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Evaluation of antinociceptive and antioxidant properties of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one in mice.
Naunyn Schmiedebergs Arch Pharmacol. 2013 Jun; 386(6):493-505.NS

Abstract

The aim of this study was to evaluate the influence of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one (LPP1) on nociceptive thresholds in mouse models of persistent pain. Influence of LPP1 on motor coordination and its antioxidant capacity in mouse brain tissue homogenates were also assessed. Pain sensitivity thresholds in animals treated with LPP1 were established using 5 % formalin solution in normoglycemic mice and in streptozotocin (STZ)-treated diabetic mice in the von Frey, hot plate, innocuous, and noxious cold water tests (water at 10 °C and 4 °C, respectively). Motor deficits were assessed in the rotarod test, whereas antioxidant capacities were evaluated using ferric reducing ability of plasma (FRAP) assay, catalase (CAT), and superoxide dismutase (SOD) activities. LPP1was antinociceptive in both phases of the formalin test, in particular, in the late phase (at doses 0.9-30 mg/kg for 66-99 % vs. control normoglycemic mice) and in a statistically significant manner increased nociceptive thresholds in response to mechanical, heat, and noxious cold stimulation in neuropathic mice (at 30 mg/kg for 274, 192, and 316 %, respectively vs. diabetic control). LPP1 did not impair motor coordination of mice in the rotarod revolving at 6 or 18 rpm. In brain tissue homogenates, it demonstrated antioxidant capacity in FRAP assay and increased SOD activity for 63 % (acute administration) and 28 % (chronic administration) vs. control. No influence on CAT activity was observed. LPP1 has significant antinociceptive properties in the formalin model and elevates pain thresholds in neuropathic mice. It has antioxidant capacity and is devoid of negative influence on animals' motor coordination.

Authors+Show Affiliations

Department of Pharmacodynamics, Jagiellonian University, Medical College, Medyczna 9, 30-688, Cracow, Poland. salat.kinga@gmail.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

23494125

Citation

Sałat, Kinga, et al. "Evaluation of Antinociceptive and Antioxidant Properties of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one in Mice." Naunyn-Schmiedeberg's Archives of Pharmacology, vol. 386, no. 6, 2013, pp. 493-505.
Sałat K, Gawlik K, Witalis J, et al. Evaluation of antinociceptive and antioxidant properties of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one in mice. Naunyn Schmiedebergs Arch Pharmacol. 2013;386(6):493-505.
Sałat, K., Gawlik, K., Witalis, J., Pawlica-Gosiewska, D., Filipek, B., Solnica, B., Więckowski, K., & Malawska, B. (2013). Evaluation of antinociceptive and antioxidant properties of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one in mice. Naunyn-Schmiedeberg's Archives of Pharmacology, 386(6), 493-505. https://doi.org/10.1007/s00210-013-0847-2
Sałat K, et al. Evaluation of Antinociceptive and Antioxidant Properties of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one in Mice. Naunyn Schmiedebergs Arch Pharmacol. 2013;386(6):493-505. PubMed PMID: 23494125.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Evaluation of antinociceptive and antioxidant properties of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one in mice. AU - Sałat,Kinga, AU - Gawlik,Katarzyna, AU - Witalis,Jadwiga, AU - Pawlica-Gosiewska,Dorota, AU - Filipek,Barbara, AU - Solnica,Bogdan, AU - Więckowski,Krzysztof, AU - Malawska,Barbara, Y1 - 2013/03/14/ PY - 2012/10/22/received PY - 2013/02/28/accepted PY - 2013/3/16/entrez PY - 2013/3/16/pubmed PY - 2013/12/29/medline SP - 493 EP - 505 JF - Naunyn-Schmiedeberg's archives of pharmacology JO - Naunyn Schmiedebergs Arch Pharmacol VL - 386 IS - 6 N2 - The aim of this study was to evaluate the influence of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one (LPP1) on nociceptive thresholds in mouse models of persistent pain. Influence of LPP1 on motor coordination and its antioxidant capacity in mouse brain tissue homogenates were also assessed. Pain sensitivity thresholds in animals treated with LPP1 were established using 5 % formalin solution in normoglycemic mice and in streptozotocin (STZ)-treated diabetic mice in the von Frey, hot plate, innocuous, and noxious cold water tests (water at 10 °C and 4 °C, respectively). Motor deficits were assessed in the rotarod test, whereas antioxidant capacities were evaluated using ferric reducing ability of plasma (FRAP) assay, catalase (CAT), and superoxide dismutase (SOD) activities. LPP1was antinociceptive in both phases of the formalin test, in particular, in the late phase (at doses 0.9-30 mg/kg for 66-99 % vs. control normoglycemic mice) and in a statistically significant manner increased nociceptive thresholds in response to mechanical, heat, and noxious cold stimulation in neuropathic mice (at 30 mg/kg for 274, 192, and 316 %, respectively vs. diabetic control). LPP1 did not impair motor coordination of mice in the rotarod revolving at 6 or 18 rpm. In brain tissue homogenates, it demonstrated antioxidant capacity in FRAP assay and increased SOD activity for 63 % (acute administration) and 28 % (chronic administration) vs. control. No influence on CAT activity was observed. LPP1 has significant antinociceptive properties in the formalin model and elevates pain thresholds in neuropathic mice. It has antioxidant capacity and is devoid of negative influence on animals' motor coordination. SN - 1432-1912 UR - https://www.unboundmedicine.com/medline/citation/23494125/Evaluation_of_antinociceptive_and_antioxidant_properties_of_3_[4__3_trifluoromethyl_phenyl__piperazin_1_yl]_dihydrofuran_2_one_in_mice_ L2 - https://dx.doi.org/10.1007/s00210-013-0847-2 DB - PRIME DP - Unbound Medicine ER -