15 results on '"Carruba M"'
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2. The effect of 5,6-dihydroxytryptamine on sexual behaviour of male rats
- Author
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Da Prada, M., primary, Carruba, M., additional, O'Brien, R.A., additional, Saner, A., additional, and Pletscher, A., additional
- Published
- 1972
- Full Text
- View/download PDF
3. Pharmacological antagonism of lipoprivic feeding induced by sodium mercaptoacetate
- Author
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Garosi, V. L., Nisoli, E., Blundell, J. E., and Carruba, M. O.
- Published
- 1995
- Full Text
- View/download PDF
4. SR 58611A: a novel thermogenic -adrenoceptor agonist
- Author
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Nisoli, E., Tonello, C., and Carruba, M. O.
- Published
- 1994
- Full Text
- View/download PDF
5. SR59230A blocks beta3-adrenoceptor-linked modulation of upcoupling protein-1 and leptin in rat brown adipocytes.
- Author
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Tonello C, Dioni L, Briscini L, Nisoli E, and Carruba MO
- Subjects
- Adipocytes drug effects, Adipocytes metabolism, Adipose Tissue, Brown cytology, Adipose Tissue, Brown metabolism, Animals, Base Sequence, Cells, Cultured, DNA Primers, Ion Channels, Leptin, Male, Mitochondrial Proteins, Rats, Rats, Sprague-Dawley, Receptors, Adrenergic, beta drug effects, Receptors, Adrenergic, beta-3, Reverse Transcriptase Polymerase Chain Reaction, Uncoupling Protein 1, Adipose Tissue, Brown drug effects, Adrenergic beta-Agonists pharmacology, Carrier Proteins metabolism, Membrane Proteins metabolism, Propanolamines pharmacology, Proteins metabolism
- Abstract
Experimental evidence suggests that, by stimulating energy expenditure in brown fat, selective beta3-adrenoceptor agonists can reduce body weight in obese rodents. In order to investigate further the physiological role of beta3-adrenoceptors in brown adipocytes, we analysed the effects of selective beta3-adrenoceptor agonists and antagonists on uncoupling protein-1 and leptin gene expression in culture-differentiated brown fat cells. Our main findings were that: (i) the leptin gene is expressed in brown adipocytes; (ii) the selective beta3-adrenoceptor agonist, N[(2S)-7-carbethoxy-1,2,3,4-tetrahydronaphth-2-yl]-(2R)-2-hydroxy- 2-(3-chlorophenil)ethanamine hydrochloride (SR58611A), inhibits leptin gene while inducing uncoupling protein-1 gene expression; (iii) these opposite effects of SR58611A are antagonized by the selective beta3-adrenoceptor antagonist, SS-enantiomer 3-(2-ethylphenoxy)-1-(1S),2,3,4-tetrahydronaphth-1-ylamin ol]-(2S)-2-propanol oxalate (SR59230A), but not by the selective beta1-adrenoceptor antagonist (+/-)-[2-(3-carbamoyl-4-hydroxyphenoxy)-ethylamino]-3-[4(1-methyl- 4-trifluoromethyl-2-imidazolyl)-phenoxy]-2 propanol (CGP20712A); and (iv) these effects are due to increased cyclic AMP levels. These results confirm by means of a different experimental approach that beta3-adrenoceptors play a central role in controlling the expression of genes that are important for brown fat function.
