Gabriele E. M. Biella | Consiglio Nazionale delle Ricerche (CNR) (original) (raw)

Papers by Gabriele E. M. Biella

Research paper thumbnail of The descending inhibitory pathways. Their role in analgesia, after consideration of specific spinal adrenergic involvement

PubMed, 1989

The four main descending pathways - from the cortex, the diencephalon, the mesencephalon and the ... more The four main descending pathways - from the cortex, the diencephalon, the mesencephalon and the pontobulbar structures - are briefly examined with regard to their role as regulatory systems with an overall inhibitory action processing the afferents to the spinal cord. Sketches are given of the possible analgesic properties in the selective gating of C and Ad nociceptive afferences. The involvement of neuronal subpopulations in the spinal cord presenting alpha-2 and alpha-1 receptors, their hypothetic role in certain reactive analgesic processes, and their coactivation are mentioned briefly.

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Research paper thumbnail of Effects of tenoxicam on nociceptive thalamic neuronal firing in arthritic rats

PubMed, 1987

The antinociceptive action of tenoxicam, a new non-steroidal anti-inflammatory drug, has been inv... more The antinociceptive action of tenoxicam, a new non-steroidal anti-inflammatory drug, has been investigated by exploring the spontaneous and evoked electrophysiological patterns of firing of thalamic neurons in arthritic rats. A marked decrease in the firing activity evoked by ankle mobilization has been found to be present at doses of tenoxicam of 0.6 mg/kg i.v. A similar effect is obtainable with aspirin (as reference drug) but with doses of 54 mg/kg i.v. On studying the effects of increasing doses of tenoxicam a progressively longer time-course inhibition has been found and the analysis confirmed a linear correlation. Findings are discussed postulating that the final antinociceptive effect of tenoxicam can be correlated with its anti-inflammatory activity.

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Research paper thumbnail of A role for locus coeruleus in Parkinson tremor

Frontiers in Human Neuroscience, 2012

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Research paper thumbnail of Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration

Neurochemistry International, May 1, 2004

The peripheral-type benzodiazepine receptors (PBRs) are only minimally expressed in normal brain ... more The peripheral-type benzodiazepine receptors (PBRs) are only minimally expressed in normal brain parenchyma, where they are primarily localized in glial cells. Their basal expression rises in different neurodegenerative disorders, due to the presence of infiltrating inflammatory cells and activated microglia. [11C]PK11195, a selective PBR antagonist, has been used for the in vivo PET monitoring of neurodegeneration in clinical observations. We recently developed and labeled with carbon-11 three new carboxamide derivatives: [11C]VC193M, [11C]VC195 and [11C]VC198M. Aim of this study was to evaluate these ligands for the in vivo measuring of PBRs expression in neurodegenerations and compare their kinetic behavior with that of the reference tracer [11C]PK11195. Radioligands were evaluated in a preclinical model of Huntington's disease consisting in the monolateral striatal injection of quinolinic acid (QA). Activated microglia and astrocytic gliosis was present only within the affected striatum. A concomitant increase in radioactivity accumulation was observed for all the tracers examined (P<0.01). Among the new compounds, [11C]VC195 showed higher levels of lesioned/unlesioned striatum ratios (3.28+/-0.44), in comparison with [11C]VC193M and [11C]VC198M (2.69+/-0.53 and 1.52+/-0.36, respectively), but slightly inferior to that observed for [11C]PK11195 (3.76+/-1.41).In conclusion, the results of the study indicate that [11C]VC195 is a promising candidate for in vivo PET monitoring of neurodegenerative processes but its in vivo behavior overlap that of [11C]PK11195.

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Research paper thumbnail of Where thought lives: place or palace?

Springer eBooks, 2002

... Author Index Acernese F 165 Apolloni B 301 Aversano G 178 Barone F 165 BastiG 313 Bertoni A 8... more ... Author Index Acernese F 165 Apolloni B 301 Aversano G 178 Barone F 165 BastiG 313 Bertoni A 87 Bianchini M 96 Biella GEM 328 Bisio GM ... 187 Ferrari-Trecate G 114 Fiori S 63 Frattale Mascioli FM 23 Fruhwirth M 228 Funaro M 187 GaitoS 301 Gers FA 193 Giordano F 201 ...

