inhibition typical of Parkinson's disease. (bvsalud.org)
  • Here, we investigated whether antagonism of CB(1) receptors would improve emotional and cognitive deficits in a rat model of premotor Parkinson's disease. (bvsalud.org)
  • Here we aimed to clarify the role of D2-like receptors in regulation of differentiation and function of T lymphocyte subsets, including helper T (Th)1, Th2, Th17 and regulatory T (Treg) cells. (nel.edu)
  • SKF38393, an agonist of dopamine D1-like receptors (D1 and D5 receptors) only reduced the IFN-γ production, but did not significantly affect the proliferative response, IL-4 production, cAMP content or CREB activation of the lymphocytes. (nel.edu)
  • Quinpirole, an agonist of dopamine D2-like receptors (D2, D3 and D4 receptors) attenuated the lymphocyte proliferation to Con A, and decreased the IFN-γ but increased the IL-4 production. (nel.edu)
  • D2-like receptors are involved in suppression of T helper 1 (Th1) cell function and enhancement of Th2 cell function through negative link to cAMP-CREB pathway. (nel.edu)
  • Activation of renal dopamine-1 receptors decreases sodium transport. (elsevier.com)
  • 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)
  • In rat neostriatal neurons, D1 dopamine receptors regulate the activity of cyclic AMP-dependent protein kinase (PKA) and protein phosphatase 1 (PP1). (cornell.edu)
  • The findings suggest the presence of both D 1 and D 2 DA receptors in rat anococcygeus muscle and that DA also acts on adrenergic receptors to produce a contractile response of this muscle preparation. (pcom.edu)
  • 1 Department of Pharmacology, College of Pharmacy, University of Houston, Texas 77204-5515. (nih.gov)
  • 2 This work was presented in abstract at the International Union of Pharmacology, Munich, Germany, 1998. (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)
  • Gáborján, A, Lendvai, B & Vízi, E 1999, ' Neurochemical evidence of dopamine release by lateral olivocochlear efferents and its presynaptic modulation in guinea-pig cochlea ', Neuroscience , vol. 90, no. 1, pp. 131-138. (elsevier.com)
  • 1999;90(1):131-138. (elsevier.com)
  • 1999 Jan 1;21(8):781-784. (elsevier.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)
  • D 2 agonists and antagonists failed to modulate the release of dopamine, indicating the lack of negative feedback modulation of dopamine release. (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)
  • Lymphocyte proliferation and production of interferon-γ (IFN-γ) and interleukin-4 (IL-4) in response to concanavalin A (Con A) were measured by colorimetric methyl-thiazole-tetrazolium assay and cytometric bead array, respectively, after the cells were exposed to dopamine D1-like or D2-like receptor agonists and antagonists. (nel.edu)
  • α 2 antagonists yohimbine (10 -5 M) and idazoxan (10 -5 M) blocked the response to DA in a competitive manner, while α 1 antagonist prazosin (10 -5 M) completely blocked the response to DA. (pcom.edu)
  • 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. (biomedsearch.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)
  • This sensitivity was enhanced when we evoked the currents by the GABA C receptor agonist cis -4-aminocrotonic acid (CACA). (chemweb.com)
  • 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)
  • The results showed that, compared with control group , CUMS rats showed depression -like behavioral changes, higher concentration of glutamic acid , lower expressions of NMDA receptor (NR1) and AMPA receptor (GluR2/3) in hippocampus . (bvsalud.org)
  • Pretreatment with injection of SKF38393 could rescue such depression effect of CUMS, decrease the concentration of glutamic acid , and increase the expressions of NMDA receptor (NR1), AMPA receptor (GluR2/3) in hippocampus . (bvsalud.org)
  • A process for the manufacturing of levetiracetam, wherein said process comprises the steps of: (1) reacting the (−)-(S)-alpha-ethyl-2-oxo-1-pyrrolidine acetic acid with a substoichiometric amount of an activating agent in an alcoholic solvent, and (2) subjecting the resulting reaction solution of step (1) to an ammonolysis process with gaseous ammonia. (google.com)
  • More in particular, the present invention relates to an improved process for the conversion of the (−)-(S)-alpha-ethyl-2-oxo-1-pyrrolidineacetic acid to levetiracetam through the activation of the carboxylic acid group and its conversion with gaseous ammonia. (google.com)
  • The full D1-dopamine agonist l,(R,S)1-aminomethyl-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran hydrochloride (A-68930), like SKF-38393, produced a dose-dependent, D1-selective increase in locomotor activity and striatal c-fos-like immunoreactivity. (epa.gov)
