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Enza Maria Galati - One of the best experts on this subject based on the ideXlab platform.

  • ursolic acid plays a role in nepeta sibthorpii bentham cns depressing effects
    Phytotherapy Research, 2007
    Co-Authors: Maria Fernanda Taviano, Natalizia Miceli, M. T. Monforte, Olga Tzakou, Enza Maria Galati
    Abstract:

    The sedative, anticonvulsant and analgesic activity of ursolic acid, a terpenoid bioassay-isolated from Nepeta sibthorpii Bentham, was evaluated in mice. The oral administration of ursolic acid (2.3 mg/kg) produced a significant depressant effect on CNS by reducing spontaneous motor activity and the number and lethality of pentylenetetrazol (PTZ)-induced seizures. Two models of nociception, the writhing Test and the Hot Plate Test, were also used to examine the analgesic effect of ursolic acid. At a dose of 2.3 mg/kg, ursolic acid caused an inhibition of acetic acid-induced abdominal constriction, but was inactive in the Hot Plate Test. Treatment at a higher dose (20 mg/kg) significantly increased the reaction time in the Hot Plate Test. This effect, reversed by naloxone, evidently involves opioid receptors, but the analgesic activity of ursolic acid may be related also to the antiinflammatory and antioxidant properties of this compound. Copyright © 2007 John Wiley & Sons, Ltd.

  • Ursolic acid plays a role in Nepeta sibthorpii Bentham CNS depressing effects
    Phytotherapy research : PTR, 2007
    Co-Authors: Maria Fernanda Taviano, Natalizia Miceli, M. T. Monforte, Olga Tzakou, Enza Maria Galati
    Abstract:

    The sedative, anticonvulsant and analgesic activity of ursolic acid, a terpenoid bioassay-isolated from Nepeta sibthorpii Bentham, was evaluated in mice. The oral administration of ursolic acid (2.3 mg/kg) produced a significant depressant effect on CNS by reducing spontaneous motor activity and the number and lethality of pentylenetetrazol (PTZ)-induced seizures. Two models of nociception, the writhing Test and the Hot Plate Test, were also used to examine the analgesic effect of ursolic acid. At a dose of 2.3 mg/kg, ursolic acid caused an inhibition of acetic acid-induced abdominal constriction, but was inactive in the Hot Plate Test. Treatment at a higher dose (20 mg/kg) significantly increased the reaction time in the Hot Plate Test. This effect, reversed by naloxone, evidently involves opioid receptors, but the analgesic activity of ursolic acid may be related also to the antiinflammatory and antioxidant properties of this compound.

Maria Fernanda Taviano - One of the best experts on this subject based on the ideXlab platform.

  • ursolic acid plays a role in nepeta sibthorpii bentham cns depressing effects
    Phytotherapy Research, 2007
    Co-Authors: Maria Fernanda Taviano, Natalizia Miceli, M. T. Monforte, Olga Tzakou, Enza Maria Galati
    Abstract:

    The sedative, anticonvulsant and analgesic activity of ursolic acid, a terpenoid bioassay-isolated from Nepeta sibthorpii Bentham, was evaluated in mice. The oral administration of ursolic acid (2.3 mg/kg) produced a significant depressant effect on CNS by reducing spontaneous motor activity and the number and lethality of pentylenetetrazol (PTZ)-induced seizures. Two models of nociception, the writhing Test and the Hot Plate Test, were also used to examine the analgesic effect of ursolic acid. At a dose of 2.3 mg/kg, ursolic acid caused an inhibition of acetic acid-induced abdominal constriction, but was inactive in the Hot Plate Test. Treatment at a higher dose (20 mg/kg) significantly increased the reaction time in the Hot Plate Test. This effect, reversed by naloxone, evidently involves opioid receptors, but the analgesic activity of ursolic acid may be related also to the antiinflammatory and antioxidant properties of this compound. Copyright © 2007 John Wiley & Sons, Ltd.

  • Ursolic acid plays a role in Nepeta sibthorpii Bentham CNS depressing effects
    Phytotherapy research : PTR, 2007
    Co-Authors: Maria Fernanda Taviano, Natalizia Miceli, M. T. Monforte, Olga Tzakou, Enza Maria Galati
    Abstract:

    The sedative, anticonvulsant and analgesic activity of ursolic acid, a terpenoid bioassay-isolated from Nepeta sibthorpii Bentham, was evaluated in mice. The oral administration of ursolic acid (2.3 mg/kg) produced a significant depressant effect on CNS by reducing spontaneous motor activity and the number and lethality of pentylenetetrazol (PTZ)-induced seizures. Two models of nociception, the writhing Test and the Hot Plate Test, were also used to examine the analgesic effect of ursolic acid. At a dose of 2.3 mg/kg, ursolic acid caused an inhibition of acetic acid-induced abdominal constriction, but was inactive in the Hot Plate Test. Treatment at a higher dose (20 mg/kg) significantly increased the reaction time in the Hot Plate Test. This effect, reversed by naloxone, evidently involves opioid receptors, but the analgesic activity of ursolic acid may be related also to the antiinflammatory and antioxidant properties of this compound.

