Carla Ghelardini

Summary

Affiliation: University of Florence
Country: Italy

Publications

  1. ncbi Antisense 'knockdowns' of M1 receptors induces transient anterograde amnesia in mice
    C Ghelardini
    Department of Pharmacology, University of Florence, Italy
    Neuropharmacology 38:339-48. 1999
  2. ncbi Amitriptyline and clomipramine activate Gi-protein signaling pathway in the induction of analgesia
    Carla Ghelardini
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, 50139 Florence, Italy
    Naunyn Schmiedebergs Arch Pharmacol 365:1-7. 2002
  3. ncbi Local anaesthetic activity of beta-caryophyllene
    C Ghelardini
    Department of Pharmacology, University of Florence, Italy
    Farmaco 56:387-9. 2001
  4. ncbi M1 receptor activation is a requirement for arecoline analgesia
    C Ghelardini
    Department of Pharmacology, University of Florence, Italy
    Farmaco 56:383-5. 2001
  5. ncbi Pharmacological identification of SM-21, the novel sigma(2) antagonist
    C Ghelardini
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini 6, University of Florence, I 50139, Florence, Italy
    Pharmacol Biochem Behav 67:659-62. 2000
  6. pmc Loss of muscarinic antinociception by antisense inhibition of M(1) receptors
    C Ghelardini
    Department of Pharmacology, Viale G Pieraccini 6, University of Florence, I 50139 Florence, Italy
    Br J Pharmacol 129:1633-40. 2000
  7. ncbi Local anaesthetic activity of the essential oil of Lavandula angustifolia
    C Ghelardini
    Department of Pharmacology, University of Florence, Italy
    Planta Med 65:700-3. 1999
  8. ncbi Binding profiles of a series of 2-arylpropionic acid esters on cloned human muscarinic receptor subtypes (m1-m5) and their relationship to nootropic activity
    C Ghelardini
    Department of Preclinical and Clinical Pharmacology, University of Florence, Italy
    Arzneimittelforschung 49:483-8. 1999
  9. doi A prolonged protein kinase C-mediated, opioid-related antinociceptive effect of st John's Wort in mice
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50 139 Florence, Italy
    J Pain 11:149-59. 2010
  10. ncbi Blockade of intracellular calcium release induces an antidepressant-like effect in the mouse forced swimming test
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50139 Florence, Italy
    Neuropharmacology 50:309-16. 2006

Detail Information

Publications93

  1. ncbi Antisense 'knockdowns' of M1 receptors induces transient anterograde amnesia in mice
    C Ghelardini
    Department of Pharmacology, University of Florence, Italy
    Neuropharmacology 38:339-48. 1999
    ..Neither aODN, dODN nor vehicle produced any behavioral impairment of mice. These results indicate that the integrity and functionality of M1 receptors are fundamental in the modulation of memory processes...
  2. ncbi Amitriptyline and clomipramine activate Gi-protein signaling pathway in the induction of analgesia
    Carla Ghelardini
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, 50139 Florence, Italy
    Naunyn Schmiedebergs Arch Pharmacol 365:1-7. 2002
    ..These results indicate that amitriptyline and clomipramine induce their analgesic effect by activating all three subtypes of the Gi-proteins...
  3. ncbi Local anaesthetic activity of beta-caryophyllene
    C Ghelardini
    Department of Pharmacology, University of Florence, Italy
    Farmaco 56:387-9. 2001
    ..In conclusion, these data evidence the local anaesthetic activity of beta-caryophyllene, which appears to be strictly dependent on its chemical structure...
  4. ncbi M1 receptor activation is a requirement for arecoline analgesia
    C Ghelardini
    Department of Pharmacology, University of Florence, Italy
    Farmaco 56:383-5. 2001
    ..This effect was detected 24 h after the last i.c.v. injection of aODN. These results indicate that arecoline antinociception is mediated by the activation of central M1 muscarinic receptors...
  5. ncbi Pharmacological identification of SM-21, the novel sigma(2) antagonist
    C Ghelardini
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini 6, University of Florence, I 50139, Florence, Italy
    Pharmacol Biochem Behav 67:659-62. 2000
    ..5 microl) in the red nucleus. These data indicate that SM-21 is a potent and selective sigma(2) antagonist...
  6. pmc Loss of muscarinic antinociception by antisense inhibition of M(1) receptors
    C Ghelardini
    Department of Pharmacology, Viale G Pieraccini 6, University of Florence, I 50139 Florence, Italy
    Br J Pharmacol 129:1633-40. 2000
    ..These results indicate that activation of M(1) muscarinic receptor subtype is fundamental to induce central cholinergic analgesia in mice...
  7. ncbi Local anaesthetic activity of the essential oil of Lavandula angustifolia
    C Ghelardini
    Department of Pharmacology, University of Florence, Italy
    Planta Med 65:700-3. 1999
    ....
