Abstract
| Original language | English |
|---|---|
| Pages (from-to) | 110-120 |
| Number of pages | 11 |
| Journal | British Journal of Pharmacology |
| Volume | 166 |
| Issue number | 1 |
| Early online date | 10 Apr 2012 |
| DOIs | |
| Publication status | Published - May 2012 |
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Keywords
- calcitonin
- CGRP
- adrenomedullin
- intermedin
- amylin
- calcitonin receptor-like receptor
- RAMP
- receptor activity-modifying protein
- prolactin
- hypotension
Cite this
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The pharmacology of adrenomedullin 2/intermedin. / Hong, Yanguo; Hay, Debbie L.; Quirion, Remi; Poyner, David R.
In: British Journal of Pharmacology, Vol. 166, No. 1, 05.2012, p. 110-120.Research output: Contribution to journal › Article
TY - JOUR
T1 - The pharmacology of adrenomedullin 2/intermedin
AU - Hong, Yanguo
AU - Hay, Debbie L.
AU - Quirion, Remi
AU - Poyner, David R.
N1 - © 2011 The Authors. British Journal of Pharmacology © 2011 The British Pharmacological Society.
PY - 2012/5
Y1 - 2012/5
N2 - Adrenomedullin 2 (AM2) or intermedin is a member of the calcitonin gene-related peptide (CGRP)/calcitonin family of peptides and was discovered in 2004. Unlike other members of this family, no unique receptor has yet been identified for it. It is extensively distributed throughout the body. It causes hypotension when given peripherally, but when given into the CNS, it increases blood pressure and causes sympathetic activation. It also increases prolactin release, is anti-diuretic and natriuretic and reduces food intake. Whilst its effects resemble those of AM, it is frequently more potent. Some characterization of AM2 has been done on molecularly defined receptors; the existing data suggest that it preferentially activates the AM receptor formed from calcitonin receptor-like receptor and receptor activity modifying protein 3. On this complex, its potency is generally equivalent to that of AM. There is no known receptor-activity where it is more potent than AM. In tissues and in animals it is frequently antagonised by CGRP and AM antagonists; however, situations exist in which an AM2 response is maintained even in the presence of supramaximal concentrations of these antagonists. Thus, there is a partial mismatch between the pharmacology seen in tissues and that on cloned receptors. The only AM2 antagonists are peptide fragments, and these have limited selectivity. It remains unclear as to whether novel AM2 receptors exist or whether the mismatch in pharmacology can be explained by factors such as metabolism. © 2011 The British Pharmacological Society.
AB - Adrenomedullin 2 (AM2) or intermedin is a member of the calcitonin gene-related peptide (CGRP)/calcitonin family of peptides and was discovered in 2004. Unlike other members of this family, no unique receptor has yet been identified for it. It is extensively distributed throughout the body. It causes hypotension when given peripherally, but when given into the CNS, it increases blood pressure and causes sympathetic activation. It also increases prolactin release, is anti-diuretic and natriuretic and reduces food intake. Whilst its effects resemble those of AM, it is frequently more potent. Some characterization of AM2 has been done on molecularly defined receptors; the existing data suggest that it preferentially activates the AM receptor formed from calcitonin receptor-like receptor and receptor activity modifying protein 3. On this complex, its potency is generally equivalent to that of AM. There is no known receptor-activity where it is more potent than AM. In tissues and in animals it is frequently antagonised by CGRP and AM antagonists; however, situations exist in which an AM2 response is maintained even in the presence of supramaximal concentrations of these antagonists. Thus, there is a partial mismatch between the pharmacology seen in tissues and that on cloned receptors. The only AM2 antagonists are peptide fragments, and these have limited selectivity. It remains unclear as to whether novel AM2 receptors exist or whether the mismatch in pharmacology can be explained by factors such as metabolism. © 2011 The British Pharmacological Society.
KW - calcitonin
KW - CGRP
KW - adrenomedullin
KW - intermedin
KW - amylin
KW - calcitonin receptor-like receptor
KW - RAMP
KW - receptor activity-modifying protein
KW - prolactin
KW - hypotension
UR - http://www.scopus.com/inward/record.url?scp=84856528059&partnerID=8YFLogxK
UR - http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2011.01530.x/abstract
U2 - 10.1111/j.1476-5381.2011.01530.x
DO - 10.1111/j.1476-5381.2011.01530.x
M3 - Article
C2 - 21658025
VL - 166
SP - 110
EP - 120
JO - British Journal of Pharmacology
JF - British Journal of Pharmacology
SN - 0007-1188
IS - 1
ER -