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Research paper thumbnail of Extraction and Characterization of Essential Discharge Patterns from Multisite Recordings of Spiking Ongoing Activity

PLOS ONE, Jan 28, 2009

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Research paper thumbnail of Paclitaxel alters angiogenesis in the peripheral and central nervous system of neuropathic rats

74 Congresso della Società Italiana di Anatomia ed Istologia, 2021

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Research paper thumbnail of Monte Carlo simulation of near-infrared light propagation in a realistic, three-dimensional human head and brain model

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Research paper thumbnail of Cefoperazone pharmacokinetics and sputum levels after single/multiple i.m. injections in bronchopneumopathic patients and bone, pulmonary and prostatic tissue penetration

PubMed, 1983

Cefoperazone is a third-generation semisynthetic injectable cephalosporin. It has been reported t... more Cefoperazone is a third-generation semisynthetic injectable cephalosporin. It has been reported that cefoperazone has beta-lactamase resistance and quite a broad antimicrobial spectrum against many Gram-positive and Gram-negative microorganisms and most anaerobes. In this study, the pharmacokinetics of cefoperazone were examined in a group of 10 patients suffering from acute exacerbations of chronic bronchitis, with purulent or mucopurulent expectorations. Cefoperazone was administered at the dose of 1 g i.m. every 12 hours. Serum and urinary parameters and the profile of bronchial mucus diffusion were assessed after the first administration and during the whole period of treatment which lasted for 7 days. In a second, third, and fourth group of volunteer patients who had to undergo surgical operations, bone, lung and prostatic penetration of cefoperazone was determined in correlation with serum levels.

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Research paper thumbnail of Evaluation of domifen bromide in the treatment of acute infectious oral diseases

PubMed, 1983

By means of a double blind, placebo controlled trial, we have studied 29 patients (14 M and 15 F)... more By means of a double blind, placebo controlled trial, we have studied 29 patients (14 M and 15 F) affected by different acute infectious oral diseases. Our results suggest that domifen bromide may be useful in treating infectious oral diseases in combination with antibiotics, and in relieving pain and inflammation.

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Research paper thumbnail of Comparative study on the electrophysiological responses at thalamic level to different analgesic peptides

PubMed, 1985

Using electrophysiological methods to detect the extracellular activity of single neurons in the ... more Using electrophysiological methods to detect the extracellular activity of single neurons in the thalamus of anaesthetized rats, their response to mechanical and thermal noxious stimuli were assessed before and after administration of 4 analgesic peptides of various types. Dermophin, a peptide extracted from frog's skin, was found to have an opioid-like antinociceptive activity antagonized by naloxone. Caerulein, which has a similar origin, failed to suppress the nociceptive responses of thalamic neurons evoked by peripheral stimuli. Calcitonin, a peptide found at brain level, induced an alteration of the increased firing characteristic of noxious stimuli, and its action was not reversed by naloxone. FK 33-824, a synthetic peptide, induced a morphine-like action when injected i.c.v. at a dosage 1000 times lower than that of morphine on a molar basis. It is concluded that electrophysiological investigations on peptides endowed with analgesic activity contribute greatly to a more precise profile of the peptides as candidate drugs in pain control.

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Research paper thumbnail of Pharmacokinetics and sputum levels of josamycin after single and multiple administrations in bronchopneumopathic patients

PubMed, 1983

Josamycin is a new macrolide antibiotic with low toxicity and effective therapeutic activity in m... more Josamycin is a new macrolide antibiotic with low toxicity and effective therapeutic activity in many bacterial diseases, particularly bronchopulmonary infections. In the present study the pharmacokinetics of josamycin were investigated in a group of 10 patients suffering from acute exacerbation of chronic bronchitis, with purulent or mucopurulent expectoration. Patients were given one oral administration of 1 g of josamycin every 12 hours for seven days. Serum, urinary parameters and the profile of bronchial mucus diffusion were assessed after the first and the last administration.