  8. ncbi Binding profiles of a series of 2-arylpropionic acid esters on cloned human muscarinic receptor subtypes (m1-m5) and their relationship to nootropic activity
    C Ghelardini
    Department of Preclinical and Clinical Pharmacology, University of Florence, Italy
    Arzneimittelforschung 49:483-8. 1999
    ..p.) in the mouse passive-avoidance test. Compounds 1 and 7, at the highest antiamnesic doses, do not modify motor coordination and spontaneous motility as evaluated by the rota-rod test and Animex apparatus experiments...
  9. doi A prolonged protein kinase C-mediated, opioid-related antinociceptive effect of st John's Wort in mice
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50 139 Florence, Italy
    J Pain 11:149-59. 2010
    ..In particular, the presence of hypericin was fundamental to induce both thermal and chemical antinociception through the inhibition of the PKC activity, whereas hyperforin selectively produced a thermal opioid antinociception...
  10. ncbi Blockade of intracellular calcium release induces an antidepressant-like effect in the mouse forced swimming test
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50139 Florence, Italy
    Neuropharmacology 50:309-16. 2006
    ..In particular, the blockade of both InsP3Rs and RyRs appears to play an important role in the induction of an antidepressant-like effect, whereas the stimulation of these receptors is involved in a depressant-like response of mice...
  11. ncbi Molecular interaction in the mouse PAG between NMDA and opioid receptors in morphine-induced acute thermal nociception
    Carla Ghelardini
    Department of Clinical and Preclinical Pharmacology, University of Florence, Italy
    J Neurochem 105:91-100. 2008
    ..Protein kinase C appears to be the key element that links microOR activation by morphine administration to mice with the recruitment of the NMDA/glutamatergic system involved in the thermal hyperalgesic response...
  12. pmc The central analgesia induced by antimigraine drugs is independent from Gi proteins: superiority of a fixed combination of indomethacin, prochlorperazine and caffeine, compared to sumatriptan, in an in vivo model
    Carla Ghelardini
    Department of Pharmacology, University of Florence, Viale G Pieraccini, 6, 50139 Florence, Italy
    J Headache Pain 10:435-40. 2009
    ..This study suggests that the central antinociceptive action induced by antimigraine drugs is independent from Gi proteins...
  13. ncbi Acetyl-L-carnitine requires phospholipase C-IP3 pathway activation to induce antinociception
    Nicoletta Galeotti
    Department of Pharmacology, University of Florence, Viale G Pieraccini 6, I 50139 Florence, Italy
    Neuropharmacology 47:286-94. 2004
    ..These results indicate that central ALCAR analgesia in mice requires the activation of the PLC-IP(3) pathway. By contrast, the simultaneous activation of PKC may represent a pathway of negative modulation of ALCAR antinociception...
  14. doi Pleiotropic effect of histamine H4 receptor modulation in the central nervous system
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50139 Florence, Italy
    Neuropharmacology 71:141-7. 2013
    ..These results show the antinociceptive, antiamnesic, anxiolytic and anorexant effects induced by neuronal H4R agonism, suggesting that H4 modulators may have broader utility further the control of inflammatory and immune processes...
  15. doi Salvianolic acid B and its liposomal formulations: anti-hyperalgesic activity in the treatment of neuropathic pain
    Benedetta Isacchi
    Department of Pharmaceutical Sciences, University of Florence, via U Schiff 6, Sesto Fiorentino, Florence, Italy
    Eur J Pharm Sci 44:552-8. 2011
    ..p. administration and the effect was still significant at 45 min. Thus, PEGylated formulation ameliorated the performance of drug delaying, increasing and prolonging in time its antihyperalgesic effect...
  16. doi A gene-specific cerebral types 1, 2, and 3 RyR protein knockdown induces an antidepressant-like effect in mice
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini, Florence, Italy
    J Neurochem 106:2385-94. 2008
    ..These findings identify cerebral RyRs as critical targets underlying depressive states and should facilitate the comprehension of the pathophysiology of mood disorders and help developing of new therapeutical strategies...
  17. doi Receptor-independent modulation of reconstituted Galpha(i) protein mediated by liposomes
    Paola Luciani
    Department of Chemistry and CSGI, University of Florence, Via della Lastruccia 3, 50019 Sesto Fiorentino, Florence, Italy
    Mol Biosyst 5:356-67. 2009
    ..A correlation of the physico-chemical features and binding activity of protein-containing membrane model is proposed...
  18. doi Antihyperalgesic activity of verbascoside in two models of neuropathic pain
    Benedetta Isacchi
    Department of Pharmaceutical Sciences, University of Florence, Sesto Fiorentino Department of Preclinical and Clinical Pharmacology, University of Florence, Florence, Italy
    J Pharm Pharmacol 63:594-601. 2011
    ..This study reports on the rapid isolation of verbascoside from Lippia citriodora H.B.K. (Verbenaceae), an inexpensive and widespread source, and the evaluation of its antihyperalgesic activity...
  19. doi Synthesis and biological evaluation of 3,7-diazabicyclo[4.3.0]nonan-8-ones as potential nootropic and analgesic drugs
    Elisabetta Martini
    Department of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
    J Med Chem 54:2512-6. 2011
    ..Compounds 4 and 7 and their enantiomers displayed interesting antihyperalgesic activity in two models of neuropathic pain (streptozotocin-induced and oxalilplatin-induced neuropathy) in comparison with pregabalin...
