| Bradykinin receptors undergo ligand-induced desensitization. | |
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MedLine Citation:
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PMID: 2158343 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Bradykinin binds to specific cell surface receptors on Rat13 fibroblasts with a high affinity (2.1 nM). Prolonged exposure of cells to the ligand causes a concentration-dependent decline in surface levels of the 2.1 nM receptor from 40,000 receptors per cell to undetectable levels with a t1/2 of approximately 2 h. The decline occurs in parallel with the appearance of an equal number of lower affinity binding sites (40 nM), suggesting that ligand exposure causes desensitization by an alteration in receptor affinity. The affinity change is characterized by a faster rate of ligand dissociation while the rate of association remains unaltered. The observed desensitization is dependent on the presence of active cellular metabolism since (i) it does not occur in whole cells maintained at 4 degrees C and (ii) membranes prepared from Rat13 cells retain their high-affinity sites at 37 degrees C despite extensive ligand exposure. |
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Authors:
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R A Roberts; W J Gullick |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Biochemistry Volume: 29 ISSN: 0006-2960 ISO Abbreviation: Biochemistry Publication Date: 1990 Feb |
Date Detail:
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Created Date: 1990-05-29 Completed Date: 1990-05-29 Revised Date: 2003-11-14 |
Medline Journal Info:
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Nlm Unique ID: 0370623 Medline TA: Biochemistry Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 1975-9 Citation Subset: IM |
Affiliation:
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Imperial Cancer Research Fund, Hammersmith Hospital, London, United Kingdom. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Bradykinin / metabolism* Cell Membrane Cells, Cultured Kinetics Rats Receptors, Bradykinin Receptors, Neurotransmitter / metabolism* |
| Chemical | |
Reg. No./Substance:
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0/Receptors, Bradykinin; 0/Receptors, Neurotransmitter; 58-82-2/Bradykinin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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