  • In the present study, we report that treatment with 1 microM (+/-)-SKF-38393 hydrochloride, a selective D1 agonist, as well as 100 microM trolox, a lipophilic vitamin E analogue, significantly prevented oxidative-related necrotic cell death following exposure to 10 microM Fe2+ or 1 mM buthionine sulfoximine, an inhibitor of gamma-glutamylcysteine synthetase. (ajou.ac.kr)
  • with 2-(dimethylamino)ethanol (1:1),mixt. (uscks.com)
  • 1993 Mar;347(3):289-95. (nih.gov)
  • Although G αq and G α11 are expressed together in almost every cell type, the relative levels of expression vary across brain regions with G αq expression being 2-5 times higher than G α11 in most areas ( Milligan, 1993 ). (frontiersin.org)
  • B-HT 920 [2-amino-6-allyl-5, 6, 7, 8-tetrahydro-4H-thiazolo-(4, 5-d)-azepine] (0.05-1.0 mg/kg), a selective D2-DA agonist, induced mild per se stereotypy consisting mainly of sniffing and rearing responses. (bvsalud.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)
  • Here we show that dopamine-mediated enhancement of spike firing in NAcb shell medium spiny neurons was prevented by the PKC inhibitor bisindolylmaleimide but not by the phospholipase C inhibitor 1-[6-((17b-3-methoxyestra-1,3,5(10)-trien-17-yl) amino)hexyl]-1H-pyrrole-2,5-dione, suggesting a role for a diacylglycerol-independent atypical PKC (aPKC) isoform. (jneurosci.org)
  • For experiments with bisindolylmaleimide and 1-[6-((17b-3-methoxyestra-1,3,5(10)-trien-17-yl) amino)hexyl]-1H-pyrrole-2,5-dione ( U73122 ), slices were pre-exposed for 30-60 min to enable adequate penetration, and whole-cell patch was achieved 10-15 min before dopamine application. (jneurosci.org)
  • In this study we examined the ability of compounds varying in their in vitro potencies as inhibitors of dopamine (DA), norepinephrine (NE) or serotonin (5-HT) reuptake to enhance the discriminative stimulus (DS) effects of cocaine. (aspetjournals.org)
  • Here we investigated learning and memory performance dependent on different brain regions, glutathione antioxidant system, and extracellular signal-regulated protein kinase 1/2 (ERK1/2), serine/threonine protein kinase (AKT), cAMP response element binding (CREB) and dopamine- and cyclic AMP-regulated phosphoprotein (DARPP)-32 signaling in adult Swiss mice submitted to 9 weeks of high-intensity exercise. (bvsalud.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)
  • 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)
  • Although the role of protein kinase A (PKA) and dopamine and cyclic adenosine 3′,5′ monophosphate-regulated phosphoprotein 32 kDa in NAcb dopamine receptor throughput has been studied extensively, the contribution of protein kinase C (PKC) to NAcb firing is poorly understood. (jneurosci.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)
  • 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)
  • Using in vivo microdialysis, we report that infusions of the D1/D5 antagonist SCH 23390 [R-(+)-7-chloro-8-hydroxy-3-methyl-1-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine] (5-200 microM) directly into the striatum increased dopamine release in a concentration-dependent manner. (scienceexchange.com)
  • [0003] Atorvastatin is a competitive inhibitor of the 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase, which is a key enzyme in the biosynthesis of cholesterol in humans. (patentsencyclopedia.com)
  • In contrast, apomorphine-induced increases in JunB-, NGFI-A- and Fos 2-16 -like immunoreactivities were unaffected by either the antisense or random oligonucleotides, indicating that the antisense oligonucleotide attenuated apomorphine-induced priming by selectively blocking the synthesis of FosB proteins. (elsevier.com)
  • 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)
  • Administration of the selective D1-dopamine receptor agonist 2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine (SKF-38393) to neonatal 6-hydroxydopamine-lesioned rats results in profound behavioral manifestations and induction of striatal c-fos-like immunoreactivity. (epa.gov)
  • In contrast, 2,3,4,5‐tetrahydro‐7,8‐dihydroxy‐1‐phenyl‐1H‐3‐benzazepine HCl (SK & F 38393) whether injected intracerebrally or peripherally, induced contralateral rotation but not stereotypy. (deepdyve.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)
  • 4 Contralateral rotation induced by SK & F 38393 was not inhibited by yohimbine, prazosin, atropine, methysergide, mepyramine or propranolol. (deepdyve.com)
  • SKF-38393 (a selective D 1 agonist) increased both the resting and electrically evoked release of dopamine. (elsevier.com)
