F C Colpaert

Summary

Affiliation: Centre de Recherche Pierre Fabre
Country: France

Publications

  1. ncbi 5-HT(1A) receptor activation: new molecular and neuroadaptive mechanisms of pain relief
    Francis C Colpaert
    Institut de Recherche Pierre Fabre, 3 rue des Satellites, BP 94244, 31432 Toulouse 4, France
    Curr Opin Investig Drugs 7:40-7. 2006
  2. ncbi Evidence that mnesic states govern normal and disordered memory
    F C Colpaert
    Centre de Recherche Pierre Fabre, Castres Cedex, France
    Behav Pharmacol 12:575-89. 2001
  3. ncbi Opiate self-administration as a measure of chronic nociceptive pain in arthritic rats
    F C Colpaert
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Cedex, Castres, France
    Pain 91:33-45. 2001
  4. ncbi Memory of an operant response and of depressed mood retained in activation states of 5-HT(1A) receptors: evidence from rodent models
    F C Colpaert
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, F 81106 Cedex, Castres, France
    Behav Brain Res 117:41-51. 2000
  5. ncbi Paradoxical signal transduction in neurobiological systems
    F C Colpaert
    Centre de Recherche Pierre Fabre 17, Castres, France
    Mol Neurobiol 24:145-68. 2001
  6. ncbi Discovering risperidone: the LSD model of psychopathology
    Francis C Colpaert
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Castres Cedex, France
    Nat Rev Drug Discov 2:315-20. 2003
  7. ncbi High-efficacy 5-HT1A receptor activation causes a curative-like action on allodynia in rats with spinal cord injury
    Francis C Colpaert
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81100 Castres, France
    Eur J Pharmacol 497:29-33. 2004
  8. ncbi Large-amplitude 5-HT1A receptor activation: a new mechanism of profound, central analgesia
    F C Colpaert
    Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81106 Castres Cedex, France
    Neuropharmacology 43:945-58. 2002
  9. ncbi High-efficacy 5-hydroxytryptamine 1A receptor activation counteracts opioid hyperallodynia and affective conditioning
    Francis C Colpaert
    Centre de Recherche Pierre Fabre, Castres, France
    J Pharmacol Exp Ther 316:892-9. 2006
  10. ncbi Induction by antipsychotics of "win-shift" in the drug discrimination paradigm
    Francis Colpaert
    Centre de Recherche Pierre Fabre, 17, avenue Moulin, F 81106 Castres Cedex, France
    J Pharmacol Exp Ther 322:288-98. 2007

Detail Information

Publications63

  1. ncbi 5-HT(1A) receptor activation: new molecular and neuroadaptive mechanisms of pain relief
    Francis C Colpaert
    Institut de Recherche Pierre Fabre, 3 rue des Satellites, BP 94244, 31432 Toulouse 4, France
    Curr Opin Investig Drugs 7:40-7. 2006
    ..Although awaiting proof-of-concept evidence in humans, high-efficacy 5-HT(1A) receptor activation may uniquely challenge the opioids for pain therapy...
  2. ncbi Evidence that mnesic states govern normal and disordered memory
    F C Colpaert
    Centre de Recherche Pierre Fabre, Castres Cedex, France
    Behav Pharmacol 12:575-89. 2001
    ..The changes of mnesic state that are likely associated with excessively labile cholinergic neurotransmission may conceivably cause the complex disabilities of Alzheimer's disease...
  3. ncbi Opiate self-administration as a measure of chronic nociceptive pain in arthritic rats
    F C Colpaert
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Cedex, Castres, France
    Pain 91:33-45. 2001
    ..Paralleling patient-controlled analgesic drug intake, FSA offers a specific measure allowing the dynamic effects of neurobiological agents to be studied in this unique animal model of persistent nociceptive pain...
  4. ncbi Memory of an operant response and of depressed mood retained in activation states of 5-HT(1A) receptors: evidence from rodent models
    F C Colpaert
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, F 81106 Cedex, Castres, France
    Behav Brain Res 117:41-51. 2000
    ..It is suggested that depression may in part be acquired in the course of ontogeny and may be available for retrieval in the same but not in other states; various biological rhythms conceivably define such states...