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Research paper thumbnail of Eseroline depresses the responses of dorsal horn neurons to C-fiber afferents in the spinal rat

Neuroscience Letters, Oct 1, 1986

Eseroline not only has some structural features in common with morphine but also has a specific a... more Eseroline not only has some structural features in common with morphine but also has a specific antinociceptive action like opioid drugs. The effects of eseroline on the responses of rat dorsal horn lamina V neurons to C-fiber-related noxious stimuli were investigated. The data obtained showed that 15 min after eseroline administration, the neuronal responses to C-fiber-related afferents were almost totally suppressed. Morphine was used as reference drug. The postulated action of eseroline on opioid receptors was confirmed by reversal of eseroline-driven cell activity after naloxone injection.

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Research paper thumbnail of Effect of Melatonin on Sleep Microstructure: Preliminary Results in Healthy Subjects

Sleep, Dec 1, 1993

The ability of melatonin (MLT) to potentiate the effects of gamma-aminobutyric acid and the benzo... more The ability of melatonin (MLT) to potentiate the effects of gamma-aminobutyric acid and the benzodiazepines has been demonstrated repeatedly in animal models, and recent experimental data favored the hypothesis that MLT, given together with threshold doses of benzodiazepines, could significantly improve the quality of sleep. This preliminary study was designed to compare the effects of MLT (100 mg) with those of a benzodiazepine hypnotic [triazolam (TRI) 0.125 mg] and to explore the effects of a combination of MLT and TRI at a low dose in healthy volunteers. No significant changes in the classical polysomnographic variables were observed following MLT, TRI and MLT + TRI, whereas MLT and especially MLT + TRI resulted in significant modulation of some microstructural parameters. These changes were paralleled by ameliorated subjective sleep quality. A combination of MLT and low benzodiazepine doses could avoid the residual, dose-related benzodiazepine effects.

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Research paper thumbnail of Calcitonin gene-related peptide: antinociceptive activity in rats, comparison with calcitonin

Regulatory Peptides, Aug 1, 1987

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Research paper thumbnail of Inhibitory effect of eseroline, an opiate like drug, on the rat nociceptive thalamic neurons activated by peripheral noxious stimuli

Brain Research, Mar 1, 1984

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Research paper thumbnail of Dermorphin, a new peptide from amphibian skin, inhibits the nociceptive thalamic neurons firing rate evoked by noxious stimuli

Neuroscience Letters, Nov 1, 1984

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Research paper thumbnail of Depressant effects of suprofen, a new non-steroidal anti-inflammatory drug on thalamic evoked neuronal firing in arthritic rats

Neuropharmacology, Sep 1, 1986

The effects of suprofen, a new non-steroidal anti-inflammatory drug, (NSAID), the activity of whi... more The effects of suprofen, a new non-steroidal anti-inflammatory drug, (NSAID), the activity of which is mainly antinociceptive, were compared with those of aspirin (as a reference drug) in a study of spontaneous and evoked firing of thalamic neurons (nucleus lateralis and ventrobasalis) in rats rendered arthritic by injection of Freund's adjuvant into the paw. Suprofen (3.7 mg/kg, i.v.) induced a marked decrease in the firing evoked in arthritic rats by ankle mobilization. This effect, after a rapid onset, lasted on the average for 60 min. A similar effect was obtained with aspirin, but with 54 mg/kg (i.v.) (14 times more than suprofen). With increasing doses of suprofen, it was possible to obtain an increased long-lasting inhibition of the evoked activity, with a significant dose-effect linear regression. The possibility that there are both CNS and peripheral effects of suprofen is discussed in relation to the possible role of aspirin (the reference standard for NSAIDs) in enhancing presynaptic inhibition, thus reducing the effectiveness of incoming sensory stimuli.