  • To determine the functional consequences of such positive interaction we measured the local rates of cerebral glucose utilization (lCMR(glc)) in lesioned rats treated with MK-801 (0.1 mg/kg) and the D-1 agonist SKF 38393 (1.5 mg/kg), either alone or in combination. (elsevier.com)
  • There were no differences between age-matched control and antipsychotic drug (APD) treated groups regarding the effects of the D 1 -agonist (+)-SKF 38393 or the D 2 -agonist quinpirole on striatal cAMP content. (elsevier.com)
  • Components of behavioural arousal induced by the dopamine D-1 agonist SKF 38393, the dopamine D-2 agonist RU 24213 and the mixed D-1/D-2 agonist apomorphine were assessed using a behavioural check-list method. (ox.ac.uk)
  • Rats receiving repeated (5 times over 10 days) but not a single ECS showed enhanced grooming and sniffing in response to SKF 38393 (7.5 mg/kg) when compared to controls. (ox.ac.uk)
  • Simultaneous administration of B-HT 920 (0.1-0.5 mg/kg) with SKF 38393 (5 mg/kg), a selective D1-DA agonist, elicited dramatic increase in stereotyped behaviours in naive as well as in 24 hr reserpinised (2 mg/kg) mice . (bvsalud.org)
  • Both SKF-38393 (5-10 mg/kg) and SCH-23390 (100-200 micrograms/kg) significantly and dose dependently reduced deprivation-induced intake. (naltrexoneinfo.com)
  • We tested the hypothesis that the abnormal sodium handling in spontaneously hypertensive rats (Okamoto-Aoki strain) is related to a decreased dopaminergic response by studying the effects of the intrarenal infusion of the dopamine-1 angonist SKF-38393 and the dopamine-1 antagonist SCH-23390 in hypertensive and in normotensive Wistar-Kyoto rats. (elsevier.com)
  • Specificity of dopamine-1 effects of SKF-38393 was verified because its natriuretic effect was blocked in a dose-related manner by the dopamine-1 antagonist SCH-2390 (n = 5). (elsevier.com)
  • Intrarenal arterial infusion of the dopamine-1 agonist SKF-38393 did not affect glomerular filtration rate but resulted in a dose-related natriuresis and diuresis in normotensive but not in hypertensive rats. (elsevier.com)
  • SKF 38393, a D 1 DA agonist, potentiated the response to B-HT 920. (pcom.edu)
  • In primates, CB 1 cannabinoid receptor agonists produce sedation and psychomotor slowing, in contrast to behavioral stimulation produced by high doses of dopamine receptor agonists. (aspetjournals.org)
  • To investigate whether dopamine agonists attenuate the sedative effects of a cannabinoid agonist in monkeys, we compared the effects of D 1 or D 2 dopamine receptor agonists on spontaneous behavior in three to six cynomolgus monkeys ( Macaca fasicularis ) alone and after administration of a low dose of the CB 1 agonist levonantradol. (aspetjournals.org)
  • Thirty minutes after administration of a threshold dose of levonantradol (0.03 mg/kg), D 2 -type agonists, but not the D 1 agonist, precipitated marked sedation, ptosis, and decreased general activity and locomotor activity. (aspetjournals.org)
  • Cannabinoid agonists and D 2 dopamine agonists should be combined with caution. (aspetjournals.org)
  • [ 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)
  • 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)
  • 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)
  • Specifically, dysregulation of dopamine (DA) has been hypothesized in ADHD based on the potent efficacy of indirect dopaminergic agonists, such as methylphenidate, supported by in vivo evidence that methylphenidate effects are related to striatal occupancy of the dopamine transporter (DAT), by increasing extracellular dopamine levels in the striatum [ 2 ]. (biomedcentral.com)
  • 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)
  • [0020] The term `C 1-6 alkyl` as used herein as a group or a part of the group refers to a linear or branched saturated hydrocarbon group containing from 1 to 6 carbon atoms. (patentsencyclopedia.com)
  • [0021] The term `C 1-6 alkoxy` as used herein refers to an --O--C 1-6 alkyl group wherein C 1-6 alkyl is as defined herein. (patentsencyclopedia.com)
  • JPET articles become freely available 12 months after publication, and remain freely available for 5 years. (aspetjournals.org)
  • This graph shows the total number of publications written about "Benzazepines" by people in Harvard Catalyst Profiles by year, and whether "Benzazepines" was a major or minor topic of these publication. (harvard.edu)
  • The compounds therein broadly include 4- hydroxypyran-2-ones and the corresponding ring-opened acids derived therefrom. (google.co.uk)