  20. doi Neuroprotective effects of acetyl-L-carnitine on neuropathic pain and apoptosis: a role for the nicotinic receptor
    Lorenzo Di Cesare Mannelli
    University of Florence, Department of Preclinical and Clinical Pharmacology, Florence, Italy
    J Neurosci Res 87:200-7. 2009
    ..Taken together, these data highlight the relevance of nicotinic modulation in neuropathy treatment...
  21. pmc 4-methyl benzylamine stimulates food consumption and counteracts the hypophagic effects of amphetamine acting on brain Shaker-like Kv1.1 channels
    Renato Pirisino
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, Florence 50134, Italy
    Br J Pharmacol 147:218-24. 2006
    ..We hypothesize that 4-MBZ elicits hyperphagic effects probably by opening Shaker-like Kv1.1 subtypes in the brain, whereas AMPH and BZ are hypophagic by blocking these channels...
  22. ncbi Activity and expression of semicarbazide-sensitive benzylamine oxidase in a rodent model of diabetes: interactive effects with methylamine and alpha-aminoguanidine
    Laura Cioni
    Department of Pharmacology, University of Florence, Italy
    Eur J Pharmacol 529:179-87. 2006
    ..p. These results suggest a crucial role of semicarbazide-sensitive benzylamine oxidase activity in controlling methylamine hypophagia in hyperphagic diabetic mice...
  23. doi Design, synthesis and preliminary pharmacological evaluation of new analogues of DM232 (unifiram) and DM235 (sunifiram) as cognition modulators
    Elisabetta Martini
    Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles HeteroBioLab, Department of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
    Bioorg Med Chem 16:10034-42. 2008
    ..Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, while some cyclohexane derivatives are endowed with amnesia inducing properties...
  24. ncbi Design, synthesis and nootropic activity of new analogues of sunifiram and sapunifiram, two potent cognition-enhancers
    Elisabetta Martini
    Department of Pharmaceutical Sciences, Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles HeteroBioLab, University of Florence, 50019 Sesto Fiorentino, Italy
    Bioorg Med Chem 17:7606-14. 2009
    ..Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, and with a potency similar to the parent compounds...
  25. ncbi Role of intracellular calcium in acute thermal pain perception
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, 50139 Florence, Italy
    Neuropharmacology 47:935-44. 2004
    ....
  26. ncbi H1-receptor stimulation induces hyperalgesia through activation of the phospholipase C-PKC pathway
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini 6, I 50139 Florence, Italy
    Neuropharmacology 47:295-303. 2004
    ..These results indicate a role for the PLC-PKC pathway in central H(1)-induced hyperalgesia in mice. Furthermore, activation of PLC-IP(3) did not appear to play a major role in the modulation of pain perception by H(1)-receptor agonists...
  27. pmc Therapeutic effects of the superoxide dismutase mimetic compound MnIIMe2DO2A on experimental articular pain in rats
    Lorenzo Di Cesare Mannelli
    Department of Pharmacology, University of Florence, Viale Pieraccini 6, 50139 Florence, Italy
    Mediators Inflamm 2013:905360. 2013
    ..Therefore MnL4 appears as a novel protective compound potentially suitable for the treatment of joint diseases...
  28. doi Antidepressant-like effect of artemin in mice: a mechanism for acetyl-L-carnitine activity on depression
    Lorenzo Di Cesare Mannelli
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50139 Florence, Italy
    Psychopharmacology (Berl) 218:347-56. 2011
    ..Depression may be associated with altered plasticity of the nervous system. The importance of neurotrophic factor levels is strongly suggested, and the neuronal-related family is extensively studied with respect to glial-derived one...
  29. doi Antidepressant phenotype by inhibiting the phospholipase Cβ(1)--protein kinase Cγ pathway in the forced swim test
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini 6, 50139 Florence, Italy
    Neuropharmacology 60:937-43. 2011
    ..We demonstrate that selective blockade of PLCβ(1)-PKCγ signalling pathway produces an antidepressant-like phenotype in mice...
  30. ncbi Signaling pathway of morphine induced acute thermal hyperalgesia in mice
    Nicoletta Galeotti
    Department of Clinical and Preclinical Pharmacology, University of Florence, Florence, Italy
    Pain 123:294-305. 2006
    ..The clinical management of pain by morphine may be revisited in light of the identification of the signaling molecules of the hyperalgesic pathway...
  31. ncbi Role of Gi proteins in the antidepressant-like effect of amitriptyline and clomipramine
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Florence, Italy
    Neuropsychopharmacology 27:554-64. 2002
    ....
  32. doi Regionally selective activation and differential regulation of ERK, JNK and p38 MAP kinase signalling pathway by protein kinase C in mood modulation
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Florence, Italy
    Int J Neuropsychopharmacol 15:781-93. 2012
    ..An antidepressant-like phenotype produced by acute blockade of MAPK signalling was also demonstrated...