- Published
- 1998
- Full Text
- View/download PDF
6. SR 58611A: a novel thermogenic beta-adrenoceptor agonist.
- Author
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Nisoli E, Tonello C, and Carruba MO
- Subjects
- Adenylyl Cyclases metabolism, Adipose Tissue, Brown enzymology, Adipose Tissue, Brown metabolism, Adrenergic beta-Antagonists pharmacology, Animals, Cyclic AMP analysis, Cyclic AMP biosynthesis, Drug Interactions, Glycerol metabolism, Imidazoles pharmacology, Lipid Metabolism, Male, Obesity drug therapy, Propanolamines pharmacology, Radioimmunoassay, Rats, Rats, Sprague-Dawley, Tetrahydronaphthalenes antagonists & inhibitors, Adipose Tissue, Brown drug effects, Adrenergic beta-Agonists pharmacology, Tetrahydronaphthalenes pharmacology
- Abstract
N(2S)-7-carbethoxymethoxy-1,2,3,4-tetrahydronaphth-2-yl]-(2R )-2-hydroxy-2-(3-chlorophenyl)ethanamine hydrochloride (SR 58611A) increased cyclic AMP levels in membrane homogenates from rat interscapular brown adipose tissue with an EC50 of 20 +/- 2 nM. Substitution of GTP with the GDP analog, guanosine-5'-O[thiodiphosphate], in the incubation medium suppressed the stimulation of adenylyl cyclase activity by SR 58611A. This compound also stimulated glycerol release from the brown fat cells, with an EC50 of 11 +/- 0.4 nM. Only at doses higher than 10 microM did the non-selective beta-adrenoceptor antagonists, propranolol and alprenolol, as well as the selective beta 1- and beta 2-adrenoceptor antagonists, (+-)-[2-(3-carbamoyl-4-hydroxy-phenoxy)- ethylamino]-3-[4(1-methyl-4-trifluoromethyl-2-imidazolyl)-phenoxy]-2 propanol (CGP 20712A) and erythro-(+-)-1-(7-methylindan-4-yloxy)-3-iso-propylamino butan-2-ol-hydrochloride (ICI 118,551), antagonize the SR 58611A-induced stimulation of both adenylyl cyclase activity and lipid metabolism. Since, at high doses, all these beta-adrenoceptor antagonists lack selectivity for beta 1- or beta 2-adrenoceptors, these results suggest that the beta-adrenoceptor agonist, SR 58611A, activates thermogenesis by acting on brown fat cell beta 3-adrenoceptors. This implies that this compound might be useful for treatment of obesity.
- Published
- 1994
- Full Text
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7. Tolerance to hypoactivity and sensitization to hyperactivity after chronic treatment with a presynaptic dose of lisuride in rats.
- Author
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Nisoli E, Tonello C, Memo M, Pizzi M, Spano P, Reina G, and Carruba MO
- Subjects
- 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine analogs & derivatives, 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine pharmacology, Adenylyl Cyclases metabolism, Analysis of Variance, Animals, Brain drug effects, Brain metabolism, Down-Regulation, Drug Tolerance, Ergolines pharmacology, Fenoldopam, Lisuride administration & dosage, Male, Quinpirole, Radioimmunoassay, Rats, Rats, Inbred Strains, Receptors, Dopamine metabolism, Lisuride pharmacology, Motor Activity drug effects, Receptors, Dopamine drug effects
- Abstract
We studied the adaptive changes of the locomotor effects of lisuride, a selective agonist for dopamine (DA) D2 receptors, and the functional state of D1 and D2 receptors after repeated administration of lisuride at a dose supposed to act preferentially on DA autoreceptors. Rats were treated daily with saline or lisuride, at a dose that causes a significant reduction in locomotor activity when given to naive rats (25 micrograms/kg i.p.), for 33 days and the effect of different challenging doses of the drug on locomotor activity was measured at different times during and after the treatment. The functional state of D1 and D2 DA receptors was evaluated by measuring SKF 82526-stimulated and LY 171555-inhibited adenylate cyclase (AC) activity in the caudatus/putamen, nucleus accumbens and substantia nigra and naive and chronically treated rats. There was a progressive decline in the ability of lisuride to decrease locomotor activity in rats given daily injections of lisuride, and there was a marked reduction in the threshold dose of lisuride for causing hypermotility. The functional state of DA receptors, positively or negatively linked to AC activity, was not modified by the treatment. The most suitable explanation of the reported adaptive behavioral changes is a down-regulation of DA autoreceptors after chronic treatment with presynaptic doses of lisuride.
