| P-7521--a new irreversible opioid ligand. | |
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MedLine Citation:
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PMID: 2558497 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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In the receptor binding assay, P-7521 was a potent opioid ligand which acted mainly on mu receptor. The relative affinity ratio at mu, delta and kappa sites was 66:8:1. The inhibitory effects of P-7521 were 1868 and 6060 times more potent than morphine on the electrically evoked contractions in guinea pig ileum and mouse vas deferens, respectively and were readily antagonized by naloxone and Mr2266. These results indicate that P-7521 acted on mu receptor in guinea pig ileum and mouse vas deferens. In rabbit vas deferens, the compound had no agonist activity, but could antagonize the inhibitory effect of U-50488 H, a kappa agonist, showing the antagonistic characterization was on kappa receptor. The dissociation of P-7521 binding to opioid receptor were very difficult in mu binding assay and bioassays. |
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Authors:
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W Q Jin; L Q Fan; X J Chen; Z Q Chi |
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Publication Detail:
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Type: In Vitro; Journal Article |
Journal Detail:
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Title: Zhongguo yao li xue bao = Acta pharmacologica Sinica Volume: 10 ISSN: 0253-9756 ISO Abbreviation: Zhongguo Yao Li Xue Bao Publication Date: 1989 May |
Date Detail:
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Created Date: 1990-02-15 Completed Date: 1990-02-15 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8100330 Medline TA: Zhongguo Yao Li Xue Bao Country: CHINA |
Other Details:
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Languages: eng Pagination: 205-10 Citation Subset: IM |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Analgesics* Animals Bicyclo Compounds / pharmacology* Bicyclo Compounds, Heterocyclic* Bridged Compounds / pharmacology* Guinea Pigs Male Mice Muscle Contraction / drug effects Rabbits Radioligand Assay Receptors, Opioid / drug effects* Receptors, Opioid, delta Receptors, Opioid, kappa Receptors, Opioid, mu |
| Chemical | |
Reg. No./Substance:
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0/Analgesics; 0/Bicyclo Compounds; 0/Bicyclo Compounds, Heterocyclic; 0/Bridged Compounds; 0/Receptors, Opioid; 0/Receptors, Opioid, delta; 0/Receptors, Opioid, kappa; 0/Receptors, Opioid, mu; 92836-37-8/P 7521 |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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