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Research paper thumbnail of Depression of neuronal evoked firing by eseroline, a new opiate-like drug, in the rat dorsal horn

Pain, 1984

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Research paper thumbnail of Melatonin signal transduction and mechanism of action in the central nervous system: using the rabbit cortex as a model

Endocrinology, 1992

The cortex of the rabbit (Oryctolagus cuniculus) is rich in melatonin binding sites, and particul... more The cortex of the rabbit (Oryctolagus cuniculus) is rich in melatonin binding sites, and particularly abundant is the parietal cortex. Consequently, we characterized the putative melatonin receptor in the parietal cortex by a series of in vitro ligand-receptor binding experiments and biochemical and electrophysiological studies. The in vitro saturation and competition experiments demonstrated that the binding in the crude cortical membrane preparations was of high affinity and specificity. Guanine nucleotides (GDP, GTP, and GTP gamma S) inhibited the specific 2-[125I]iodomelatonin binding in a dose-dependent manner. Coincubation with a nonhydrolyzable GTP analog provoked a shift in the binding affinity; the numerical values of the Kd increased from 20-30 to 200-600 pM. Melatonin, in nanomolar concentrations, was able to inhibit the forskolin-stimulated accumulation of cAMP in parietal cortex explants, and preincubation with pertussis toxin counteracted this effect of melatonin. Apparently, the melatonin binding site in the rabbit parietal cortex is linked to its second messenger via a pertussis toxin-sensitive G-protein, probably of the inhibitory Gi class, similar to what has been described for different parts of the brain of other vertebrates. The experiments on the spontaneous firing activity of single neurons in the third to fourth layer of the parietal cortex in anesthetized animals showed that melatonin and its potent agonist 2-iodomelatonin exhibited gamma-aminobutyric acid (GABA)-like effects and were able alone, in nanomolar concentrations, to significantly slow the neuronal firing activity. Moreover, both melatonin and 2-iodomelatonin potentiated the effect of GABA on the neuronal activity, leading to powerful inhibition of the tested neurons. Undoubtedly, the binding site in the rabbit parietal cortex possesses all of the characteristics of a functional receptor. We suggest that melatonin is involved in the control of fundamental cortical functions and that it acts in concert with GABA, one of the two major inhibitory neurotransmitters in the central nervous system.

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Research paper thumbnail of The descending inhibitory pathways. Their role in analgesia, after consideration of specific spinal adrenergic involvement

PubMed, 1989

The four main descending pathways - from the cortex, the diencephalon, the mesencephalon and the ... more The four main descending pathways - from the cortex, the diencephalon, the mesencephalon and the pontobulbar structures - are briefly examined with regard to their role as regulatory systems with an overall inhibitory action processing the afferents to the spinal cord. Sketches are given of the possible analgesic properties in the selective gating of C and Ad nociceptive afferences. The involvement of neuronal subpopulations in the spinal cord presenting alpha-2 and alpha-1 receptors, their hypothetic role in certain reactive analgesic processes, and their coactivation are mentioned briefly.

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Effects of tenoxicam on nociceptive thalamic neuronal firing in arthritic rats

PubMed, 1987

The antinociceptive action of tenoxicam, a new non-steroidal anti-inflammatory drug, has been inv... more The antinociceptive action of tenoxicam, a new non-steroidal anti-inflammatory drug, has been investigated by exploring the spontaneous and evoked electrophysiological patterns of firing of thalamic neurons in arthritic rats. A marked decrease in the firing activity evoked by ankle mobilization has been found to be present at doses of tenoxicam of 0.6 mg/kg i.v. A similar effect is obtainable with aspirin (as reference drug) but with doses of 54 mg/kg i.v. On studying the effects of increasing doses of tenoxicam a progressively longer time-course inhibition has been found and the analysis confirmed a linear correlation. Findings are discussed postulating that the final antinociceptive effect of tenoxicam can be correlated with its anti-inflammatory activity.