- Published
- 1992
- Full Text
- View/download PDF
8. Repeated administration of lisuride down-regulates dopamine D-2 receptor function in mesostriatal and in mesolimbocortical rat brain regions.
- Author
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Nisoli E, Memo M, Missale C, Carruba MO, and Spano PF
- Subjects
- 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine analogs & derivatives, 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine pharmacology, Adenylyl Cyclase Inhibitors, Adenylyl Cyclases metabolism, Animals, Cerebral Cortex drug effects, Cerebral Cortex enzymology, Corpus Striatum drug effects, Corpus Striatum enzymology, Dose-Response Relationship, Drug, Fenoldopam, Hippocampus drug effects, Hippocampus enzymology, Hippocampus metabolism, Limbic System drug effects, Limbic System enzymology, Lisuride adverse effects, Male, Nucleus Accumbens drug effects, Nucleus Accumbens enzymology, Nucleus Accumbens metabolism, Rats, Rats, Inbred Strains, Cerebral Cortex metabolism, Corpus Striatum metabolism, Down-Regulation drug effects, Ergolines pharmacology, Limbic System metabolism, Lisuride pharmacology, Receptors, Dopamine drug effects
- Abstract
Functional modifications of both D-1 and D-2 dopamine (DA) receptor subtypes following repeated administration of lisuride, a DA agonist that acts selectively on D-2 DA receptors were studied. The functional state of D-1 and D-2 DA receptors was evaluated from measurements of SKF 82526-stimulated and bromocriptine-inhibited adenylate cyclase activity in different brain regions of rats treated daily for 26 days with saline or lisuride (100 micrograms/kg i.p.). Persistent stimulation by lisuride of DA receptors in striatum, nucleus accumbens, substantia nigra, frontal cortex, hippocampus and pituitary gland induced a down-regulation of D-2 receptors without changing the functional activity of D-1 receptors.
- Published
- 1990
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9. Behavioural effects of a new non-phenylethylamine anorexigenic agent: mazindol.
- Author
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Zambotti F, Carruba MO, Barzaghi F, Vicentini L, Groppetti A, and Mantegazza P
- Subjects
- Animals, Appetite drug effects, Body Temperature drug effects, Dextroamphetamine pharmacology, Humans, Male, Methyltyrosines pharmacology, Motor Activity drug effects, Pimozide pharmacology, Rats, Stereotyped Behavior drug effects, Behavior, Animal drug effects, Indoles pharmacology, Mazindol pharmacology
- Abstract
Mazindol, a new anorexigenic agent which possesses a different chemical structure from phenylethylamine derivatives such as amphetamine, causes anorexia along with increases in locomotor activity and body temperature. Mazindol also induces stereotyped behaviour and, if injected into rats with unilateral nigro-striatal lesions, causes turning towards the lesioned side. Mazindol-induced anorexia is antagonized by pretreatment with alpha-methyl-p-tyrosine or pimozide. Pimozide pretreatment prevents the rotation induced by Mazindol in rats with unilateral nigro-striatal lesions. The involvement of dopamine in the mechanism whereby Mazindol elicits anorexia and turning behaviour is discussed.
- Published
- 1976
- Full Text
- View/download PDF
10. Evidence for the presence of D1 and D2 dopamine receptors in the rat adrenal cortex.
- Author
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Missale C, Memo M, Liberini P, Carruba MO, and Spano P
- Subjects
- Adenylyl Cyclases analysis, Animals, Benzazepines pharmacology, Dopamine pharmacology, Male, Rats, Rats, Inbred Strains, Adrenal Cortex analysis, Receptors, Dopamine analysis