  5. ncbi Paradoxical signal transduction in neurobiological systems
    F C Colpaert
    Centre de Recherche Pierre Fabre 17, Castres, France
    Mol Neurobiol 24:145-68. 2001
    ..The transduction mechanism defines a continuously evolving process; the process's most peculiar feature is that it makes any input generate not one but two outcomes that are paradoxical, or opposite in sign...
  6. ncbi Discovering risperidone: the LSD model of psychopathology
    Francis C Colpaert
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Castres Cedex, France
    Nat Rev Drug Discov 2:315-20. 2003
    ..These concepts enabled the discovery of the antipsychotic risperidone, a unique full antagonist of the interoceptive effects of LSD...
  7. ncbi High-efficacy 5-HT1A receptor activation causes a curative-like action on allodynia in rats with spinal cord injury
    Francis C Colpaert
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81100 Castres, France
    Eur J Pharmacol 497:29-33. 2004
    ..F 13640-induced analgesia persisted during this post-treatment period. The data offer initial evidence that high-efficacy 5-HT(1A) receptor activation produces an unprecedented curative-like action on pathological pain...
  8. ncbi Large-amplitude 5-HT1A receptor activation: a new mechanism of profound, central analgesia
    F C Colpaert
    Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81106 Castres Cedex, France
    Neuropharmacology 43:945-58. 2002
    ....
  9. ncbi High-efficacy 5-hydroxytryptamine 1A receptor activation counteracts opioid hyperallodynia and affective conditioning
    Francis C Colpaert
    Centre de Recherche Pierre Fabre, Castres, France
    J Pharmacol Exp Ther 316:892-9. 2006
    ..The data also indicate that F 13640 may be effective with opioid-resistant pain. It further is suggested that opioid addiction may represent self-therapy of opioid-induced pathological pain...
  10. ncbi Induction by antipsychotics of "win-shift" in the drug discrimination paradigm
    Francis Colpaert
    Centre de Recherche Pierre Fabre, 17, avenue Moulin, F 81106 Castres Cedex, France
    J Pharmacol Exp Ther 322:288-98. 2007
    ....
  11. ncbi 5-HT1A receptor activation and antidepressant-like effects: F 13714 has high efficacy and marked antidepressant potential
    W Koek
    Centre de Recherche Pierre Fabre, 17 Ave Jean Moulin, 81106 Cedex, Castres, France
    Eur J Pharmacol 420:103-12. 2001
    ....
  12. ncbi Profound, non-opioid analgesia produced by the high-efficacy 5-HT(1A) agonist F 13640 in the formalin model of tonic nociceptive pain
    L Bardin
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, F 81106 Castres Cedex, France
    Pharmacology 67:182-94. 2003
    ....
  13. ncbi Experimental conditions for the continuous subcutaneous infusion of four central analgesics in rats
    L A Bruins Slot
    Centre de Recherche Pierre Fabre 17, avenue Jean Moulin, 81106 Castres Cedex, France
    Pharmacol Biochem Behav 72:943-51. 2002
    ..The conditions identified here appear appropriate for future studies of these four compounds in rat models of chronic pain and neuropathic allodynia...
  14. ncbi How efficacious are 5-HT1B/D receptor ligands: an answer from GTP gamma S binding studies with stably transfected C6-glial cell lines
    P J Pauwels
    Centre de Recherche Pierre Fabre, Laboratory of Cellular and Molecular Neurobiology, Castres, France
    Neuropharmacology 36:499-512. 1997
    ..The results document the utility of using [35S]GTP gamma S binding studies to assess agonist efficacy, and to characterize 5-HT1B/D receptor ligands as apparently neutral antagonists and inverse agonists at the G-protein level...
  15. ncbi Agonist efficacy at the alpha2A-adrenoceptor:G alpha15 fusion protein: an analysis based on Ca2+ responses
    P J Pauwels
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, Castres, France
    Naunyn Schmiedebergs Arch Pharmacol 361:672-9. 2000
    ..In conclusion, the fusion protein approach opens perspectives to quantify intrinsic activities of ligands under controlled experimental conditions of a fixed receptor:G alpha15 protein ratio of 1...
  16. ncbi F 11356, a novel 5-hydroxytryptamine (5-HT) derivative with potent, selective, and unique high intrinsic activity at 5-HT1B/1D receptors in models relevant to migraine
    G W John
    Centre de Recherche Pierre Fabre, Castres Cedex, France
    J Pharmacol Exp Ther 290:83-95. 1999
    ....