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Research paper thumbnail of A role for locus coeruleus in Parkinson tremor

Frontiers in Human Neuroscience, 2012

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Research paper thumbnail of Evaluation of three quinoline-carboxamide derivatives as potential radioligands for the in vivo pet imaging of neurodegeneration

Neurochemistry International, May 1, 2004

The peripheral-type benzodiazepine receptors (PBRs) are only minimally expressed in normal brain ... more The peripheral-type benzodiazepine receptors (PBRs) are only minimally expressed in normal brain parenchyma, where they are primarily localized in glial cells. Their basal expression rises in different neurodegenerative disorders, due to the presence of infiltrating inflammatory cells and activated microglia. [11C]PK11195, a selective PBR antagonist, has been used for the in vivo PET monitoring of neurodegeneration in clinical observations. We recently developed and labeled with carbon-11 three new carboxamide derivatives: [11C]VC193M, [11C]VC195 and [11C]VC198M. Aim of this study was to evaluate these ligands for the in vivo measuring of PBRs expression in neurodegenerations and compare their kinetic behavior with that of the reference tracer [11C]PK11195. Radioligands were evaluated in a preclinical model of Huntington's disease consisting in the monolateral striatal injection of quinolinic acid (QA). Activated microglia and astrocytic gliosis was present only within the affected striatum. A concomitant increase in radioactivity accumulation was observed for all the tracers examined (P<0.01). Among the new compounds, [11C]VC195 showed higher levels of lesioned/unlesioned striatum ratios (3.28+/-0.44), in comparison with [11C]VC193M and [11C]VC198M (2.69+/-0.53 and 1.52+/-0.36, respectively), but slightly inferior to that observed for [11C]PK11195 (3.76+/-1.41).In conclusion, the results of the study indicate that [11C]VC195 is a promising candidate for in vivo PET monitoring of neurodegenerative processes but its in vivo behavior overlap that of [11C]PK11195.

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Research paper thumbnail of Where thought lives: place or palace?

Springer eBooks, 2002

... Author Index Acernese F 165 Apolloni B 301 Aversano G 178 Barone F 165 BastiG 313 Bertoni A 8... more ... Author Index Acernese F 165 Apolloni B 301 Aversano G 178 Barone F 165 BastiG 313 Bertoni A 87 Bianchini M 96 Biella GEM 328 Bisio GM ... 187 Ferrari-Trecate G 114 Fiori S 63 Frattale Mascioli FM 23 Fruhwirth M 228 Funaro M 187 GaitoS 301 Gers FA 193 Giordano F 201 ...

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Research paper thumbnail of Extraction and Characterization of Essential Discharge Patterns from Multisite Recordings of Spiking Ongoing Activity

PLOS ONE, Jan 28, 2009

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Research paper thumbnail of Paclitaxel alters angiogenesis in the peripheral and central nervous system of neuropathic rats

74 Congresso della Società Italiana di Anatomia ed Istologia, 2021

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Monte Carlo simulation of near-infrared light propagation in a realistic, three-dimensional human head and brain model

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Cefoperazone pharmacokinetics and sputum levels after single/multiple i.m. injections in bronchopneumopathic patients and bone, pulmonary and prostatic tissue penetration

PubMed, 1983

Cefoperazone is a third-generation semisynthetic injectable cephalosporin. It has been reported t... more Cefoperazone is a third-generation semisynthetic injectable cephalosporin. It has been reported that cefoperazone has beta-lactamase resistance and quite a broad antimicrobial spectrum against many Gram-positive and Gram-negative microorganisms and most anaerobes. In this study, the pharmacokinetics of cefoperazone were examined in a group of 10 patients suffering from acute exacerbations of chronic bronchitis, with purulent or mucopurulent expectorations. Cefoperazone was administered at the dose of 1 g i.m. every 12 hours. Serum and urinary parameters and the profile of bronchial mucus diffusion were assessed after the first administration and during the whole period of treatment which lasted for 7 days. In a second, third, and fourth group of volunteer patients who had to undergo surgical operations, bone, lung and prostatic penetration of cefoperazone was determined in correlation with serum levels.