- Published
- 1985
- Full Text
- View/download PDF
11. Plasma catecholamines in rats exposed to cold: effects of ganglionic and adrenoreceptor blockade.
- Author
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Picotti GB, Carruba MO, Ravazzani C, Cesura AM, Galva MD, and Da Prada M
- Subjects
- Adrenalectomy, Animals, Dopamine blood, Epinephrine blood, Male, Norepinephrine blood, Rats, Adrenergic alpha-Antagonists pharmacology, Adrenergic beta-Antagonists pharmacology, Catecholamines blood, Cold Temperature, Ganglionic Blockers pharmacology
- Abstract
Exposure to cold (4 degrees C) of catheterized rats acclimated to 20 degrees C resulted in a progressive increase in plasma noradrenaline (NA) concentrations which reached values consistently more than twice the basal ones (20 degrees C) by about 30 min. No further increase in plasma NA levels were detected when the cold exposure was continued for 24 h. Plasma adrenaline (A) and dopamine levels did not change at any time studied. Adrenalectomized rats exposed to cold exhibited percent rises in plasma NA similar to those in intact rats. An increase in plasma A levels concomitant with that of NA was observed following exposure to cold of rats in which either basal catecholamine release was impaired by chlorisondamine or the vasoconstrictor response was impeded by phentolamine. Propranolol did not modify the acute neurosympathetic response to cold. Exposure to cold (4 degrees C) for short periods of time combined with the measurement of plasma catecholamines is proposed as a useful and reproducible method for studying a pure neurosympathetic response in the rat.
- Published
- 1981
- Full Text
- View/download PDF
12. Anorectic effect of lisuride and other ergot derivatives in the rat.
- Author
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Carruba MO, Ricciardi S, Müller EE, and Mantegazza P
- Subjects
- Animals, Apomorphine pharmacology, Bromocriptine pharmacology, Dose-Response Relationship, Drug, Eating drug effects, Haloperidol pharmacology, Humans, Male, Motor Activity drug effects, Pimozide pharmacology, Rats, Receptors, Dopamine drug effects, Stereotyped Behavior drug effects, Time Factors, Appetite Depressants, Ergolines pharmacology, Ergot Alkaloids pharmacology, Lisuride pharmacology
- Abstract
Three ergot derivatives, lisuride, lergotrile and bromocriptine, given to rats trained to eat 4 h a day, induced a dose- and time-related anorexia. They were more potent in this context than either amphetamine or fenfluramine. Lisuride and lergotrile failed to increase locomotor activity or to induce stereotyped behaviour at doses corresponding to the ID50 on food intake. At this dose, bromocriptine slightly stimulated motor activity. The anorectic effect of the three compounds was selectively antagonized by blockers of dopamine (DA) receptors in the central nervous system but not by either inhibiton of catecholamine synthesis or blockade of alpha- or beta-adrenoceptors or of serotonergic receptors. Also two blockers of 'peripheral' DA receptors failed to antagonize ergoline-induced anorexia. These findings indicate that stimulation of DA receptors involved in feeding behaviour was responsible for the anorexigenic effect of the ergot derivatives investigated. In most instances this effect occurred at dose levels which failed to induce central stimulant effects.
- Published
- 1980
- Full Text
- View/download PDF
13. Repeated administration of (-)sulpiride and SCH 23390 differentially up-regulate D-1 and D-2 dopamine receptor function in rat mesostriatal areas but not in cortical-limbic brain regions.
- Author
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Memo M, Pizzi M, Nisoli E, Missale C, Carruba MO, and Spano P
- Subjects
- Adenylyl Cyclases metabolism, Animals, Brain enzymology, Bromocriptine pharmacology, Cerebral Cortex drug effects, Cerebral Cortex enzymology, Corpus Striatum drug effects, Corpus Striatum enzymology, Fenoldopam, Limbic System drug effects, Limbic System enzymology, Male, Pituitary Gland drug effects, Pituitary Gland metabolism, Rats, Rats, Inbred Strains, Vasodilator Agents pharmacology, Antipsychotic Agents pharmacology, Benzazepines pharmacology, Brain drug effects, Receptors, Dopamine drug effects, Sulpiride pharmacology
- Abstract
We studied the possible functional modifications of both D-1 and D-2 dopamine (DA) receptor subtypes following repeated administration of DA antagonists that act selectively on a single class of DA receptors. The functional state of D-1 and D-2 DA receptors in particular was evaluated by measuring SKF 82526-stimulated and bromocriptine-inhibited adenylate cyclase activity in different brain regions of rats treated with saline, SCH 23390, or (-)sulpiride for 21 days. The results indicate that chronic blockade of D-1 DA receptors in striatum, nucleus accumbens, and substantia nigra by SCH 23390 induced up-regulation of the D-1 receptors without changing the functional activity of D-2 receptors. Likewise, chronic blockade of D-2 DA receptors by (-)sulpiride caused up-regulation of D-2 but not D-1 DA receptors in striatum, nucleus accumbens, substantia nigra and pituitary. SCH 23390 or (-)sulpiride did not modify the functional activity of either D-1 or D-2 DA receptors located in frontal cortex and hippocampus. In conclusion, these results indicate that chronic treatment with selective D-1 or D-2 DA receptor blockers induces a receptor-specific up-regulation which involves the DA receptors located in the nigrostriatal system and pituitary but not those in the limbic-cortical areas.