  17. ncbi In the formalin model of tonic nociceptive pain, 8-OH-DPAT produces 5-HT1A receptor-mediated, behaviorally specific analgesia
    L Bardin
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, F 81106 Cedex, Castres, France
    Eur J Pharmacol 421:109-14. 2001
    ..e., forepaw treading) of the 5-HT syndrome which 8-OH-DPAT also induces...
  18. ncbi Mutation in a protein kinase C phosphorylation site of the 5-HT1A receptor preferentially attenuates Ca2+ responses to partial as opposed to higher-efficacy 5-HT1A agonists
    T Wurch
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81106 Castres Cedex, France
    Neuropharmacology 44:873-81. 2003
    ..In conclusion, the amplitude of the Ca(2+) responses induced by partial, but not that to fuller 5-HT(1A) receptor agonists, is affected by the Thr(149)Ala mutation of the 5-HT(1A):G(alpha)(15) fusion protein...
  19. ncbi Facilitation of constitutive alpha(2A)-adrenoceptor activity by both single amino acid mutation (Thr(373)Lys) and g(alphao) protein coexpression: evidence for inverse agonism
    P J Pauwels
    Department of Cellular Biology, Centre de Recherche Pierre Fabre, Castres Cedex, France
    J Pharmacol Exp Ther 292:654-63. 2000
    ..The observed spectrum of intrinsic activities for the various ligands suggests that pure, neutral antagonists are rather uncommon in this specified alpha(2A)-AR system...
  20. pmc Partial to complete antagonism by putative antagonists at the wild-type alpha(2C)-adrenoceptor based on kinetic analyses of agonist:antagonist interactions
    P J Pauwels
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81106 Castres Cedex France
    Br J Pharmacol 131:1385-90. 2000
    ..4. In conclusion, kinetic analyses of agonist : antagonist interactions at the alpha(2C) AR demonstrate a wide spectrum of partial to complete antagonism of the low-magnitude Ca(2+) response for structurally related alpha(2) AR ligands...
  21. ncbi F 12511, a novel ACAT inhibitor, and atorvastatin regulate endogenous hypercholesterolemia in a synergistic manner in New Zealand rabbits fed a casein-enriched diet
    D Junquero
    Centre de Recherche Pierre Fabre, 17 Avenue Jean Moulin 81106 Cedex, Castres, France
    Atherosclerosis 155:131-42. 2001
    ..Thus, the combination of the ACAT inhibitor F 12511 with atorvastatin can represent a better approach than either agent alone to regulate lipoprotein metabolism in certain pathophysiological situations...
  22. ncbi Dynamic dopamine-antagonist interactions at recombinant human dopamine D(2short) receptor: dopamine-bound versus antagonist-bound receptor states
    P J Pauwels
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Castres Cedex, France
    J Pharmacol Exp Ther 297:133-40. 2001
    ..These Ca2+ data indicate that putative DA antagonists act differently, in particular, at the DA-bound D(2short) receptor...
  23. ncbi Analysis of ligand activation of alpha 2-adrenoceptor subtypes under conditions of equal G alpha protein stoichiometry
    P J Pauwels
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, Castres, France
    Naunyn Schmiedebergs Arch Pharmacol 363:526-36. 2001
    ..Most antagonists may actually possess partial agonist properties at the alpha2 AR subtypes, which are facilitated by the same mutation in the distal portion of their third intracellular loop...
  24. pmc Real-time analysis of dopamine: antagonist interactions at recombinant human D2long receptor upon modulation of its activation state
    P J Pauwels
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81106 Castres Cedex, France
    Br J Pharmacol 134:88-97. 2001
    ..The observed attenuation of dopamine-mediated Ca(2+) signal generation with different decay-times may underlie distinct properties of the dopaminergic ligands...
  25. pmc Disparate ligand-mediated Ca(2+) responses by wild-type, mutant Ser(200)Ala and Ser(204)Ala alpha(2A)-adrenoceptor: G(alpha15) fusion proteins: evidence for multiple ligand-activation binding sites
    P J Pauwels
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin 81106 Castres Cédex, France
    Br J Pharmacol 130:1505-12. 2000
    ..In conclusion, these Ca(2+) data suggest that multiple activation binding sites exist for these ligands at the alpha(2A) AR, and that their activation may be affected in different ways by the mutations being investigated...