  33. ncbi Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers
    Elisabetta Martini
    Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles HeteroBioLab, Department of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Italy
    Bioorg Med Chem 16:1431-43. 2008
    ..In addition, the 3-aminopiperidine moiety appears to be a promising scaffold to synthesize new drugs endowed with cognition-enhancing activity...
  34. pmc Different involvement of type 1, 2, and 3 ryanodine receptors in memory processes
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, I 50139 Florence, Italy
    Learn Mem 15:315-23. 2008
    ..These findings also showed the involvement of type 2 and type 3 RyR in the modulation of memory functions identifying these cerebral RyR isoforms as critical targets underlying memory processes...
  35. ncbi Prochlorperazine induces central antinociception mediated by the muscarinic system
    Carla Ghelardini
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50139 Florence, Italy
    Pharmacol Res 50:351-8. 2004
    ..On the basis of the above data, it can be postulated that prochlorperazine exerted an antinociceptive effect mediated by a central cholinergic mechanism...
  36. pmc Inhibition of the PKCγ-ε pathway relieves from meningeal nociception in an animal model: an innovative perspective for migraine therapy?
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini 6, Florence, 50139, Italy
    Neurotherapeutics 10:329-39. 2013
    ..These results suggest the relevance of the PKC-mediated pathway in the induction of meningeal nociception and might help clarify the etiopathology of migraines. We can suggest PKC as a new target for migraine pain...
  37. doi Reversal of NO-induced nociceptive hypersensitivity by St. John's wort and hypericin: NF-κB, CREB and STAT1 as molecular targets
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini 6, 50139, Florence, Italy
    Psychopharmacology (Berl) 227:149-63. 2013
    ..John's wort (SJW), is a medicinal plant mainly used as antidepressant with a favorable safety profile than standard antidepressants. Some studies have also documented other SJW bioactivities, including pain modulation...
  38. doi Protective effect of alpha7 nAChR: behavioural and morphological features on neuropathy
    Alessandra Pacini
    Dept of Anatomy Histology and Forensic Medicine, University of Florence, Viale Morgagni 85, 50139 Florence, Italy
    Pain 150:542-9. 2010
    ..These results strongly suggest the pivotal role of alpha7 nAChR in the neuroprotection during neuropathy...
  39. ncbi Menthol: a natural analgesic compound
    Nicoletta Galeotti
    Department of Pharmacology, Viale G Pieraccini 6, University of Florence, I 50139, Florence, Italy
    Neurosci Lett 322:145-8. 2002
    ..o.; 10-30 microg per mouse i.c.v.) was unable to modify the pain threshold. These results indicate that (-)-menthol is endowed with analgesic properties mediated through a selective activation of kappa-opioid receptors...
  40. ncbi A recombinant transductor-effector system: in vitro study of G inhibitory protein (G-alpha-i1) direct activators
    Lorenzo Di Cesare Mannelli
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50134 Florence, Italy
    Arch Biochem Biophys 453:151-60. 2006
    ..In this functional transductor-effector system BC5 was able to activate Gi signalling, moreover providing a new tool to give a better insight into G-protein receptor-independent modulation...
  41. doi Effect of preparation technique on the properties and in vivo efficacy of benzocaine-loaded ethosomes
    Francesca Maestrelli
    Department of Pharmaceutical Sciences, University of Florence, Italy
    J Liposome Res 19:253-60. 2009
    ..The overall results suggest that a suitably developed ethosomal formulation of BZC can be of actual value for improving its clinical effectiveness in topical anesthesia...
  42. doi Selective modulation of the PKCɛ/p38MAP kinase signalling pathway for the antidepressant-like activity of amitriptyline
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini 6, 50139 Florence, Italy
    Neuropharmacology 62:289-96. 2012
    ..This article is part of a Special Issue entitled 'Anxiety and Depression'...
  43. ncbi Ryanodine receptors are involved in muscarinic antinociception in mice
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50139 Florence, Italy
    Behav Brain Res 164:165-71. 2005
    ..In particular, the stimulation of RyRs appears to play an important role in the increase of the pain threshold produced by physostigmine and oxotremorine in mice...
  44. ncbi Alpha-2 agonist-induced memory impairment is mediated by the alpha-2A-adrenoceptor subtype
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Viale G Pieraccini 6, I 50139 Florence, Italy
    Behav Brain Res 153:409-17. 2004
    ..These results indicate that clonidine and guanabenz impaired memory processes in a mouse passive avoidance paradigm through the selective activation of the alpha2A-adrenoceptor subtype...
  45. ncbi Indomethacin, alone and combined with prochlorperazine and caffeine, but not sumatriptan, abolishes peripheral and central sensitization in in vivo models of migraine
    Carla Ghelardini
    Department of Preclinical and Clinical Pharmacology, University of Florence, Firenze, Italy
    J Pain 5:413-9. 2004
    ....