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Evaluation of domifen bromide in the treatment of acute infectious oral diseases

PubMed, 1983

By means of a double blind, placebo controlled trial, we have studied 29 patients (14 M and 15 F)... more By means of a double blind, placebo controlled trial, we have studied 29 patients (14 M and 15 F) affected by different acute infectious oral diseases. Our results suggest that domifen bromide may be useful in treating infectious oral diseases in combination with antibiotics, and in relieving pain and inflammation.

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Comparative study on the electrophysiological responses at thalamic level to different analgesic peptides

PubMed, 1985

Using electrophysiological methods to detect the extracellular activity of single neurons in the ... more Using electrophysiological methods to detect the extracellular activity of single neurons in the thalamus of anaesthetized rats, their response to mechanical and thermal noxious stimuli were assessed before and after administration of 4 analgesic peptides of various types. Dermophin, a peptide extracted from frog's skin, was found to have an opioid-like antinociceptive activity antagonized by naloxone. Caerulein, which has a similar origin, failed to suppress the nociceptive responses of thalamic neurons evoked by peripheral stimuli. Calcitonin, a peptide found at brain level, induced an alteration of the increased firing characteristic of noxious stimuli, and its action was not reversed by naloxone. FK 33-824, a synthetic peptide, induced a morphine-like action when injected i.c.v. at a dosage 1000 times lower than that of morphine on a molar basis. It is concluded that electrophysiological investigations on peptides endowed with analgesic activity contribute greatly to a more precise profile of the peptides as candidate drugs in pain control.

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Pharmacokinetics and sputum levels of josamycin after single and multiple administrations in bronchopneumopathic patients

PubMed, 1983

Josamycin is a new macrolide antibiotic with low toxicity and effective therapeutic activity in m... more Josamycin is a new macrolide antibiotic with low toxicity and effective therapeutic activity in many bacterial diseases, particularly bronchopulmonary infections. In the present study the pharmacokinetics of josamycin were investigated in a group of 10 patients suffering from acute exacerbation of chronic bronchitis, with purulent or mucopurulent expectoration. Patients were given one oral administration of 1 g of josamycin every 12 hours for seven days. Serum, urinary parameters and the profile of bronchial mucus diffusion were assessed after the first and the last administration.

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Eseroline depresses the responses of dorsal horn neurons to C-fiber afferents in the spinal rat

Neuroscience Letters, Oct 1, 1986

Eseroline not only has some structural features in common with morphine but also has a specific a... more Eseroline not only has some structural features in common with morphine but also has a specific antinociceptive action like opioid drugs. The effects of eseroline on the responses of rat dorsal horn lamina V neurons to C-fiber-related noxious stimuli were investigated. The data obtained showed that 15 min after eseroline administration, the neuronal responses to C-fiber-related afferents were almost totally suppressed. Morphine was used as reference drug. The postulated action of eseroline on opioid receptors was confirmed by reversal of eseroline-driven cell activity after naloxone injection.

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Effect of Melatonin on Sleep Microstructure: Preliminary Results in Healthy Subjects

Sleep, Dec 1, 1993

The ability of melatonin (MLT) to potentiate the effects of gamma-aminobutyric acid and the benzo... more The ability of melatonin (MLT) to potentiate the effects of gamma-aminobutyric acid and the benzodiazepines has been demonstrated repeatedly in animal models, and recent experimental data favored the hypothesis that MLT, given together with threshold doses of benzodiazepines, could significantly improve the quality of sleep. This preliminary study was designed to compare the effects of MLT (100 mg) with those of a benzodiazepine hypnotic [triazolam (TRI) 0.125 mg] and to explore the effects of a combination of MLT and TRI at a low dose in healthy volunteers. No significant changes in the classical polysomnographic variables were observed following MLT, TRI and MLT + TRI, whereas MLT and especially MLT + TRI resulted in significant modulation of some microstructural parameters. These changes were paralleled by ameliorated subjective sleep quality. A combination of MLT and low benzodiazepine doses could avoid the residual, dose-related benzodiazepine effects.