  26. ncbi Modulation of ligand responses by coupling of alpha(2A)-adrenoceptors to diverse G(alpha)-proteins
    P J Pauwels
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, F 81106, Castres Cedex, France
    Biochem Pharmacol 61:1079-92. 2001
    ..0. These data indicate that a single ligand may display different magnitudes of activation at the alpha(2A) AR subtype coupled to chimeric G(alphao) proteins under controlled conditions of alpha(2A) AR: G(alphao)-protein expression...
  27. ncbi Lack of toxic effects of F 12511, a novel potent inhibitor of acyl-coenzyme A: cholesterol O-acyltransferase, on human adrenocortical cells in culture
    D Junquero
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, F 81106 Castres Cedex, France
    Biochem Pharmacol 61:387-98. 2001
    ....
  28. ncbi Promotion of cell growth by stimulation of cloned human 5-HT1D receptor sites in transfected C6-glial cells is highly sensitive to intrinsic activity at 5-HT1D receptors
    P J Pauwels
    Laboratory of Cellular and Molecular Neurobiology, Centre de Recherche Pierre Fabre, Castres, France
    Naunyn Schmiedebergs Arch Pharmacol 354:136-44. 1996
    ..In conclusion, human 5-HT1D receptors are involved in the growth of C6-glial/5-HT1D cells. This cellular response is highly sensitive to the intrinsic activity of compounds at 5-HT1D receptors...
  29. pmc Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1A receptor agonist
    A Newman-Tancredi
    Neurobiology 2 Division, Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, Castres, France
    Br J Pharmacol 156:338-53. 2009
    ..Activation of post-synaptic 5-HT(1A) receptors may provide enhanced therapy against depression. We describe the signal transduction profile of F15599, a novel 5-HT(1A) receptor agonist...
  30. ncbi Repeated treatment with 8-OH-DPAT induces tolerance to its ability to produce the 5-HT1A behavioural syndrome, but not to its ability to attenuate haloperidol-induced catalepsy
    E P Prinssen
    Centre de Recherche Pierre Fabre, Castres, France
    Behav Pharmacol 11:299-305. 2000
    ....
  31. ncbi Sign-reversal during persistent activation in mu-opioid signal transduction
    L A Bruins Slot
    Centre de Recherche Pierre Fabre 17, avenue Jean Moulin, Castres Cedex, F81106, France
    J Theor Biol 215:169-82. 2002
    ..The findings indicate that with opioid signaling systems, transduction mechanisms operate that may cause the sign of the effect to reverse not only when activation is discontinued but also whilst it is maintained at a constant magnitude...
  32. ncbi Heterogeneous ligand-mediated Ca(++) responses at wt and mutant alpha(2A)-adrenoceptors suggest multiple ligand activation binding sites at the alpha(2A)-adrenoceptor
    P J Pauwels
    Centre de Recherche Pierre Fabre, Department of Cellular and Molecular Biology, 17, avenue Jean Moulin, 81106 Castres Cedex, France
    Neuropharmacology 39:2101-11. 2000
    ..The observed heterogeneity of Ca(++) responses produced by different ligands at wt and mutant alpha(2A) AR may be explained by assuming the existence of multiple ligand activation binding sites at the alpha(2A) AR...
  33. ncbi Protective effect of the alpha2-adrenoceptor antagonist, dexefaroxan, against spatial memory deficit induced by cortical devascularization in the adult rat
    P Chopin
    Centre de Recherche Pierre Fabre, 81106 Castres Cedex, France
    Exp Neurol 185:198-200. 2004
    ..A 28-day subcutaneous infusion with dexefaroxan (0.63, 2.5, and 10 mg rat(-1) day(-1)), starting from the moment of the devascularization, protected against this spatial memory deficit...
  34. ncbi A persistent opioid-addiction state of memory
    L A Bruins Slot
    Centre de Recherche Pierre Fabre, Castres Cedex, France
    Behav Pharmacol 14:167-71. 2003
    ..Thus, because tolerance did not develop to the morphine state, an increasingly large body of engrams became encoded in that state, rendering retrieval increasingly dependent...