  46. ncbi Inactivation of Gi proteins induces an antidepressant-like effect in the mouse forced-swimming test
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, Univeristy of Florence, Viale G Pieraccini 6, I 50139, Florence, Italy
    Neuropharmacology 43:457-65. 2002
    ..These results indicate the involvement of Gi(2), Gi(3), Go(1), and Go(2), but not Gi(1), protein subtypes in the transduction mechanism responsible for the induction of an antidepressant-like effect in the mouse forced swimming test...
  47. ncbi Effects of dietary extra-virgin olive oil on behaviour and brain biochemical parameters in ageing rats
    Vanessa Pitozzi
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, 50139 Florence, Italy
    Br J Nutr 103:1674-83. 2010
    ..These results indicate a previously undetected effect of a diet containing an olive oil rich in phenols. Further studies are warranted to verify whether specific food antioxidants might also have an effect on emotional behaviour...
  48. ncbi Acetyl-l-carnitine induces muscarinic antinocieption in mice and rats
    Carla Ghelardini
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50139, Florence, Italy
    Neuropharmacology 43:1180-7. 2002
    ..In the antinociceptive dose-range, ALCAR did not impair mouse performance evaluated by the rota-rod and hole-board tests...
  49. doi Differentiation state affects morphine induced cell regulation in neuroblastoma cultured cells
    Giovina Fiore
    Department of Pharmacology, University of Siena, Italy
    Neurosci Lett 555:51-6. 2013
    ..Therefore, cell differentiation state bimodally affects the cellular regulation activity triggered by morphine in isolated cultured neuroblastoma cells raising concerns about the application of morphine to this type of cancer patients. ..
  50. pmc Analgesic and antineuropathic drugs acting through central cholinergic mechanisms
    Alessandro Bartolini
    University of Florence, Department of Preclinical and Clinical Pharmacology, Italy
    Recent Pat CNS Drug Discov 6:119-40. 2011
    ..At least 9 patents covering novel chemicals for cholinergic system modulation and pain control are discussed...
  51. ncbi Gi/o proteins: expression for direct activation enquiry
    Lorenzo Di Cesare Mannelli
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50134 Florence, Italy
    Protein Expr Purif 47:303-10. 2006
    ..Our results show that recombinant subunits are stable, properly folded and, fully active, which makes them suitable candidates for functional studies...
  52. ncbi Methylamine: a new endogenous modulator of neuron firing?
    Renato Pirisino
    Department of Pharmacology, University of Florence, Florence, Italy
    Med Sci Monit 11:RA257-61. 2005
    ..Moreover, the activity of methylamine as an inducer of NO release suggests a role for the amine and for the enzymatic activity that degrades it in neurodegenerative diseases...
  53. doi A novel manganese complex effective as superoxide anion scavenger and therapeutic agent against cell and tissue oxidative injury
    Paola Failli
    Department of Preclinical and Clinical Pharmacology, University of Florence, V le G Pieraccini 6, Florence, Italy
    J Med Chem 52:7273-83. 2009
    ..MnL4] toxicity was very low on both cell cultures in vitro and mice in vivo. Hence, we propose [MnL4] as a novel stable oxygen radical scavenging molecule, active at low doses and with a low toxicity...
  54. doi Nicotine is a pain reliever in trauma- and chemotherapy-induced neuropathy models
    Lorenzo Di Cesare Mannelli
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50139 Florence, Italy
    Eur J Pharmacol 711:87-94. 2013
    ..These results support the nAChR modulation as a possible therapeutic approach to the complex, undertreated chemotherapy-induced neuropathies...
  55. doi St. John's Wort reduces neuropathic pain through a hypericin-mediated inhibition of the protein kinase Cgamma and epsilon activity
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 50139 Florence, Italy
    Biochem Pharmacol 79:1327-36. 2010
    ..Our results indicate SJW as a prolonged antihyperalgesic treatment through inhibition of PKC isoforms and their phosphorylation...
  56. ncbi Arylpiperazinylalkylpyridazinones and analogues as potent and orally active antinociceptive agents: synthesis and studies on mechanism of action
    Nicoletta Cesari
    Dipartimento di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy
    J Med Chem 49:7826-35. 2006
    ..The antinociception of some of the most interesting new molecules was completely prevented by pretreatment with alpha2-antagonist yohimbine, suggesting the involvement of alpha2-adrenoceptors, as with prototype A...
  57. ncbi The phospholipase C-IP3 pathway is involved in muscarinic antinociception
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale G Pieraccini 6, I 10539 Florence, Italy
    Neuropsychopharmacology 28:888-97. 2003
    ..These results indicate a role for the PLC-IP(3) pathway in central muscarinic analgesia in mice. Furthermore, activation of PKC by cholinomimetic drugs may represent a pathway of negative modulation of muscarinic antinociception...
  58. doi Morphologic features and glial activation in rat oxaliplatin-dependent neuropathic pain
    Lorenzo Di Cesare Mannelli
    Department of Neurosciences, Psychology, Drug Research and Child Health NEUROFARBA, Pharmacology and Toxicology Section, University of Florence, Florence, Italy
    J Pain 14:1585-600. 2013
    ..In particular, on day 21, a significant astrocyte increase was measured in the anterior cingulate cortex, somatosensory area 1, neostriatum, ventrolateral periaqueductal gray, and nucleus raphe magnus...
