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Analgesic, antioedematous and antioxidant activity of γ-butyrolactone derivatives in rodents.
Behav Pharmacol. 2012 Aug; 23(4):407-16.BP

Abstract

In this paper, the analgesic, antioedematous, motor-impairing and antioxidant properties of four γ-butyrolactone derivatives (BM113, BM113A, BM138 and BM138A) are described. Pain was induced by thermal (hot-plate test), chemical (writhing test) or mechanical (Randall-Selitto model) stimulation. All in-vivo assays were carried out in mice pretreated intraperitoneally with the test compounds, except for the evaluation of anti-inflammatory and analgesic activities in the carrageenan-induced paw oedema model, in which rats were pretreated orally with these compounds. In the hot-plate assay, BM113A and BM138A dose dependently prolonged the latency of the nociceptive reaction. Their analgesic activity, measured as a median effective dose (ED(50)=4.7 mg/kg), was similar to that of morphine (2.4 mg/kg). In the writhing test, all four compounds, in particular BM113A and BM138A, showed higher potency than the reference drug acetylsalicylic acid (the ED(50) values were 3.7, 2.3 and 46.1 mg/kg, respectively). BM138 caused a dose-dependent diminution of paw oedema (up to 49%) in the carrageenan model and BM138A at 200 mg/kg reduced mechanical hyperalgesia in the Randall-Selitto test (∼30% when compared with the control). None of the γ-butyrolactone derivatives tested at the ED(50) obtained in the hot-plate test influenced the locomotor activity of mice, although in the rotarod test at 24 rpm, BM113A and BM138 at 100 mg/kg showed some motor-impairing properties. In vitro, a concentration-dependent ABTS radical cation-scavenging activity of BM138 and BM138A (up to 80% inhibition of the radical absorbance) was observed. The results of the present study suggest that BM138 and BM138A could be of interest for future investigations as antinociceptive and antioedematous agents with potential free radical-scavenging properties.

Authors+Show Affiliations

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

Pub Type(s)

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

Language

eng

PubMed ID

22785386

Citation

Salat, Kinga, et al. "Analgesic, Antioedematous and Antioxidant Activity of Γ-butyrolactone Derivatives in Rodents." Behavioural Pharmacology, vol. 23, no. 4, 2012, pp. 407-16.
Salat K, Librowski T, Moniczewski A, et al. Analgesic, antioedematous and antioxidant activity of γ-butyrolactone derivatives in rodents. Behav Pharmacol. 2012;23(4):407-16.
Salat, K., Librowski, T., Moniczewski, A., Stanisz-Wallis, K., Wieckowski, K., & Malawska, B. (2012). Analgesic, antioedematous and antioxidant activity of γ-butyrolactone derivatives in rodents. Behavioural Pharmacology, 23(4), 407-16. https://doi.org/10.1097/FBP.0b013e3283566042
Salat K, et al. Analgesic, Antioedematous and Antioxidant Activity of Γ-butyrolactone Derivatives in Rodents. Behav Pharmacol. 2012;23(4):407-16. PubMed PMID: 22785386.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Analgesic, antioedematous and antioxidant activity of γ-butyrolactone derivatives in rodents. AU - Salat,Kinga, AU - Librowski,Tadeusz, AU - Moniczewski,Andrzej, AU - Stanisz-Wallis,Krystyna, AU - Wieckowski,Krzysztof, AU - Malawska,Barbara, PY - 2012/7/13/entrez PY - 2012/7/13/pubmed PY - 2012/12/10/medline SP - 407 EP - 16 JF - Behavioural pharmacology JO - Behav Pharmacol VL - 23 IS - 4 N2 - In this paper, the analgesic, antioedematous, motor-impairing and antioxidant properties of four γ-butyrolactone derivatives (BM113, BM113A, BM138 and BM138A) are described. Pain was induced by thermal (hot-plate test), chemical (writhing test) or mechanical (Randall-Selitto model) stimulation. All in-vivo assays were carried out in mice pretreated intraperitoneally with the test compounds, except for the evaluation of anti-inflammatory and analgesic activities in the carrageenan-induced paw oedema model, in which rats were pretreated orally with these compounds. In the hot-plate assay, BM113A and BM138A dose dependently prolonged the latency of the nociceptive reaction. Their analgesic activity, measured as a median effective dose (ED(50)=4.7 mg/kg), was similar to that of morphine (2.4 mg/kg). In the writhing test, all four compounds, in particular BM113A and BM138A, showed higher potency than the reference drug acetylsalicylic acid (the ED(50) values were 3.7, 2.3 and 46.1 mg/kg, respectively). BM138 caused a dose-dependent diminution of paw oedema (up to 49%) in the carrageenan model and BM138A at 200 mg/kg reduced mechanical hyperalgesia in the Randall-Selitto test (∼30% when compared with the control). None of the γ-butyrolactone derivatives tested at the ED(50) obtained in the hot-plate test influenced the locomotor activity of mice, although in the rotarod test at 24 rpm, BM113A and BM138 at 100 mg/kg showed some motor-impairing properties. In vitro, a concentration-dependent ABTS radical cation-scavenging activity of BM138 and BM138A (up to 80% inhibition of the radical absorbance) was observed. The results of the present study suggest that BM138 and BM138A could be of interest for future investigations as antinociceptive and antioedematous agents with potential free radical-scavenging properties. SN - 1473-5849 UR - https://www.unboundmedicine.com/medline/citation/22785386/Analgesic_antioedematous_and_antioxidant_activity_of_γ_butyrolactone_derivatives_in_rodents_ L2 - https://doi.org/10.1097/FBP.0b013e3283566042 DB - PRIME DP - Unbound Medicine ER -