  35. ncbi Pharmacological profile of F 12511, (S)-2',3', 5'-trimethyl-4'-hydroxy-alpha-dodecylthioacetanilide a powerful and systemic acylcoenzyme A: cholesterol acyltransferase inhibitor
    D Junquero
    Centre de Recherche Pierre Fabre, 81106 Cedex, Castres, France
    Biochem Pharmacol 61:97-108. 2001
    ....
  36. ncbi Evidence for protean agonism of RX 831003 at alpha 2A-adrenoceptors by co-expression with different G alpha protein subunits
    P J Pauwels
    Centre de Recherche Pierre Fabre, Department of Cellular and Molecular Biology, 17, avenue Jean Moulin, 81106 Castres Cedex, France
    Neuropharmacology 42:855-63. 2002
    ..These data indicate that the alpha(2) AR ligand RX 831003 behaves as a protean agonist at the alpha(2A) AR and that its activity is highly dependent on the co-expressed G(alpha) protein subunit...
  37. ncbi Differential signalling of both wild-type and Thr(343)Arg dopamine D(2short) receptor by partial agonists in a G-protein-dependent manner
    P J Pauwels
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, F 81106, Castres, France
    Biochem Pharmacol 62:723-32. 2001
    ....
  38. ncbi Ethanol state dependence involving a lever press response requirement in rats
    L A Bruins Slot
    Centre de Recherche Pierre Fabre, Castres, France
    Behav Pharmacol 10:229-33. 1999
    ..Extensive parametric studies are needed to unravel the apparently subtle conditions that govern the occurrence and features of the state dependence produced by various CNS compounds...
  39. ncbi Sequence and functional analysis of cloned guinea pig and rat serotonin 5-HT1D receptors: common pharmacological features within the 5-HT1D receptor subfamily
    T Wurch
    Laboratory of Cellular and Molecular Neurobiology, Centre de Recherche Pierre Fabre, Castres, France
    J Neurochem 68:410-8. 1997
    ..In conclusion, the pharmacology of the cloned 5-HT1D receptor subtype seems, unlike the 5-HT1B receptor subtype, conserved among various mammal species such as the human, guinea pig, and rat...
  40. pmc Intrinsic activity of the non-prostanoid thromboxane A2 receptor antagonist, daltroban (BM 13,505), in human platelets in vitro and in the rat vasculature in vivo
    F Bertolino
    Centre de Recherche Pierre Fabre, Castres, France
    Br J Pharmacol 115:210-6. 1995
    ....
  41. ncbi The novel analgesic, F 13640, produces intra- and postoperative analgesia in a rat model of surgical pain
    Ivan Kiss
    Klinik für Anästhesie, Intensivmedizin und Schmerztherapie, Alfried Krupp Krankenhaus, 45117 Essen, Germany
    Eur J Pharmacol 523:29-39. 2005
    ..Unlike the opioid, remifentanil, F 13640 caused no hyperalgesia with ongoing postoperative pain, and should remain effective with protracted postoperative use...
  42. ncbi Differential ion current activation by human 5-HT(1A) receptors in Xenopus oocytes: evidence for agonist-directed trafficking of receptor signalling
    Peter Heusler
    Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, F 81106 Castres Cedex, France
    Neuropharmacology 49:963-76. 2005
    ..Together, these results suggest the existence of distinct and agonist-specific signalling states of this receptor...
  43. ncbi The novel analgesic and high-efficacy 5-HT1A receptor agonist F 13640 inhibits nociceptive responses, wind-up, and after-discharges in spinal neurons and withdrawal reflexes
    Hao Jun You
    Center for Sensory Motor Interaction, Laboratory for Experimental Pain Research Aalborg University, Aalborg 9220, Denmark
    Exp Neurol 191:174-83. 2005
    ....
  44. ncbi Effects of the combined continuous administration of morphine and the high-efficacy 5-HT1A agonist, F 13640 in a rat model of trigeminal neuropathic pain
    Kristof R Deseure
    Laboratory of Anesthesiology, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    Eur J Pain 8:547-54. 2004
    ..The stable effects of F 13640 during the second week of treatment surpassed those of morphine and were not improved by the addition of morphine to F 13640...