Tatsuo Yamamoto - One of the best experts on this subject based on the ideXlab platform.

  • analgesic effect of intrathecally administered orexin a in the rat formalin Test and in the rat Hot Plate Test
    British Journal of Pharmacology, 2002
    Co-Authors: Tatsuo Yamamoto, Natsuko Nozakitaguchi, Tanemichi Chiba
    Abstract:

    1. Orexin-A and orexin-B (also known as hypocretin-1 and hypocretin-2) are hypothalamic peptides and regulate feeding behaviour, energy metabolism and the sleep-wake cycle. Orexin-A binds equally to both orexin-1 and orexin-2 receptors, while orexin-B has a preferential affinity for orexin-2 receptors. 2. Orexins are also known to be concentrated in superficial laminae of the spinal dorsal horn, and orexin-A and orexin-1 receptors are found in the dorsal root ganglion cells. 3. In the present study, the authors examined the effect of intrathecal injection of either orexin-A or orexin-B in the rat formalin Test (a model of inflammatory pain) and in the rat Hot Plate Test. The paw formalin injection induces biphasic flinching (phase 1: 0-6 min; phase 2: 10-60 min) of the injected paw. 4. Intrathecal injection of orexin-A, but not orexin-B, decreased the sum of flinches in phases 1 and 2 in the formalin Test and increased the Hot Plate latency. These effects of orexin-A were completely antagonized by pre-treatment with SB-334867, a selective orexin-1 receptor antagonist. Intrathecal injection of SB-334867 alone had no effect in the formalin Test or in the Hot Plate Test. 5. Intrathecal injection of orexin-A suppressed the expression of Fos-like immunoreactivity (Fos-LI), induced by paw formalin injection, in laminae I-II of L4-5 of the spinal cord. 6. These data suggest that the spinal orexin-1 receptor is involved in the nociceptive transmission and that the activation of the spinal orexin-1 receptor produces analgesic effects in the rat formalin Test and in the rat Hot Plate Test.

  • Analgesic effect of intrathecally administered orexin‐A in the rat formalin Test and in the rat Hot Plate Test
    British journal of pharmacology, 2002
    Co-Authors: Tatsuo Yamamoto, Natsuko Nozaki-taguchi, Tanemichi Chiba
    Abstract:

    1. Orexin-A and orexin-B (also known as hypocretin-1 and hypocretin-2) are hypothalamic peptides and regulate feeding behaviour, energy metabolism and the sleep-wake cycle. Orexin-A binds equally to both orexin-1 and orexin-2 receptors, while orexin-B has a preferential affinity for orexin-2 receptors. 2. Orexins are also known to be concentrated in superficial laminae of the spinal dorsal horn, and orexin-A and orexin-1 receptors are found in the dorsal root ganglion cells. 3. In the present study, the authors examined the effect of intrathecal injection of either orexin-A or orexin-B in the rat formalin Test (a model of inflammatory pain) and in the rat Hot Plate Test. The paw formalin injection induces biphasic flinching (phase 1: 0-6 min; phase 2: 10-60 min) of the injected paw. 4. Intrathecal injection of orexin-A, but not orexin-B, decreased the sum of flinches in phases 1 and 2 in the formalin Test and increased the Hot Plate latency. These effects of orexin-A were completely antagonized by pre-treatment with SB-334867, a selective orexin-1 receptor antagonist. Intrathecal injection of SB-334867 alone had no effect in the formalin Test or in the Hot Plate Test. 5. Intrathecal injection of orexin-A suppressed the expression of Fos-like immunoreactivity (Fos-LI), induced by paw formalin injection, in laminae I-II of L4-5 of the spinal cord. 6. These data suggest that the spinal orexin-1 receptor is involved in the nociceptive transmission and that the activation of the spinal orexin-1 receptor produces analgesic effects in the rat formalin Test and in the rat Hot Plate Test.

