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Antinociceptive Agent

The Experts below are selected from a list of 144 Experts worldwide ranked by ideXlab platform

Brigitte Olympe Depelchin – 1st expert on this subject based on the ideXlab platform

  • advantageous safety profile of a dual selective alpha 2c agonist alpha 2a antagonist Antinociceptive Agent
    Fundamental & Clinical Pharmacology, 2014
    Co-Authors: Annie Delaunois, Paul Dedoncker, Marieluce Rosseels, Miranda Cornet, Eric Jnoff, Etienne Hanon, Michel Guyaux, Brigitte Olympe Depelchin

    Abstract:

    : A selective α2C -adrenoceptor (AR) agonist was developed for the treatment of neuropathic pain. The objective was to dissociate analgesic activity from cardiovascular and sedative side effects commonly observed with nonselective Agents. A 2-amino-oxazoline derivative (compound A), identified as a dual α2C -AR agonist/α2A -AR antagonist in in vitro-binding assays, exhibited in vivo efficacy in rodent pain models. Its safety profile was compared with that of clonidine in six different in vivo models. Contrary to clonidine, compound A did not induce hypotension in pentobarbital-anesthetized rats, in conscious spontaneous hypertensive rats, or in telemetered dogs. Both Agents induced similar dose-dependent decreases in heart rate in dogs and rats. In anesthetized pithed rats, clonidine showed dose-dependent hypertension and inhibited electrical nerve stimulation-induced tachycardia at doses close to its efficacious doses in the mouse formalin test, while compound A had much weaker vasoconstrictive and antichronotropic effects. Finally, in a mouse Irwin test, no sedation was observed with compound A at 30-fold its ED50 in the mouse formalin test, while sedative effects of clonidine started from three-fold its ED50 . These data confirm the advantageous safety profile of the new dual α2C -AR agonist/α2A -AR antagonist Agent vs. the nonselective agonist clonidine.

  • Advantageous safety profile of a dual selective alpha(2C) agonist/alpha(2A) antagonist Antinociceptive Agent.
    Fundamental & Clinical Pharmacology, 2013
    Co-Authors: Annie Delaunois, Paul Dedoncker, Marieluce Rosseels, Miranda Cornet, Eric Jnoff, Etienne Hanon, Michel Guyaux, Brigitte Olympe Depelchin

    Abstract:

    : A selective α2C -adrenoceptor (AR) agonist was developed for the treatment of neuropathic pain. The objective was to dissociate analgesic activity from cardiovascular and sedative side effects commonly observed with nonselective Agents. A 2-amino-oxazoline derivative (compound A), identified as a dual α2C -AR agonist/α2A -AR antagonist in in vitro-binding assays, exhibited in vivo efficacy in rodent pain models. Its safety profile was compared with that of clonidine in six different in vivo models. Contrary to clonidine, compound A did not induce hypotension in pentobarbital-anesthetized rats, in conscious spontaneous hypertensive rats, or in telemetered dogs. Both Agents induced similar dose-dependent decreases in heart rate in dogs and rats. In anesthetized pithed rats, clonidine showed dose-dependent hypertension and inhibited electrical nerve stimulation-induced tachycardia at doses close to its efficacious doses in the mouse formalin test, while compound A had much weaker vasoconstrictive and antichronotropic effects. Finally, in a mouse Irwin test, no sedation was observed with compound A at 30-fold its ED50 in the mouse formalin test, while sedative effects of clonidine started from three-fold its ED50 . These data confirm the advantageous safety profile of the new dual α2C -AR agonist/α2A -AR antagonist Agent vs. the nonselective agonist clonidine.