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Calcitonin gene-related peptide: antinociceptive activity in rats, comparison with calcitonin

Regulatory Peptides, Aug 1, 1987

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Inhibitory effect of eseroline, an opiate like drug, on the rat nociceptive thalamic neurons activated by peripheral noxious stimuli

Brain Research, Mar 1, 1984

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Dermorphin, a new peptide from amphibian skin, inhibits the nociceptive thalamic neurons firing rate evoked by noxious stimuli

Neuroscience Letters, Nov 1, 1984

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Depressant effects of suprofen, a new non-steroidal anti-inflammatory drug on thalamic evoked neuronal firing in arthritic rats

Neuropharmacology, Sep 1, 1986

The effects of suprofen, a new non-steroidal anti-inflammatory drug, (NSAID), the activity of whi... more The effects of suprofen, a new non-steroidal anti-inflammatory drug, (NSAID), the activity of which is mainly antinociceptive, were compared with those of aspirin (as a reference drug) in a study of spontaneous and evoked firing of thalamic neurons (nucleus lateralis and ventrobasalis) in rats rendered arthritic by injection of Freund's adjuvant into the paw. Suprofen (3.7 mg/kg, i.v.) induced a marked decrease in the firing evoked in arthritic rats by ankle mobilization. This effect, after a rapid onset, lasted on the average for 60 min. A similar effect was obtained with aspirin, but with 54 mg/kg (i.v.) (14 times more than suprofen). With increasing doses of suprofen, it was possible to obtain an increased long-lasting inhibition of the evoked activity, with a significant dose-effect linear regression. The possibility that there are both CNS and peripheral effects of suprofen is discussed in relation to the possible role of aspirin (the reference standard for NSAIDs) in enhancing presynaptic inhibition, thus reducing the effectiveness of incoming sensory stimuli.

Bookmarks Related papers MentionsView impact

Research paper thumbnail of Depression of neuronal evoked firing by eseroline, a new opiate-like drug, in the rat dorsal horn

Pain, 1984

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Research paper thumbnail of Melatonin signal transduction and mechanism of action in the central nervous system: using the rabbit cortex as a model

Endocrinology, 1992

The cortex of the rabbit (Oryctolagus cuniculus) is rich in melatonin binding sites, and particul... more The cortex of the rabbit (Oryctolagus cuniculus) is rich in melatonin binding sites, and particularly abundant is the parietal cortex. Consequently, we characterized the putative melatonin receptor in the parietal cortex by a series of in vitro ligand-receptor binding experiments and biochemical and electrophysiological studies. The in vitro saturation and competition experiments demonstrated that the binding in the crude cortical membrane preparations was of high affinity and specificity. Guanine nucleotides (GDP, GTP, and GTP gamma S) inhibited the specific 2-[125I]iodomelatonin binding in a dose-dependent manner. Coincubation with a nonhydrolyzable GTP analog provoked a shift in the binding affinity; the numerical values of the Kd increased from 20-30 to 200-600 pM. Melatonin, in nanomolar concentrations, was able to inhibit the forskolin-stimulated accumulation of cAMP in parietal cortex explants, and preincubation with pertussis toxin counteracted this effect of melatonin. Apparently, the melatonin binding site in the rabbit parietal cortex is linked to its second messenger via a pertussis toxin-sensitive G-protein, probably of the inhibitory Gi class, similar to what has been described for different parts of the brain of other vertebrates. The experiments on the spontaneous firing activity of single neurons in the third to fourth layer of the parietal cortex in anesthetized animals showed that melatonin and its potent agonist 2-iodomelatonin exhibited gamma-aminobutyric acid (GABA)-like effects and were able alone, in nanomolar concentrations, to significantly slow the neuronal firing activity. Moreover, both melatonin and 2-iodomelatonin potentiated the effect of GABA on the neuronal activity, leading to powerful inhibition of the tested neurons. Undoubtedly, the binding site in the rabbit parietal cortex possesses all of the characteristics of a functional receptor. We suggest that melatonin is involved in the control of fundamental cortical functions and that it acts in concert with GABA, one of the two major inhibitory neurotransmitters in the central nervous system.

Bookmarks Related papers MentionsView impact