  • Effect of nocistatin and its interaction with nociceptin/orphanin FQ on the rat formalin Test
    Neuroscience letters, 1999
    Co-Authors: Tatsuo Yamamoto, Yoshihiko Sakashita
    Abstract:

    Nocistatin is a 17 amino acid peptide and is processed from prepronociceptin. Nocistatin does not bind to the nociceptin receptor, but nocistatin blocks allodynia induced by nociceptin/orphanin FQ. In this study, we examined the effect of intrathecal nocistatin and its interaction with nociceptin/orphanin FQ in the rat formalin Test and the Hot Plate Test. Intrathecal nocistatin attenuated the formalin induced phase 1, but not phase 2, flinching behavior. Coadministration of nocistatin with nociceptin/orphanin FQ did not block the analgesic effect of nociceptin/orphanin FQ. Nocistatin had no effect on the Hot Plate Test. These data suggest that nocistatin produces analgesic effect in the formalin Test, but not in the Hot Plate Test, and that the mechanisms underlying the analgesic effect of nocistatin is complex.

Jarogniew J. Łuszczki - One of the best experts on this subject based on the ideXlab platform.

  • Synergistic interaction of pregabalin with the synthetic cannabinoid WIN 55,212-2 mesylate in the Hot-Plate Test in mice: an isobolographic analysis.
    Pharmacological reports : PR, 2012
    Co-Authors: Jarogniew J. Łuszczki, Magdalena Florek-Łuszczki
    Abstract:

    Abstract Background The aim of the study was to determine the type of interaction between pregabalin (a 3 rd -generation antiepileptic drug) and WIN 55,212-2 mesylate (WIN – a highly potent non-selective cannabinoid CB1 and CB2 receptor agonist) administered in combination at a fixed ratio of 1:1, in the acute thermal pain model (Hot-Plate Test) in mice. Methods Linear regression analysis was used to evaluate the dose-response relationships between logarithms of drug doses and their resultant maximum possible antinociceptive effects in the mouse Hot-Plate Test. From linear equations, doses were calculated that increased the antinociceptive effect by 30% (ED 30 values) for pregabalin, WIN, and their combination. The type of interaction between pregabalin and WIN was assessed using the isobolographic analysis. Results Results indicated that both compounds produced a definite antinociceptive effect, and the experimentally-derived ED 30 values for pregabalin and WIN, when applied alone, were 29.4 mg/kg and 10.5 mg/kg, respectively. With isobolography, the experimentally derived ED 30 mix value for the fixed ratio combination of 1:1 was 5.7 mg/kg, and differed significantly from the theoretically calculated ED 30 add value of 19.95 mg/kg (p  Conclusions Isobolographic analysis demonstrated that the combination of WIN with pregabalin at a fixed ratio of 1:1 exerted synergistic interaction in the mouse model of acute thermal pain. If the results from this study could be adapted to clinical settings, the combination of WIN with pregabalin might be beneficial for pain relief in humans.

  • Dose-response relationship analysis of pregabalin doses and their antinociceptive effects in Hot-Plate Test in mice.
    Pharmacological reports : PR, 2010
    Co-Authors: Jarogniew J. Łuszczki
    Abstract:

    The aim of this study was to determine the analgesic effects of pregabalin (a third-generation antiepileptic drug) using the acute thermal pain model (Hot-Plate Test) in mice. Linear regression analysis was used to evaluate a dose-response relationship between logarithms of pregabalin doses and their resultant maximum possible antinociceptive effects (MPAE) using the Hot-Plate Test in mice. From the linear equation of the dose-response relationship, doses of pregabalin that increased antinociceptive effects by 20%, 30%, 40%, and 50% were calculated and amounted to 9.33, 24.80, 65.93, and 175.26 mg/kg, respectively. In conclusion, pregabalin produces analgesic effects in a dose-dependent manner, as demonstrated using the Hot-Plate Test in mice.

  • Synergistic interaction of gabapentin with tiagabine in the Hot-Plate Test in mice: an isobolographic analysis.
    Pharmacological reports : PR, 2009
    Co-Authors: Jarogniew J. Łuszczki, Agnieszka Kołacz, Ewa Wojda, Mirosław Czuczwar, Krzysztof Przesmycki, Stanisław J Czuczwar
    Abstract:

