| Chronic treatment with dexmedetomidine desensitizes alpha 2-adrenergic signal transduction. | |
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MedLine Citation:
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PMID: 9164555 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Tolerance to the hypnotic response was induced in rats by chronically infusing dexmedetomidine, a novel alpha 2-adrenergic agonist. The alpha 2-adrenoceptor affinity for dexmedtomidine and para-iodoclonidine was significantly reduced in tolerant rats, while Bmax was uncharged. The ability of pertussis toxin (PTX) to ribosylate guanine nucleotide regulatory proteins (G proteins) ex vivo was reduced in tolerant rats; the quantity of PTX-sensitive G proteins was unchanged. Forskolin-stimulated adenylyl cyclase was less sensitive to inhibition by dexmedetomidine in the tolerant rats; however, acute intraperitoneal injection of dexmedetomidine still reduced cyclic adenosine monophosphate levels in tolerant rats. Both the decrease in ribosylation and the lower alpha 2-adrenoceptor binding affinity may reflect a decrease in the ability of the G protein to couple to the alpha 2-adrenoceptors in the locus coeruleus of tolerant rats. In this state, the alpha 2 adrenoceptors are less capable of transducing the effector response (inhibition of adenylyl cyclase). |
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Authors:
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K Reid; Y Hayashi; J Hsu; P A Maguire; B C Rabin; T Z Guo; M Maze |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Pharmacology, biochemistry, and behavior Volume: 57 ISSN: 0091-3057 ISO Abbreviation: Pharmacol. Biochem. Behav. Publication Date: 1997 May-Jun |
Date Detail:
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Created Date: 1997-07-30 Completed Date: 1997-07-30 Revised Date: 2003-11-14 |
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: 63-71 Citation Subset: IM |
Affiliation:
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Department of Anesthesia, Stanford University, CA, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Adenylate Cyclase
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metabolism Adenylate Cyclase Toxin* Adrenergic alpha-Agonists / pharmacology* Animals Cyclic AMP / metabolism Drug Evaluation, Preclinical Drug Tolerance GTP-Binding Proteins / metabolism Hypnotics and Sedatives / pharmacology* Imidazoles / pharmacology* Infusion Pumps, Implantable Medetomidine Pertussis Toxin* Radioligand Assay Rats Receptors, Adrenergic, alpha-2 / agonists*, metabolism Signal Transduction / drug effects* Time Factors Virulence Factors, Bordetella / pharmacology* |
| Chemical | |
Reg. No./Substance:
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0/Adenylate Cyclase Toxin; 0/Adrenergic alpha-Agonists; 0/Hypnotics and Sedatives; 0/Imidazoles; 0/Receptors, Adrenergic, alpha-2; 0/Virulence Factors, Bordetella; 60-92-4/Cyclic AMP; 86347-14-0/Medetomidine; EC 2.4.2.31/Pertussis Toxin; EC 3.6.1.-/GTP-Binding Proteins; EC 4.6.1.1/Adenylate Cyclase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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