  45. ncbi Dual, hyperalgesic, and analgesic effects of the high-efficacy 5-hydroxytryptamine 1A (5-HT1A) agonist F 13640 [(3-chloro-4-fluoro-phenyl)-[4-fluoro-4-{[(5-methyl-pyridin-2-ylmethyl)-amino]-methyl}piperidin-1-yl]methanone, fumaric acid salt]: relationship
    Laurent Bardin
    Department of General Pharmacology, Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Castres Cedex, France
    J Pharmacol Exp Ther 312:1034-42. 2005
    ..These results demonstrate that F 13640 induces hyperalgesia and/or analgesia with a time course that parallels the occupancy of 5-HT(1A) receptors and the presence of the compound in blood and brain...
  46. ncbi Curative-like analgesia in a neuropathic pain model: parametric analysis of the dose and the duration of treatment with a high-efficacy 5-HT(1A) receptor agonist
    Kristof Deseure
    Laboratory of Anesthesiology, University of Antwerp, Universiteitsplein 1, 2610 Antwerp, Belgium
    Eur J Pharmacol 568:134-41. 2007
    ....
  47. ncbi Long-lasting descending and transitory short-term spinal controls on deep spinal dorsal horn nociceptive-specific neurons in response to persistent nociception
    Hao Jun You
    Department of Physiology and Pathophysiology, Xi an Jiaotong University School of Medicine, Xi an, Shaanxi 710061, PR China
    Brain Res Bull 75:34-41. 2008
    ....
  48. ncbi Cardiovascular drugs inhibit MMP-9 activity from human THP-1 macrophages
    Yves Rival
    Centre de Recherche Pierre Fabre, Castres Cedex, France
    DNA Cell Biol 23:283-92. 2004
    ..These results show that THP-1 macrophages could be an useful cellular model to investigate effects of compounds on plaque vulnerability through MMP-9 activity...
  49. ncbi Role of spinal 5-HT(1A) receptors in morphine analgesia and tolerance in rats
    Laurent Bardin
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, Castres Cédex F 81106, France
    Eur J Pain 8:253-61. 2004
    ..These findings demonstrate that 5-HT(1A) receptor agonists can act in the spinal cord to produce both hyper- and hypo-algesic effects and play a major role in the opioid analgesia and tolerance...
  50. ncbi Noradrenergic mechanisms in neurodegenerative diseases: a theory
    Marc R Marien
    Centre de Recherche Pierre Fabre, Neurobiology I, 17 avenue Jean Moulin, 81106 Castres Cedex, France
    Brain Res Brain Res Rev 45:38-78. 2004
    ....
  51. ncbi 5-HT1A receptor activation and anti-cataleptic effects: high-efficacy agonists maximally inhibit haloperidol-induced catalepsy
    Eric P M Prinssen
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, F 81106 Cedex, Castres, France
    Eur J Pharmacol 453:217-21. 2002
    ....
  52. ncbi The 5-HT(1A) receptor agonist F 13640 attenuates mechanical allodynia in a rat model of trigeminal neuropathic pain
    Kristof Deseure
    Laboratory of Anesthesiology S4, University of Antwerp, Universiteitsplein 1, B 2610 Antwerp, Belgium
    Eur J Pharmacol 456:51-7. 2002
    ..The present data extend recent evidence that high-efficacy 5-HT(1A) receptor activation constitutes a new mechanism of central analgesia the spectrum of which may also encompass trigeminal neuropathic pain...
  53. ncbi Constitutive coupling of a chimeric dopamine D2/alpha 1B receptor to the phospholipase C pathway: inverse agonism to silent antagonism by neuroleptic drugs
    Thierry Wurch
    Department of Cellular and Molecular Biology, Centre de Recherche Pierre Fabre, Castres Cedex, France
    J Pharmacol Exp Ther 304:380-90. 2003
    ....
  54. ncbi Donitriptan selectively decreases jugular venous oxygen saturation in the anesthetized pig: further insights into its mechanism of action relevant to headache relief
    Robert Letienne
    Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81106 Castres Cedex, France
    J Pharmacol Exp Ther 305:749-54. 2003
    ..Since donitriptan also increased pVCO(2), an effect upon cerebral oxygen consumption and metabolism is suggested in addition to cranial vasoconstriction, which may be relevant to its headache-relieving effects...
  55. ncbi PPARalpha and PPARdelta activators inhibit cytokine-induced nuclear translocation of NF-kappaB and expression of VCAM-1 in EAhy926 endothelial cells
    Yves Rival
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Cedex, Castres, France
    Eur J Pharmacol 435:143-51. 2002
    ..These results show that EAhy926 endothelial cells are an adequate tool to substantiate and characterize inflammatory impacts of PPAR activators...