    Abstract This study was aimed at determining the analgesic effect of gabapentin and tiagabine, two antiepileptic drugs that were administered alone and in combination at a fixed ratio of 1:1, in the acute thermal pain model (Hot-Plate Test) in mice. Linear regression analysis was used to evaluate the dose-response relationships between logarithms of antiepileptic drug doses and their resultant maximum possible antinociceptive effects in the mouse Hot-Plate Test. From linear equations, we calculated doses that increased the antinociceptive effect by 50% (ED 50 values) for gabapentin, tiagabine and their combination. The type of interaction between gabapentin and tiagabine was assessed using the isobolographic analysis. Results indicated that both antiepileptic drugs produced the definite antinociceptive effect, and the experimentally derived ED 50 values for gabapentin and tiagabine, when applied alone, were 504.4 mg/kg and 5.67 mg/kg, respectively.With isobolography, the experimentally derived ED 50 mix value for the fixed ratio combination of 1:1 was 139.31 mg/kg and significantly differed from the theoretically calculated ED 50 add value, which was 255.04 mg/kg (p  In conclusion, the combination of tiagabine with gabapentin at a fixed ratio of 1:1 exerted a synergistic interaction in the mouse model of nociceptive pain. If the results from this study could be extrapolated to clinical settings, the combination of tiagabine with gabapentin might be beneficial for pain relief in humans.

Tanemichi Chiba - One of the best experts on this subject based on the ideXlab platform.

  • analgesic effect of intrathecally administered orexin a in the rat formalin Test and in the rat Hot Plate Test
    British Journal of Pharmacology, 2002
    Co-Authors: Tatsuo Yamamoto, Natsuko Nozakitaguchi, Tanemichi Chiba
    Abstract:

    1. Orexin-A and orexin-B (also known as hypocretin-1 and hypocretin-2) are hypothalamic peptides and regulate feeding behaviour, energy metabolism and the sleep-wake cycle. Orexin-A binds equally to both orexin-1 and orexin-2 receptors, while orexin-B has a preferential affinity for orexin-2 receptors. 2. Orexins are also known to be concentrated in superficial laminae of the spinal dorsal horn, and orexin-A and orexin-1 receptors are found in the dorsal root ganglion cells. 3. In the present study, the authors examined the effect of intrathecal injection of either orexin-A or orexin-B in the rat formalin Test (a model of inflammatory pain) and in the rat Hot Plate Test. The paw formalin injection induces biphasic flinching (phase 1: 0-6 min; phase 2: 10-60 min) of the injected paw. 4. Intrathecal injection of orexin-A, but not orexin-B, decreased the sum of flinches in phases 1 and 2 in the formalin Test and increased the Hot Plate latency. These effects of orexin-A were completely antagonized by pre-treatment with SB-334867, a selective orexin-1 receptor antagonist. Intrathecal injection of SB-334867 alone had no effect in the formalin Test or in the Hot Plate Test. 5. Intrathecal injection of orexin-A suppressed the expression of Fos-like immunoreactivity (Fos-LI), induced by paw formalin injection, in laminae I-II of L4-5 of the spinal cord. 6. These data suggest that the spinal orexin-1 receptor is involved in the nociceptive transmission and that the activation of the spinal orexin-1 receptor produces analgesic effects in the rat formalin Test and in the rat Hot Plate Test.

  • Analgesic effect of intrathecally administered orexin‐A in the rat formalin Test and in the rat Hot Plate Test
    British journal of pharmacology, 2002
    Co-Authors: Tatsuo Yamamoto, Natsuko Nozaki-taguchi, Tanemichi Chiba
    Abstract:

    1. Orexin-A and orexin-B (also known as hypocretin-1 and hypocretin-2) are hypothalamic peptides and regulate feeding behaviour, energy metabolism and the sleep-wake cycle. Orexin-A binds equally to both orexin-1 and orexin-2 receptors, while orexin-B has a preferential affinity for orexin-2 receptors. 2. Orexins are also known to be concentrated in superficial laminae of the spinal dorsal horn, and orexin-A and orexin-1 receptors are found in the dorsal root ganglion cells. 3. In the present study, the authors examined the effect of intrathecal injection of either orexin-A or orexin-B in the rat formalin Test (a model of inflammatory pain) and in the rat Hot Plate Test. The paw formalin injection induces biphasic flinching (phase 1: 0-6 min; phase 2: 10-60 min) of the injected paw. 4. Intrathecal injection of orexin-A, but not orexin-B, decreased the sum of flinches in phases 1 and 2 in the formalin Test and increased the Hot Plate latency. These effects of orexin-A were completely antagonized by pre-treatment with SB-334867, a selective orexin-1 receptor antagonist. Intrathecal injection of SB-334867 alone had no effect in the formalin Test or in the Hot Plate Test. 5. Intrathecal injection of orexin-A suppressed the expression of Fos-like immunoreactivity (Fos-LI), induced by paw formalin injection, in laminae I-II of L4-5 of the spinal cord. 6. These data suggest that the spinal orexin-1 receptor is involved in the nociceptive transmission and that the activation of the spinal orexin-1 receptor produces analgesic effects in the rat formalin Test and in the rat Hot Plate Test.