In-depth characterization of CGRP receptors in human intracranial arteries
(2003) In European Journal of Pharmacology 481(2-3). p.207-216- Abstract
- The purpose of the present study was to characterize the effects of human (h) alpha- and beta-calcitonin gene-related peptide (CGRP) on intracranial arteries from man and to investigate the presence of mRNA for the calcitonin receptor like receptor (CRLR) and the receptor activity modifying proteins (RAMPs) 1, 2 and 3, in cerebral and middle meningeal arteries with and without endothelium, in microvessels and in the endothelial cells isolated from the human basilar artery. Reverse transcriptase-polymerase chain reaction (RT-PCR) revealed the presence of CRLR, RAMP 1, RAMP 2 and RAMP 3 in cerebral and middle meningeal arteries with and without endothelium as well as in microvessels and in the endothelial cells. Human and rat a- and p-CGRP,... (More)
- The purpose of the present study was to characterize the effects of human (h) alpha- and beta-calcitonin gene-related peptide (CGRP) on intracranial arteries from man and to investigate the presence of mRNA for the calcitonin receptor like receptor (CRLR) and the receptor activity modifying proteins (RAMPs) 1, 2 and 3, in cerebral and middle meningeal arteries with and without endothelium, in microvessels and in the endothelial cells isolated from the human basilar artery. Reverse transcriptase-polymerase chain reaction (RT-PCR) revealed the presence of CRLR, RAMP 1, RAMP 2 and RAMP 3 in cerebral and middle meningeal arteries with and without endothelium as well as in microvessels and in the endothelial cells. Human and rat a- and p-CGRP, amylin, adrenomedullin and [acetamidomethyl-Cys(2,7)]human CGRP induced strong concentration-dependent relaxation of human cerebral and middle meningeal arteries. Removal of the endothelium neither changed the maximum relaxant response nor the pIC(50) values for alpha- and beta-CGRP as compared to the responses in arteries with an intact endothelium. Human alpha-CGRP-(8-37) caused a shift of halpha- and hbeta-CGRP-induced relaxations in cerebral and middle meningeal arteries. Calculation of pK(B) values revealed that halpha-CGRP-(8-37) could not significantly discriminate between relaxations induced by halpha-CGRP (pK(B) around 6.8) and hbeta-CGRP (pK(B) around 5.4). There was no significant difference in pK(B) value of halpha-CGRP-(8-37) on hbeta-CGRP-induced relaxation of human cerebral and middle meningeal arteries with and without endothelium. In conclusion, our molecular and pharmacological data support the existence of a single type of CGRP(1) receptors in the human intracranial circulation. (C) 2003 Elsevier B.V. All rights reserved. (Less)
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/293877
- author
- Jansen-Olesen, I ; Jorgensen, L ; Engel, U and Edvinsson, Lars LU
- organization
- publishing date
- 2003
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- human, calcitonin gene-related peptide, vasomotor response, cerebral, artery, meningeal artery
- in
- European Journal of Pharmacology
- volume
- 481
- issue
- 2-3
- pages
- 207 - 216
- publisher
- Elsevier
- external identifiers
-
- wos:000186925400012
- pmid:14642788
- scopus:0344827157
- ISSN
- 1879-0712
- DOI
- 10.1016/j.ejphar.2003.09.021
- language
- English
- LU publication?
- yes
- id
- 372d328a-2e7c-4668-a76e-18aec1d91a1c (old id 293877)
- date added to LUP
- 2016-04-01 11:44:35
- date last changed
- 2024-02-23 04:15:17
@article{372d328a-2e7c-4668-a76e-18aec1d91a1c,
abstract = {{The purpose of the present study was to characterize the effects of human (h) alpha- and beta-calcitonin gene-related peptide (CGRP) on intracranial arteries from man and to investigate the presence of mRNA for the calcitonin receptor like receptor (CRLR) and the receptor activity modifying proteins (RAMPs) 1, 2 and 3, in cerebral and middle meningeal arteries with and without endothelium, in microvessels and in the endothelial cells isolated from the human basilar artery. Reverse transcriptase-polymerase chain reaction (RT-PCR) revealed the presence of CRLR, RAMP 1, RAMP 2 and RAMP 3 in cerebral and middle meningeal arteries with and without endothelium as well as in microvessels and in the endothelial cells. Human and rat a- and p-CGRP, amylin, adrenomedullin and [acetamidomethyl-Cys(2,7)]human CGRP induced strong concentration-dependent relaxation of human cerebral and middle meningeal arteries. Removal of the endothelium neither changed the maximum relaxant response nor the pIC(50) values for alpha- and beta-CGRP as compared to the responses in arteries with an intact endothelium. Human alpha-CGRP-(8-37) caused a shift of halpha- and hbeta-CGRP-induced relaxations in cerebral and middle meningeal arteries. Calculation of pK(B) values revealed that halpha-CGRP-(8-37) could not significantly discriminate between relaxations induced by halpha-CGRP (pK(B) around 6.8) and hbeta-CGRP (pK(B) around 5.4). There was no significant difference in pK(B) value of halpha-CGRP-(8-37) on hbeta-CGRP-induced relaxation of human cerebral and middle meningeal arteries with and without endothelium. In conclusion, our molecular and pharmacological data support the existence of a single type of CGRP(1) receptors in the human intracranial circulation. (C) 2003 Elsevier B.V. All rights reserved.}},
author = {{Jansen-Olesen, I and Jorgensen, L and Engel, U and Edvinsson, Lars}},
issn = {{1879-0712}},
keywords = {{human; calcitonin gene-related peptide; vasomotor response; cerebral; artery; meningeal artery}},
language = {{eng}},
number = {{2-3}},
pages = {{207--216}},
publisher = {{Elsevier}},
series = {{European Journal of Pharmacology}},
title = {{In-depth characterization of CGRP receptors in human intracranial arteries}},
url = {{http://dx.doi.org/10.1016/j.ejphar.2003.09.021}},
doi = {{10.1016/j.ejphar.2003.09.021}},
volume = {{481}},
year = {{2003}},
}