  56. ncbi Tolerance and inverse tolerance to the hyperalgesic and analgesic actions, respectively, of the novel analgesic, F 13640
    Liesbeth A Bruins Slot
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Castres Cedex, France
    Eur J Pharmacol 466:271-9. 2003
    ..Producing the mirror opposite of morphine's neuroadaptive actions, F 13640 causes an analgesia that becomes more powerful with chronic administration, and this at the expense of the initial hyperalgesia which it may also produce...
  57. ncbi Continuous administration of the 5-hydroxytryptamine1A agonist (3-Chloro-4-fluoro-phenyl)-[4-fluoro-4-[[(5-methyl-pyridin-2-ylmethyl) -amino]-methyl]piperidin-1-yl]-methadone (F 13640) attenuates allodynia-like behavior in a rat model of trigeminal neurop
    Kristof Deseure
    Laboratory of Anesthesiology, Universiteit Antwerpen, Antwerpen, Belgium
    J Pharmacol Exp Ther 306:505-14. 2003
    ..The data presented here suggest that F 13640 may perhaps offer a lasting treatment of trigeminal neuralgia...
  58. ncbi Ca2+ responses in Chinese hamster ovary-K1 cells demonstrate an atypical pattern of ligand-induced 5-HT1A receptor activation
    Petrus J Pauwels
    Centre d Immunologie Pierre Fabre, 5 avenue Napoléon III BP 497, F 74164 Saint Julien en Genevois Cedex, France
    J Pharmacol Exp Ther 307:608-14. 2003
    ..e., F 13640) may in a selective way induce responses that may be not at all be achieved with other ligands (i.e., buspirone). In conclusion, the pharmacology of 5-HT1A receptor ligands seems to be codetermined by the effector pathway...
  59. ncbi The very-high-efficacy 5-HT1A receptor agonist, F 13640, preempts the development of allodynia-like behaviors in rats with spinal cord injury
    Wei ping Wu
    Division of Clinical Neurophysiology, Department of Medical Laboratory Sciences and Technology, Huddinge University Hospital, Huddinge, Sweden
    Eur J Pharmacol 478:131-7. 2003
    ..Importantly, the preemptive effect of F 13640 persisted for 2 months after treatment was discontinued. The data warrant the study of the possible effects of the early administration of F 13640 in patients sustaining spinal cord injury...
  60. ncbi KC 12291: an atypical sodium channel blocker with myocardial antiischemic properties
    Gareth W John
    Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81100 Castres, France
    Cardiovasc Drug Rev 22:17-26. 2004
    ..Cardiac VGSC blockers such as KC 12291, which block cardiac VGSCs in atypical fashion by effectively inhibiting the sustained component of Na+ current, represent, therefore, promising potential antiischemic and cardioprotective drugs...
  61. ncbi Tacrine-scopolamine interactions on state-dependent retrieval
    Liesbeth A Bruins Slot
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Castres Cedex, France
    Psychopharmacology (Berl) 166:33-9. 2003
    ..This study examined the effects of tacrine on scopolamine-induced state-dependence...
  62. ncbi Ability of dopamine antagonists to inhibit the locomotor effects of cocaine in sensitized and non-sensitized C57BL/6 mice depends on the challenge dose
    Eric P M Prinssen
    Centre de Recherche Pierre Fabre, 17 avenue Jean Moulin, 81106 Castres Cedex, France
    Psychopharmacology (Berl) 172:409-14. 2004
    ..A potential issue with these studies is that the same challenge dose is used in sensitized and control conditions even though that dose may occupy different positions on the respective dose-response curves...
  63. ncbi Nociceptive spinal withdrawal reflexes but not spinal dorsal horn wide-dynamic range neuron activities are specifically inhibited by halothane anaesthesia in spinalized rats
    Hao Jun You
    Center for Sensory Motor Interaction SMI, Laboratory for Experimental Pain Research, Aalborg University, Fredrik Bajers Vej 7 D 3, DK 9220 Aalborg, Denmark
    Eur J Neurosci 22:354-60. 2005
    ..We conclude that halothane at high concentrations (1.5-2%) seems to play a predominant inhibitory role via spinal multireceptors on ventral horn (VH) motor neurons, and less on DH sensory WDR neurons, of the spinal cord...