Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
37
|
| pubmed:dateCreated |
1995-10-30
|
| pubmed:abstractText |
The human 5-HT1A receptor was expressed in Sf9 insect cells to examine desensitization as manifested by agonist-induced uncoupling from G proteins and second messengers. New binding sites were detected after infection of cells with the 5-HT1A receptor-bearing baculovirus. 5-HT1A receptor agonists caused inhibition of cAMP accumulation that could be attenuated by specific receptor antagonists. Brief pretreatment with 5-HT resulted in (1) an uncoupling of receptor from G proteins as evidenced by a loss of high-affinity agonist binding sites and a diminished ability of the receptor to increase incorporation of AA-GTP into endogenous Go alpha-like G proteins, (2) a decreased ability of the receptor to inhibit cAMP accumulation, and (3) increased phosphorylation of the 5-HT1A receptor on serine and threonine residues. Phosphorylation occurred in the presence of a number of cyclic nucleotide dependent kinase inhibitors, and desensitization of the cAMP response occurred in the presence of H-7 and also in cells with prolonged exposure to PMA. Both phosphorylation and desensitization were markedly attenuated by 100 nM and 1 microM heparin and demonstrated similar time courses and concentration-response relationships. Those results demonstrate a close association between agonist-induced desensitization and phosphorylation of the 5-HT1A receptor in Sf9 cells through a pathway that mainly does not involve protein kinase A or C and might involve a G protein-linked receptor kinase.
|
| pubmed:grant | |
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/8-Hydroxy-2-(di-n-propylamino)tetral...,
http://linkedlifedata.com/resource/pubmed/chemical/Cyclic AMP,
http://linkedlifedata.com/resource/pubmed/chemical/DNA Primers,
http://linkedlifedata.com/resource/pubmed/chemical/GTP-Binding Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Phorbol 12,13-Dibutyrate,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin, 5-HT1,
http://linkedlifedata.com/resource/pubmed/chemical/Recombinant Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Sep
|
| pubmed:issn |
0006-2960
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
19
|
| pubmed:volume |
34
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
11954-62
|
| pubmed:dateRevised |
2007-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:7547932-8-Hydroxy-2-(di-n-propylamino)tetralin,
pubmed-meshheading:7547932-Animals,
pubmed-meshheading:7547932-Baculoviridae,
pubmed-meshheading:7547932-Base Sequence,
pubmed-meshheading:7547932-Binding Sites,
pubmed-meshheading:7547932-Cell Line,
pubmed-meshheading:7547932-Cyclic AMP,
pubmed-meshheading:7547932-DNA Primers,
pubmed-meshheading:7547932-GTP-Binding Proteins,
pubmed-meshheading:7547932-Humans,
pubmed-meshheading:7547932-Kinetics,
pubmed-meshheading:7547932-Molecular Sequence Data,
pubmed-meshheading:7547932-Phorbol 12,13-Dibutyrate,
pubmed-meshheading:7547932-Phosphorylation,
pubmed-meshheading:7547932-Receptors, Serotonin,
pubmed-meshheading:7547932-Receptors, Serotonin, 5-HT1,
pubmed-meshheading:7547932-Recombinant Proteins,
pubmed-meshheading:7547932-Second Messenger Systems,
pubmed-meshheading:7547932-Serotonin,
pubmed-meshheading:7547932-Spodoptera
|
| pubmed:year |
1995
|
| pubmed:articleTitle |
Agonist-induced desensitization and phosphorylation of human 5-HT1A receptor expressed in Sf9 insect cells.
|
| pubmed:affiliation |
Department of Medicine (Nephrology Section), Duke University, Durham, North Carolina, USA.
|
| pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.
|