- Published
- 1987
- Full Text
- View/download PDF
14. Effects of diethyl ether, halothane, ketamine and urethane on sympathetic activity in the rat.
- Author
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Carruba MO, Bondiolotti G, Picotti GB, Catteruccia N, and Da Prada M
- Subjects
- Animals, Blood Gas Analysis, Blood Pressure drug effects, Catecholamines blood, Ether pharmacology, Halothane pharmacology, Ketamine pharmacology, Male, Rats, Rats, Inbred Strains, Urethane pharmacology, Anesthetics pharmacology, Sympathetic Nervous System drug effects
- Abstract
The present paper describes the effects of different general anaesthetics on plasma catecholamine (CA) concentrations taken as biochemical index of peripheral sympathetic activity. In chronically catheterized rats, diethyl ether, ketamine and urethane increased plasma adrenaline (A) and noradrenaline (NA) concentrations, indicating that these drugs stimulate both neurosympathetic and adrenomedullary functions. These effects appear to be centrally mediated, since ganglionic blockade or spinal transection completely counteracted the diethyl ether- and ketamine-induced increases in plasma CA levels. Halothane induced a transient decrease in circulating A and an increase in NA. These results support the concept that general anaesthetics may have different effects on sympathetic function. Arterial blood pressure and heart rate were also measured to look for possible correlations with peripheral sympathetic activity. The enhanced release of peripheral CAs seemed to be the determining factor for increasing blood pressure and heart rate with ketamine only. In the other instances the activation of the peripheral sympathetic system appeared to maintain homeostasis by counterbalancing the various depressive effects of anaesthetics on the cardiovascular system.
- Published
- 1987
- Full Text
- View/download PDF
15. Effects of mazindol and d-fenfluramine of 5-hydroxytryptamine uptake, storage and metabolism in blood platelets.
- Author
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Picotti GB, Carruba MO, Zambotti F, and Mantegazza P
- Subjects
- Animals, Blood Platelets drug effects, Female, Guinea Pigs, In Vitro Techniques, Kinetics, Male, Blood Platelets metabolism, Fenfluramine pharmacology, Indoles pharmacology, Mazindol pharmacology, Serotonin blood
- Abstract
Mazindol induced a dose-related inhibition of the uptake of labelled 5-hydroxytryptamine (5-HT) by guinea pig blood platelets. It was more potent than d-fenfluramine. Mazindol and d-fenfluramine decreased 5-hydroxy-indoleacetic acid formation in intact platelets but not in sonicated ones. The inhibitory effects of both drugs appeared to the competitive in nature and were markedly reduced in platelets suspended in plasma instead of in Tyrode solution. Mazindol neither decreased the stored endogenous 5-HT nor caused efflux of the labelled amine from preloaded platelets, whereas d-fenfluramine induced a significant release of the amine. It is concluded that mazindol, like d-fenfluramine, competes with 5-HT for the same transport mechanisms at the cytoplasmic membrane level but this effect is not accompanied, as is the case with d-fenfluramine, by a concomitant release of the amine.
- Published
- 1977
- Full Text
- View/download PDF
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