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Antinociception and prevention of hyperalgesia by intrathecal administration of Ro 25-6981, a highly selective antagonist of the 2B subunit of N-methyl-D-aspartate receptor.
Pharmacol Biochem Behav. 2013 Nov; 112:56-63.PB

Abstract

BACKGROUND

NR2B subunits (NMDA receptor 2B subunit) play an important role in generation of pain and forming central sensitization of pain. Ro 25-6981, a highly selective NR2B antagonist, gained much attention in recent years. In this study, we used a rat model of incisional pain to investigate effects of postoperative analgesia and changes of postoperative hyperalgesia induced by remifentanil through the pretreatment of intrathecal administration with Ro 25-6981.

METHODS

The behavioral changes of rats have been evaluated by the paw withdrawal mechanical threshold and paw withdrawal thermal latency after intrathecal injection of Ro 25-6981. The expression of NR2B with tyrosine phosphorylation in the spinal dorsal horn was analyzed by Western blotting.

RESULTS

Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation.

CONCLUSIONS

Intrathecal injection of Ro 25-6981 had significant analgesic effects on incision pain in rats and effectively attenuated postoperative hyperalgesia induced by remifentanil.

Authors+Show Affiliations

Department of Anesthesiology, Drum Tower Hospital, Medical Department of Nanjing University, Nanjing, 210008 Jiangsu Province, PR China.No 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

24076088

Citation

Jiang, Ming, et al. "Antinociception and Prevention of Hyperalgesia By Intrathecal Administration of Ro 25-6981, a Highly Selective Antagonist of the 2B Subunit of N-methyl-D-aspartate Receptor." Pharmacology, Biochemistry, and Behavior, vol. 112, 2013, pp. 56-63.
Jiang M, Zhang W, Ma Z, et al. Antinociception and prevention of hyperalgesia by intrathecal administration of Ro 25-6981, a highly selective antagonist of the 2B subunit of N-methyl-D-aspartate receptor. Pharmacol Biochem Behav. 2013;112:56-63.
Jiang, M., Zhang, W., Ma, Z., & Gu, X. (2013). Antinociception and prevention of hyperalgesia by intrathecal administration of Ro 25-6981, a highly selective antagonist of the 2B subunit of N-methyl-D-aspartate receptor. Pharmacology, Biochemistry, and Behavior, 112, 56-63. https://doi.org/10.1016/j.pbb.2013.09.007
Jiang M, et al. Antinociception and Prevention of Hyperalgesia By Intrathecal Administration of Ro 25-6981, a Highly Selective Antagonist of the 2B Subunit of N-methyl-D-aspartate Receptor. Pharmacol Biochem Behav. 2013;112:56-63. PubMed PMID: 24076088.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Antinociception and prevention of hyperalgesia by intrathecal administration of Ro 25-6981, a highly selective antagonist of the 2B subunit of N-methyl-D-aspartate receptor. AU - Jiang,Ming, AU - Zhang,Wei, AU - Ma,Zhengliang, AU - Gu,Xiaoping, Y1 - 2013/09/27/ PY - 2013/03/26/received PY - 2013/08/08/revised PY - 2013/09/18/accepted PY - 2013/10/1/entrez PY - 2013/10/1/pubmed PY - 2014/7/17/medline KW - Antinociception KW - Hyperalgesia KW - Intrathecal administration KW - N-methyl-d-aspartate receptor KW - Prevention KW - Ro 25-6981 SP - 56 EP - 63 JF - Pharmacology, biochemistry, and behavior JO - Pharmacol Biochem Behav VL - 112 N2 - BACKGROUND: NR2B subunits (NMDA receptor 2B subunit) play an important role in generation of pain and forming central sensitization of pain. Ro 25-6981, a highly selective NR2B antagonist, gained much attention in recent years. In this study, we used a rat model of incisional pain to investigate effects of postoperative analgesia and changes of postoperative hyperalgesia induced by remifentanil through the pretreatment of intrathecal administration with Ro 25-6981. METHODS: The behavioral changes of rats have been evaluated by the paw withdrawal mechanical threshold and paw withdrawal thermal latency after intrathecal injection of Ro 25-6981. The expression of NR2B with tyrosine phosphorylation in the spinal dorsal horn was analyzed by Western blotting. RESULTS: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation. CONCLUSIONS: Intrathecal injection of Ro 25-6981 had significant analgesic effects on incision pain in rats and effectively attenuated postoperative hyperalgesia induced by remifentanil. SN - 1873-5177 UR - https://www.unboundmedicine.com/medline/citation/24076088/Antinociception_and_prevention_of_hyperalgesia_by_intrathecal_administration_of_Ro_25_6981_a_highly_selective_antagonist_of_the_2B_subunit_of_N_methyl_D_aspartate_receptor_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0091-3057(13)00223-2 DB - PRIME DP - Unbound Medicine ER -