Linked Life Data

11714898

Source:http://linkedlifedata.com/resource/pubmed/id/11714898

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
2001-11-20
pubmed:abstractText
Calcitonin gene-related peptide (CGRP) receptors are classified into CGRP subtype 1 (CGRP(1)) and CGRP subtype 2 (CGRP(2)) based on the affinity of the antagonist, human alpha (halpha)-CGRP(8-37). halpha-CGRP(8-37) antagonizes CGRP(1) receptor-mediated responses with high affinity (K(B) < 100 nM) and antagonizes CGRP(2) receptor-mediated responses with low affinity (K(B) > 1 microM). CGRP(2) receptors have been previously reported to mediate relaxation of large porcine coronary arteries because this action is antagonized with low affinity by halpha-CGRP(8-37). In the present study, we used reverse transcription-polymerase chain reaction, radioligand binding, and values from our previously reported isolated tissue experiments to compare the CGRP receptor in porcine coronary arteries with the porcine CGRP(1) receptor stably expressed in human embryonic kidney (HEK) 293 cells. We identified calcitonin receptor-like receptor and receptor activity modifying protein 1 mRNA in coronary arteries. We also found that the ligand binding characteristics of the CGRP receptor in coronary arteries and the cloned CGRP(1) receptor were highly similar. K(I) values for halpha-CGRP(8-37) were 6.6 and 5.7 nM in porcine coronary arteries and the cloned CGRP(1) receptor, respectively. The affinities (K(B)) of halpha-CGRP(8-37) and five other antagonists were 22- to 707-fold lower in functional experiments measuring relaxation of coronary arteries than in radioligand binding experiments. Despite this difference in absolute affinity values, there was a high correlation of the rank order of affinity for the antagonists determined by the two methods. Thus halpha-CGRP(8-37) antagonizes CGRP-induced relaxation of porcine coronary arteries with low affinity at the CGRP(1) receptor. Taken together, these data do not support the existence of the CGRP(2) receptor.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
299
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1086-94
pubmed:dateRevised
2010-11-18
pubmed:meshHeading
pubmed-meshheading:11714898-Animals, pubmed-meshheading:11714898-Calcitonin Gene-Related Peptide, pubmed-meshheading:11714898-Calcitonin Receptor-Like Protein, pubmed-meshheading:11714898-Cells, Cultured, pubmed-meshheading:11714898-Coronary Vessels, pubmed-meshheading:11714898-Humans, pubmed-meshheading:11714898-Intracellular Signaling Peptides and Proteins, pubmed-meshheading:11714898-Iodine Radioisotopes, pubmed-meshheading:11714898-Kinetics, pubmed-meshheading:11714898-Membrane Proteins, pubmed-meshheading:11714898-Polymerase Chain Reaction, pubmed-meshheading:11714898-RNA, Messenger, pubmed-meshheading:11714898-Radioligand Assay, pubmed-meshheading:11714898-Receptor Activity-Modifying Proteins, pubmed-meshheading:11714898-Receptors, Calcitonin, pubmed-meshheading:11714898-Receptors, Calcitonin Gene-Related Peptide, pubmed-meshheading:11714898-Swine
pubmed:year
2001
pubmed:articleTitle
Functional calcitonin gene-related peptide subtype 2 receptors in porcine coronary arteries are identified as calcitonin gene-related peptide subtype 1 receptors by radioligand binding and reverse transcription-polymerase chain reaction.
pubmed:affiliation
Department of Pharmacology, Creighton University School of Medicine, Omaha, Nebraska 68178, USA.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, U.S. Gov't, P.H.S., Research Support, Non-U.S. Gov't