  59. doi Oxaliplatin-induced neuropathy: oxidative stress as pathological mechanism. Protective effect of silibinin
    Lorenzo Di Cesare Mannelli
    Deparment of Preclinical and Clinical Pharmacology, University of Florence, Florence, Italy
    J Pain 13:276-84. 2012
    ..Antioxidants were also able to improve motor coordination. The antineuropathic effect of both molecules improved by about 50% oxaliplatin-induced behavioral alterations...
  60. pmc Methylamine, but not ammonia, is hypophagic in mouse by interaction with brain Kv1.6 channel subtype
    Renato Pirisino
    Department of Preclinical and Clinical Pharmacology, University of Florence, Viale Pieraccini 6, 50134 Florence, Italy
    Br J Pharmacol 142:381-9. 2004
    ..6 is required only for the activity of MET, and confirms the different action mechanism of ammonia and MET...
  61. doi Liposomal formulations of prilocaine: effect of complexation with hydroxypropyl-ß-cyclodextrin on drug anesthetic efficacy
    Marco Bragagni
    Department of Pharmaceutical Sciences, University of Florence, Florence, Italy
    J Liposome Res 20:315-22. 2010
    ..The technique of double loading was the most effective, giving rise to the shortest onset time and longest duration of anesthetic effect...
  62. ncbi Development, characterization and in vivo evaluation of benzocaine-loaded liposomes
    Paola Mura
    Department of Pharmaceutical Sciences, University of Florence, Italy
    Eur J Pharm Biopharm 67:86-95. 2007
    ..These results suggest that a suitably developed liposomal formulation of benzocaine can be of actual value for improving its clinical effectiveness in topical anaesthesia...
  63. ncbi Design, synthesis, and preliminary pharmacological evaluation of new quinoline derivatives as nicotinic ligands
    Luca Guandalini
    Laboratory of Design, Synthesis and Study of Biologically Active Heterocycles HeteroBioLab, Department of Pharmaceutical Sciences, University of Florence, Via Ugo Schiff 6, I 50019 Sesto Fiorentino, Italy
    J Med Chem 50:4993-5002. 2007
    ..5-10.4 A, interact with the alpha4beta2* nicotinic receptor with Ki in the microM range; compound 3c shows preference for the alpha7* subtype...
  64. ncbi Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage
    Gabriella Guerrini
    Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Firenze, Via U Schiff, 6, 50019 Polo Scientifico, Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 15:2573-86. 2007
    ..These compounds were evaluated also for their binding at Benzodiazepine site on GABA(A) receptor complex (GABA(A)/BzR complex) subtype to evaluate their subtype selectivity...
  65. doi New fluoro derivatives of the pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide system: evaluation of fluorine binding properties in the benzodiazepine site on γ-aminobutyrric acid type A (GABA(A)) receptor. Design, synthesis, biological, and molecular modeling
    Gabriella Guerrini
    Dipartimento di Scienze Farmaceutiche, Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente Attivi HeteroBioLab, Università degli Studi di Firenze, via U Schiff 6, 50019 Polo Scientifico, Sesto Fiorentino, Firenze, Italy
    J Med Chem 53:7532-48. 2010
    ..The fluorine atom was able to form a hydrogen bond interaction only when it is not in position 3...
  66. ncbi Design and study of piracetam-like nootropics, controversial members of the problematic class of cognition-enhancing drugs
    Fulvio Gualtieri
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Curr Pharm Des 8:125-38. 2002
    ..Recent developments which hopefully will lead to a revival of the class are reviewed...
  67. ncbi Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies
    Vittoria Colotta
    Dipartimento di Scienze Farmaceutiche, Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente Attivi, Polo Scientifico, Universita degli Studi di Firenze, Sesto Fiorentino, FI, Italy
    J Med Chem 49:6015-26. 2006
    ..To rationalize the trend of affinities of the reported derivatives, an intensive molecular modeling study was carried out by docking compounds to models of the Gly/NMDA, AMPA, and KA receptors...
  68. ncbi Design, synthesis, and preliminary pharmacological evaluation of a set of small molecules that directly activate gi proteins
    Dina Manetti
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, I 50019 Sesto Fiorentino FI, Italy
    J Med Chem 48:6491-503. 2005
    ..Some of the compounds synthesized and found to be active may be useful leads to develop more potent and selective Gi protein modulators...
  69. ncbi Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain
    Elisabetta Teodori
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, via U Schiff 6, 50019 Sesto Fiorentino FI, Italy
    J Med Chem 47:6070-81. 2004
    ..Two compounds that show N-type calcium channel antagonism and are endowed with potent action on pain and neuropathic pain (3 and 18) have been selected for further studies...
  70. ncbi Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
    Serena Scapecchi
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Bioorg Med Chem 12:71-85. 2004
    ..Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg...
  71. ncbi 2-pyrrolidinone moiety is not critical for the cognition-enhancing activity of piracetam-like drugs
    Serena Scapecchi
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121 Firenze, Italy
    Farmaco 58:715-22. 2003
    ..As found previously in the case of 1,4-diazabicyclo[4.3.0]nonan-9-one compounds, the cognition-enhancing activity of 2-pyrrolidinone compounds is maintained in most cases, suggesting that this moiety is not crucial for activity...
