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Bradykinin induces peripheral antinociception in PGE2-induced hyperalgesia in mice KU Leuven

Steve Peigneur
BACKGROUND: Bradykinin (BK) is an endogenous peptide involved in vascular permeability and inflammation. It has opposite effects (inducing hyperalgesia or antinociception) when administered directly in the central nervous system. The aim of this study was to evaluate whether BK may also present this dual effect when injected peripherally in a PGE2-induced nociceptive pain model, as well as to investigate the possible mechanisms of action ...

In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt1-DALDA Analogues Vrije Universiteit Brussel

Steven Ballet, Cecilia Betti, Alexandre Novoa, Csaba Tömböly, Christian Helms, Anna Lesniak, Patrycja Kleczkowska, Nga N. Chung, A.w. Lipkowski, Birger Brodin, et al.
Abstract



In this study the ? opioid receptor (MOR) ligands DALDA (Tyr-d-Arg-Phe-Lys-NH2) and Dmt1-DALDA (Dmt-d-Arg-Phe-Lys-NH2, Dmt = 2?,6?-dimethyltyrosine) were glycosylated at the N- or C-terminus. Subsequently, the modified peptides were subjected to in vitro and in vivo evaluation. In contrast to the N-terminally modified peptide (3), all peptide analogues derivatized at the C-terminus (4-7) proved to possess high ...

Comparisons of electroencephalographically derived measures of hypnosis and antinociception in response to standardized stimuli during target-controlled propofol-remifentanil anesthesia Universiteit Gent

Mehrnaz Shoushtarian, Marko M Sahinovic, Anthony R Absalom, Alain Kalmar, Hugo EM Vereecke, David TJ Liley, Michel Struys
BACKGROUND: Current electroencephalogram (EEG)-derived measures provide information on cortical activity and hypnosis but are less accurate regarding subcortical activity, which is expected to vary with the degree of antinociception. Recently, the neurophysiologically based EEG measures of cortical input (CI) and cortical state (CS) have been shown to be prospective indicators of analgesia/antinociception and hypnosis, respectively. In this ...

Multitarget μ-Opioid Receptor Agonists─Neuropeptide FF Receptor Antagonists Induce Potent Antinociception with Reduced Adverse Side Effects Vrije Universiteit Brussel

Jolien De Neve, Khadija Elhabazi, Simon Gonzalez, Claire Herby, Rosine Fellmann-Clauss, Charlotte Martin, Steven Ballet, Frédéric Bihel, Frédéric Simonin

The design of bifunctional compounds is a promising approach toward the development of strong analgesics with reduced side effects. We here report the optimization of the previously published lead peptide KGFF09, which contains opioid receptor agonist and neuropeptide FF receptor antagonist pharmacophores and is shown to induce potent antinociception and reduced side effects. We evaluated the novel hybrid peptides for their in vitro activity ...

Current trends in anesthetic depth and antinociception monitoring : an international survey Universiteit Gent

Sean Coeckelenbergh, Philippe Richebe, Dan Longrois, Alexandre Joosten, Stefan De Hert
Current trends in anesthetic depth (i.e., hypnosis) and antinociception monitoring are unclear. We thus aimed to determine contemporary perspectives on monitoring these components of anesthesia during general anesthesia. Participants received and responded anonymously to an internet-based international survey supported by the European Society of Anaesthesiology and Intensive Care. Comparisons, when applicable, were carried out using Chi(2) ...

In vivo antinociception of potent mu opioid agonist tetrapeptide analogues and comparison with a compact opioid agonist - neurokinin 1 receptor antagonist chimera Vrije Universiteit Brussel

Karel Jules Guillemyn, Patrycja Kleczkowska, Alexandre Novoa, Bart Vandormael, Isabelle Van Den Eynde, P. Kosson, Muhammad Faheem Asim, P.w. Schiller, Mariana Spetea, A.w. Lipkowski, et al.
Abstract
Background: An important limiting factor in the development of centrally acting pharmaceuticals is the bloodbrain
barrier (BBB). Transport of therapeutic peptides through this highly protective physiological barrier remains a
challenge for peptide drug delivery into the central nervous system (CNS). Because the most common strategy to
treat moderate to severe pain consists of the activation of opioid receptors in the ...

Accuracy of the composite variability index as a measure of the balance between nociception and, antinociception during anesthesia Universiteit Gent

Marco M Sahinovic, Douglas J Eleveld, Alain Kalmar, Eleonora H Heeremans, Tom De Smet, Chandran V Seshagiri, Anthony R Absalom, HUGO VEREECKE, Michel Struys
BACKGROUND: The Composite Variability Index (CVI), derived from the electroencephalogram, was developed to assess the antinociception-nociception balance, whereas the Bispectral Index (BIS) was developed to assess the hypnotic state during anesthesia. We studied the relationships between these indices, level of hypnosis (BIS level), and antinociception (predicted remifentanil effect-site concentrations, CeREMI) before and after stimulation. ...

Sedative and antinociceptive effects of dexmedetomidine and buprenorphine after oral transmucosal or intramuscular administration in cats Universiteit Gent

Nathalie Porters, Tim Bosmans, Mariella Debille, Hilde De Rooster, Luc Duchateau, Ingeborgh Polis
Objective: To compare sedation and antinociception after oral transmucosal (OTM) and intramuscular (IM) administration of a dexmedetomidine-buprenorphine combination in healthy adult cats. Study design: Randomized, blinded' crossover study, with 1month washout between treatments. Animals: Six healthy neutered female cats, weighing 5.3-7.5kg. Methods: A combination of dexmedetomidine (40gkg(-1)) and buprenorphine (20gkg(-1)) was administered by ...