  • Suspensions of renal proximal tubules from Sprague-Dawley rats were incubated with dopamine, the DA-1 receptor agonist fenoldopam or the DA-2 receptor agonist SK&F 89124 in the presence or absence of either the DA-1 receptor antagonist SCH 23390 or the DA-2 receptor antagonist domperidone. (nih.gov)
  • Dopamine and fenoldopam (10(-5) to 10(-8) mol/l) produced a concentration-dependent inhibition of Na+,K(+)-ATPase activity. (nih.gov)
  • Incubation with fenoldopam (10(-5) to 10(-8) mol/l) in the presence of SK&F 89124 (10(-6) mol/l) inhibited Na+,K(+)-ATPase activity to a degree similar to that with fenoldopam alone. (nih.gov)
  • We found that, in the lower concentration range (10(-5) to 10(-7) mol/l), dopamine-induced inhibition of Na+,K(+)-ATPase activity in the presence of phentolamine was similar in magnitude to that observed with dopamine alone. (nih.gov)
  • Analysis of the relationship between behavioral and in vitro biochemical potencies indicated that inhibition of DA and 5-HT transport is responsible for the cocaine-enhancing effects of the monoamine reuptake blockers we examined. (aspetjournals.org)
  • 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)
  • Furthermore, inhibition of 5-lipoxygenase indirectly decreases the appearance of TNF-alpha (a cytokine that has a key function in irritation), and there are a variety of research demonstrating the function of leukotrienes as mediators from the gastric harm induced by ethanol plus some other toxins(13, 14). (conferencedequebec.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)
  • The specific dopamine DA1 agonist SKF 82526 caused a dose-dependent inhibition of Na+,K+-ATPase activity, which could be blocked by SCH 23390, a specific DA1 antagonist, and by PKI-(5-24) amide, a specific inhibitor of cAMP-dependent protein kinase. (cornell.edu)
  • Alone, the CB 1 cannabinoid receptor agonist levonantradol (0.01-0.3 mg/kg) induced sedation, ptosis, and decreased locomotor and general activity. (aspetjournals.org)
  • 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)
  • Positive modulation of dopamine release has been shown by a D 1 dopamine receptor agonist, an antagonist and piribedil. (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)
  • Intrastriatal delivery of an antisense, but not a random, oligonucleotide to fosB 18 and 6 h before apomorphine reduced the ability of this mixed D 1 /D 2 -like receptor agonist to prime circling induced by the specific D 1 -like receptor agonist SKF38393. (elsevier.com)
  • doi: 10.1016/s0896-6273(00)80082-3. (nih.gov)
  • 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)
  • 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)
  • The cellular localization of DARPP-32, a dopamine- and cAMP-regulated phosphoprotein of Mr 32,000 that appears to mediate certain actions of dopamine in the mammalian brain by acting as an inhibitor of protein phosphatase 1, was studied in the kidney of several species. (cornell.edu)
  • 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)
  • 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)
  • 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)
  • The effect of both drugs on stimulation-evoked release could be prevented by SKF-83566 (a selective D 1 antagonist). (elsevier.com)
  • Montelukast (MK-0476), a selective reversible cys-leukotriene-1 receptor (LTD4 receptor) antagonist can be used in the treating asthma and it is reported to lessen airway eosinophilic irritation within this disease (17-19). (conferencedequebec.org)
  • Intrarenal arterial infusion of the dopamine-1 antagonist SCH-23390 alone induced an antinatriuresis, without affecting glomerular filtration rate, in normotensive but not in hypertensive rats. (elsevier.com)
  • SCH 23390 (10 -5 M), a D 1 DA antagonist potentiated the response to DA. (pcom.edu)
  • The severe stage of obstructed kidney in unilateral ureteral blockage (UUO) is seen as a dramatic adjustments in glomerular purification rate, renal blood circulation, and interstitial edema (2, 3). (conferencedequebec.org)
  • Unilateral ureteral blockage (UUO) can be an experimental rat style of renal damage that imitates the procedure of obstructive nephropathy within an accelerated way(1). (conferencedequebec.org)
  • Numerous factors with complicated mobile and molecular relationships are also proposed as you possibly can causes that result in tubulointerstitial lesions and renal fibrosis (4-7). (conferencedequebec.org)
  • Rats (9-16 weeks old) were studied with renal nerves intact under pentobarbital anesthesia (n = 5-6 in each group). (elsevier.com)
  • The abnormal renal sodium handling in 9-16-week-old spontaneously hypertension rats is in part due to decreased response distal to the dopamine-1 receptor. (elsevier.com)