Annie Delaunois – 2nd expert on this subject based on the ideXlab platform

  • advantageous safety profile of a dual selective alpha 2c agonist alpha 2a antagonist Antinociceptive Agent
    Fundamental & Clinical Pharmacology, 2014
    Co-Authors: Annie Delaunois, Paul Dedoncker, Marieluce Rosseels, Miranda Cornet, Eric Jnoff, Etienne Hanon, Michel Guyaux, Brigitte Olympe Depelchin

    Abstract:

    : A selective α2C -adrenoceptor (AR) agonist was developed for the treatment of neuropathic pain. The objective was to dissociate analgesic activity from cardiovascular and sedative side effects commonly observed with nonselective Agents. A 2-amino-oxazoline derivative (compound A), identified as a dual α2C -AR agonist/α2A -AR antagonist in in vitro-binding assays, exhibited in vivo efficacy in rodent pain models. Its safety profile was compared with that of clonidine in six different in vivo models. Contrary to clonidine, compound A did not induce hypotension in pentobarbital-anesthetized rats, in conscious spontaneous hypertensive rats, or in telemetered dogs. Both Agents induced similar dose-dependent decreases in heart rate in dogs and rats. In anesthetized pithed rats, clonidine showed dose-dependent hypertension and inhibited electrical nerve stimulation-induced tachycardia at doses close to its efficacious doses in the mouse formalin test, while compound A had much weaker vasoconstrictive and antichronotropic effects. Finally, in a mouse Irwin test, no sedation was observed with compound A at 30-fold its ED50 in the mouse formalin test, while sedative effects of clonidine started from three-fold its ED50 . These data confirm the advantageous safety profile of the new dual α2C -AR agonist/α2A -AR antagonist Agent vs. the nonselective agonist clonidine.

  • Advantageous safety profile of a dual selective alpha(2C) agonist/alpha(2A) antagonist Antinociceptive Agent.
    Fundamental & Clinical Pharmacology, 2013
    Co-Authors: Annie Delaunois, Paul Dedoncker, Marieluce Rosseels, Miranda Cornet, Eric Jnoff, Etienne Hanon, Michel Guyaux, Brigitte Olympe Depelchin

    Abstract:

    : A selective α2C -adrenoceptor (AR) agonist was developed for the treatment of neuropathic pain. The objective was to dissociate analgesic activity from cardiovascular and sedative side effects commonly observed with nonselective Agents. A 2-amino-oxazoline derivative (compound A), identified as a dual α2C -AR agonist/α2A -AR antagonist in in vitro-binding assays, exhibited in vivo efficacy in rodent pain models. Its safety profile was compared with that of clonidine in six different in vivo models. Contrary to clonidine, compound A did not induce hypotension in pentobarbital-anesthetized rats, in conscious spontaneous hypertensive rats, or in telemetered dogs. Both Agents induced similar dose-dependent decreases in heart rate in dogs and rats. In anesthetized pithed rats, clonidine showed dose-dependent hypertension and inhibited electrical nerve stimulation-induced tachycardia at doses close to its efficacious doses in the mouse formalin test, while compound A had much weaker vasoconstrictive and antichronotropic effects. Finally, in a mouse Irwin test, no sedation was observed with compound A at 30-fold its ED50 in the mouse formalin test, while sedative effects of clonidine started from three-fold its ED50 . These data confirm the advantageous safety profile of the new dual α2C -AR agonist/α2A -AR antagonist Agent vs. the nonselective agonist clonidine.

F Porreca – 3rd expert on this subject based on the ideXlab platform

  • novel met enkephalin analogue a potent systemic mu agonist Antinociceptive Agent
    Pharmacological Research, 1995
    Co-Authors: Chandishwar Nath, G K Patnaikt, W Haqt, K B Mathur, R C Srimal, B N Dhawan, F Porreca

    Abstract:

    Abstract A new met-enkephalin analogue (compound 82/205) was evaluated for its opioidergic activity in mice. The compound showed antinociception (warm water tail-flick test), tolerance, cross tolerance to morphine and physical dependence. The time course of antinociptive effect of the compound was comparable to morphine. The Antinociceptive ED 50 (μmol kg −1 i.p.) values for the compound and morphine base were 5.31 and 7.59, respectively. Its Antinociceptive effect was blocked by naloxone, β-FNA (mu antagonist) and naloxonazine (mu 1 antagonist) but not by ICI 174,864 (delta antagonist). Naloxone precipitated withdrawal jumpings were 2.6 times less in compound 82/205 treated mice than the morphine treated group. The new analogue compound 82/205 is a potent mu agonist Antinociceptive with a possible weak dependence liability.