Linked Life Data

10648634

Source:http://linkedlifedata.com/resource/pubmed/id/10648634

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2000-3-2
pubmed:abstractText
CGP 12177 is a beta-adrenergic receptor (AR) ligand that has been used to characterize the beta3-AR and the putative beta4-AR. The ability of CGP 12177 to activate beta1-AR when overexpressed in vitro and the presence of beta1-AR in tissues expressing putative beta4-AR prompted us to investigate the actions of CGP 12177 at recombinant and natively-expressed beta-AR. CGP 12177 potently activated recombinant rat and human beta1-AR expressed in Chinese hamster ovary cells. This activation, like that of putative beta4-AR, was resistant to blockade by selective and nonselective beta-AR antagonists. Brown fat has been proposed to contain beta4-AR, as evidenced by the presence of CGP 12177-mediated thermogenesis in mice lacking beta3-AR. Therefore, the identity of the receptors mediating CGP 12177 responses in brown fat was examined using wild-type mice and mice lacking beta1-AR or beta3-AR. In wild-type mice, CGP 12177 activated adenylyl cyclase via high- and low-affinity sites. The high-affinity site, but not the low-affinity site, was blocked by CGP 20712 with potency indicating an interaction with beta1-AR. Moreover, the high-affinity site was absent in mice lacking beta1-AR. In contrast, the low-affinity, CGP 20712-resistant activation by CGP 12177 was absent in mice lacking beta3-AR. Rather, activation occurred exclusively through the high-affinity, CGP 20712-sensitive site. These data indicate that the actions of CGP 12177 in brown fat that have been attributed to novel beta-AR (i.e., beta4-AR) are mediated via an atypical interaction with beta1-AR.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0026-895X
pubmed:author
pubmed:issnType
Print
pubmed:volume
57
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
252-8
pubmed:dateRevised
2007-11-14
pubmed:meshHeading
pubmed-meshheading:10648634-Adenylate Cyclase, pubmed-meshheading:10648634-Adipose Tissue, Brown, pubmed-meshheading:10648634-Adrenergic beta-Agonists, pubmed-meshheading:10648634-Adrenergic beta-Antagonists, pubmed-meshheading:10648634-Animals, pubmed-meshheading:10648634-CHO Cells, pubmed-meshheading:10648634-Cricetinae, pubmed-meshheading:10648634-Female, pubmed-meshheading:10648634-Humans, pubmed-meshheading:10648634-Male, pubmed-meshheading:10648634-Mice, pubmed-meshheading:10648634-Mice, Inbred C57BL, pubmed-meshheading:10648634-Mice, Inbred DBA, pubmed-meshheading:10648634-Propanolamines, pubmed-meshheading:10648634-Rats, pubmed-meshheading:10648634-Receptors, Adrenergic, beta, pubmed-meshheading:10648634-Receptors, Adrenergic, beta-1, pubmed-meshheading:10648634-Receptors, Adrenergic, beta-3, pubmed-meshheading:10648634-Recombinant Proteins
pubmed:year
2000
pubmed:articleTitle
beta1-adrenergic receptors mediate beta3-adrenergic-independent effects of CGP 12177 in brown adipose tissue.
pubmed:affiliation
Cellular and Clinical Neurobiology Program, Department of Psychiatry, Wayne State University School of Medicine, Detroit, Michigan, USA.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.