  72. ncbi [(3-Chlorophenyl)piperazinylpropyl]pyridazinones and analogues as potent antinociceptive agents
    Maria Paola Giovannoni
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Gino Capponi 9, 50121 Florence, Italy
    J Med Chem 46:1055-9. 2003
    ..Furthermore, they were also active after icv administration and in the presence of a chemical, painful stimulus (abdominal constriction test)...
  73. doi Alpha2-agonists as analgesic agents
    Maria Paola Giovannoni
    Dipartimento di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino Firenze, Italy
    Med Res Rev 29:339-68. 2009
    ..Finally, the most commonly alpha(2)-agonists used in veterinary medicine are described...
  74. doi Novel 3-aroylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides 8-substituted, ligands at GABAA/benzodiazepine receptor complex: synthesis, pharmacological and molecular modeling studies
    Gabriella Guerrini
    Dipartimento di Scienze Farmaceutiche, Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente attivi HeteroBioLab Università degli Studi di Firenze, Via U Schiff, Sesto Fiorentino Firenze, Italy
    Bioorg Med Chem 16:4471-89. 2008
    ..To rationalize and qualitatively interpret the GABA(A)/Bz binding affinities of compounds 8a and 11, a dynamic molecular modeling study has been performed, with the aim of assessing the preferred geometry of protein-ligand complex...
  75. ncbi 4-amino-5-substituted-3(2H)-pyridazinones as orally active antinociceptive agents: synthesis and studies on the mechanism of action
    Maria Paola Giovannoni
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy
    J Med Chem 50:3945-53. 2007
    ..Further investigation demonstrated an indirect activation of the noradrenergic system through an amplification of noradrenaline release...
  76. doi Synthesis, in vivo evaluation, and molecular modeling studies of new pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide derivatives. Identification of a bifunctional hydrogen bond area related to the inverse agonism
    Gabriella Guerrini
    Dipartimento di Scienze Farmaceutiche, Laboratorio di Progettazione, Sintesi e Studio di Eterocicli Biologicamente Attivi HeteroBioLab, Universita degli Studi di Firenze, via U Schiff 6, 50019 Polo Scientifico, Sesto Fiorentino Firenze, Italy
    J Med Chem 52:4668-82. 2009
    ..This new pharmacophoric model allowed us to identify four structural compound typologies and thus to rationalize the affinity data of all compounds...
  77. ncbi Antisense knockdown of the Shaker-like Kv1.1 gene abolishes the central stimulatory effects of amphetamines in mice and rats
    Carla Ghelardini
    Department of Preclinical and Clinical Pharmacology, University of Florence Viale Pieraccini, Italy
    Neuropsychopharmacology 28:1096-105. 2003
    ..Our results suggest that the stimulant effects of AMPH and chemically related compounds, but not COC, require the presence of functionally active Kv1.1 channels in the brain...
  78. ncbi Indomethacin, caffeine and prochlorperazine alone and combined revert hyperalgesia in in vivo models of migraine
    Nicoletta Galeotti
    Department of Preclinical and Clinical Pharmacology, University of Florence, Florence, Italy
    Pharmacol Res 46:245-50. 2002
    ..These data provide the pharmacologic evidence of the efficacy of IndoProCaf in reverting hyperalgesia, a condition of reduction of pain threshold similar to that occurring in migraine...
  79. ncbi 4-Aminopiperidine derivatives as a new class of potent cognition enhancing drugs
    Dina Manetti
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via G Capponi 9, I 50121, Firenze, Italy
    Bioorg Med Chem Lett 13:2303-6. 2003
    ..One of the new compounds (9, active at 0.01 mg/kg ip) may represent a new lead for the development of cognition enhancers useful to treat the cognitive deficit produced by neurodegenerative pathologies like Alzheimer's disease...
  80. ncbi Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity
    Maurizio Anzini
    Dipartimento Farmaco Chimico Tecnologico, Universita degli Studi di Siena, Via A Moro, 53100 Siena, Italy
    J Med Chem 46:3853-64. 2003
    ..Finally, the potential antinociceptive and antiamnesic properties of compounds 6e and 6i have been investigated by means of the hot-plate and passive avoidance test in mice, respectively...
  81. ncbi Novel potent 5-HT(3) receptor ligands based on the pyrrolidone structure: synthesis, biological evaluation, and computational rationalization of the ligand-receptor interaction modalities
    Andrea Cappelli
    Dipartimento Farmaco Chimico Tecnologico, Universita di Siena, Via A Moro, 53100 Siena, Italy
    Bioorg Med Chem 10:779-801. 2002
    ....
  82. doi Synthesis, in vitro, and in vivo biological evaluation and molecular docking simulations of chiral alcohol and ether derivatives of the 1,5-diarylpyrrole scaffold as novel anti-inflammatory and analgesic agents
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologie del Farmaco, Universita La Sapienza, Piazzale Aldo Moro, 5, I 00185 Roma, Italy
    Bioorg Med Chem 16:8072-81. 2008
    ..The affinity data have been rationalized through docking simulations...
