| Antinociceptive mechanism of the spirocyclopiperazinium compound LXM-10 in mice and rats. | |
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MedLine Citation:
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PMID: 20100504 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Drugs typically used to treat pain are limited by their undesirable side effects, which has prompted a search for mechanistically different analgesic agents. We report the antinociception effect of the spirocyclopiperazinium compound LXM-10 via activation of peripheral alpha7 nicotinic and muscarinic acetylcholine receptors in mice. This effect was attenuated by hexamethonium, atropine methylnitrate, methyllycaconitine citrate, tropicamide, bicuculline, and phaclofen. Competition receptor-binding assays in vitro showed that LXM-10 binds with high affinity alpha7 nAchR and with low affinity M4 receptors. Our findings show that the antinociception signaling pathway of LXM-10 underlies activation of peripheral alpha7 nicotinic and possibly of M4 muscarinic receptors, which activate GABA(A) and GABA(B) receptors, resulting in antinociceptive effects without obvious side effects. |
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Authors:
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Yulan Xiong; Xia Zhao; Qi Sun; Runtao Li; Changling Li; Jia Ye |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-01-25 |
Journal Detail:
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Title: Pharmacology, biochemistry, and behavior Volume: 95 ISSN: 1873-5177 ISO Abbreviation: Pharmacol. Biochem. Behav. Publication Date: 2010 Apr |
Date Detail:
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Created Date: 2010-03-01 Completed Date: 2010-07-01 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0367050 Medline TA: Pharmacol Biochem Behav Country: United States |
Other Details:
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Languages: eng Pagination: 192-7 Citation Subset: IM |
Copyright Information:
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2010 Elsevier Inc. All rights reserved. |
Affiliation:
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State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, PR China. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Analgesics
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pharmacology* Animals Female Male Mice Mice, Inbred C57BL Piperazines / pharmacology* Rats Rats, Wistar Receptors, Muscarinic / drug effects Receptors, Nicotinic / drug effects Spiro Compounds / pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/2,4-dimethyl-9-beta-phenylethyl-3-oxo-6, 9-diazaspiro(5.5)undecane chloride; 0/Analgesics; 0/Piperazines; 0/Receptors, Muscarinic; 0/Receptors, Nicotinic; 0/Spiro Compounds |
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