  83. doi Ethyl 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as novel, highly potent, and safe antianxiety agent
    Maurizio Anzini
    Dipartimento Farmaco Chimico Tecnologico, European Research Centre for Drug Discovery and Development, Universita degli Studi di Siena, Via A Moro, 53100 Siena, Italy
    J Med Chem 51:4730-43. 2008
    ....
  84. ncbi Synthesis and biological evaluation of chiral alpha-aminoanilides with central antinociceptive activity
    Filomena Corbo
    Department of Pharmaceutical Chemistry, University of Bari, Via E Orabona n 4, 70125 Bari, Italy
    J Med Chem 50:1907-15. 2007
    ..Among all the synthesized compounds, 3f showed antinociceptive properties with a good enantioselective index...
  85. ncbi Effects of endogenous morphine deprivation on memory retention of passive avoidance learning in mice
    Massimo Guarna
    Department of Anatomical and Biomedical Sciences, University of Siena, Italy
    Int J Neuropsychopharmacol 7:311-9. 2004
    ..These findings support a role for endogenous morphine in weakening memory processes under stress conditions...
  86. doi Synthesis, biological evaluation, and enzyme docking simulations of 1,5-diarylpyrrole-3-alkoxyethyl ethers as selective cyclooxygenase-2 inhibitors endowed with anti-inflammatory and antinociceptive activity
    Maurizio Anzini
    Dipartimento Farmaco Chimico Tecnologico, Universita di Siena, Siena, Italy
    J Med Chem 51:4476-81. 2008
    ..0.5, GRID 21, and MacroModel 8.5 using the complex between COX-2 and SC-558 (1b), refined at a 3 A resolution (Brookhaven Protein Data Bank entry: 6cox )...
  87. ncbi Neurotransmitter role of endogenous morphine in CNS
    Massimo Guarna
    Department of Anatomical and Biomedical Sciences, University of Siena, Italy
    Med Sci Monit 11:RA190-193. 2005
    ..Evidence has been found for its endogenous synthesis in animal tissues as well. These findings indicate that endogenous morphine might function as neuromodulator/neurotransmitter agent in the CNS...
  88. ncbi Enantioselective synthesis and preliminary pharmacological evaluation of the enantiomers of unifiram (DM232), a potent cognition-enhancing agent
    Elisabetta Martini
    Dipartimento di Scienze Farmaceutiche, Universita di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino FI, Italy
    Med Chem 1:473-80. 2005
    ..On the contrary, (R)-(+) and (S)-(-)-(2) showed the same amnesic potency when tested in the passive-avoidance test. These findings may be useful to clarify the mechanism of action of these substances...
  89. doi Synthesis and biological evaluation of novel dimiracetam derivatives useful for the treatment of neuropathic pain
    Carlo Farina
    Brane Discovery, Insubrias BioPark, via Lepetit 34, 21040 Gerenzano, Varese, Italy
    Bioorg Med Chem 16:3224-32. 2008
    ..These results suggest that compounds 5, 7 and 8 might represent novel and well-tolerated therapeutic agents for the relief of neuropathic pain...
  90. ncbi Cyclooxygenase-2 inhibitors. 1,5-diarylpyrrol-3-acetic esters with enhanced inhibitory activity toward cyclooxygenase-2 and improved cyclooxygenase-2/cyclooxygenase-1 selectivity
    Mariangela Biava
    Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Universita La Sapienza, Piazzale Aldo Moro 5, I 00185 Roma, Italy
    J Med Chem 50:5403-11. 2007
    ....
  91. ncbi Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties
    Vincenzo Tumiatti
    Dipartimento di Scienze Farmaceutiche, Universita di Bologna, Via Belmeloro 6, 40126 Bologna, Italy
    Bioorg Med Chem 15:2312-21. 2007
    ..Both compounds were endowed with antinociceptive activity. Furthermore, in microdialysis tests in rat parietal cortex, they enhanced acetylcholine release, most likely by antagonizing presynaptic muscarinic receptor subtypes...
  92. ncbi New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists
    Clementina Manera
    Dipartimento di Scienze Farmaceutiche, Universita di Pisa, Via Bonanno 6, 56126 Pisa, Italy
    Bioorg Med Chem Lett 17:6505-10. 2007
    ..In particular, compounds 2, 5, 11, and 13 showed a high CB(2) affinity and CB(2) versus CB(1) selectivity, in agreement with molecular modeling studies. Furthermore, compound 2 also exhibited in vivo antinociceptive effects...
  93. doi Dopamine is necessary to endogenous morphine formation in mammalian brain in vivo
    Carla Neri
    Institute of Medicine and Public Health, University of Verona, Verona, Italy
    J Neurochem 106:2337-44. 2008
    ..Thus, dopamine and endogenous opiates/opioid peptides may be interconnected in the physiological processes; yet, endogenous morphine may represent a basic link of this chain...