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Research ArticleORIGINAL ARTICLE

Pharmacological Discrimination of Calcitonin Receptor: Receptor Activity-Modifying Protein Complexes

Debbie L. Hay, George Christopoulos, Arthur Christopoulos, David R. Poyner and Patrick M. Sexton
Molecular Pharmacology May 2005, 67 (5) 1655-1665; DOI: https://doi.org/10.1124/mol.104.008615
Debbie L. Hay
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George Christopoulos
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Arthur Christopoulos
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David R. Poyner
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Patrick M. Sexton
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This article has a correction. Please see:

  • Correction to “Pharmacological Discrimination of Calcitonin Receptor: Receptor Activity-Modifying Protein Complexes” - April 01, 2016

Abstract

Calcitonin (CT) receptors dimerize with receptor activity-modifying proteins (RAMPs) to create high-affinity amylin (AMY) receptors, but there is no reliable means of pharmacologically distinguishing these receptors. We used agonists and antagonists to define their pharmacology, expressing the CT(a) receptor alone or with RAMPs in COS-7 cells and measuring cAMP accumulation. Intermedin short, otherwise known as adrenomedullin 2, mirrored the action of αCGRP, being a weak agonist at CT(a), AMY2(a), and AMY3(a) receptors but considerably more potent at AMY1(a) receptors. Likewise, the linear calcitonin gene-related peptide (CGRP) analogs (Cys(ACM)2,7)hαCGRP and (Cys(Et)2,7)hαCGRP were only effective at AMY1(a) receptors, but they were partial agonists. As previously observed in COS-7 cells, there was little induction of the AMY2(a) receptor phenotype; thus, AMY2(a) was not examined further in this study. The antagonist peptide salmon calcitonin8-32 (sCT8-32) did not discriminate strongly between CT and AMY receptors; however, AC187 was a more effective antagonist of AMY responses at AMY receptors, and AC413 additionally showed modest selectivity for AMY1(a) over AMY3(a) receptors. CGRP8-37 also demonstrated receptor-dependent effects. CGRP8-37 more effectively antagonized AMY at AMY1(a) than AMY3(a) receptors, although it was only a weak antagonist of both, but it did not inhibit responses at the CT(a) receptor. Low CGRP8-37 affinity and agonism by linear CGRP analogs at AMY1(a) are the classic signature of a CGRP2 receptor. Our data indicate that careful use of combinations of agonists and antagonists may allow pharmacological discrimination of CT(a), AMY1(a), and AMY3(a) receptors, providing a means to delineate the physiological significance of these receptors.

  • Received October 21, 2004.
  • Accepted February 3, 2005.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 67 (5)
Molecular Pharmacology
Vol. 67, Issue 5
1 May 2005
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Research ArticleORIGINAL ARTICLE

Pharmacological Discrimination of Calcitonin Receptor: Receptor Activity-Modifying Protein Complexes

Debbie L. Hay, George Christopoulos, Arthur Christopoulos, David R. Poyner and Patrick M. Sexton
Molecular Pharmacology May 1, 2005, 67 (5) 1655-1665; DOI: https://doi.org/10.1124/mol.104.008615

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Research ArticleORIGINAL ARTICLE

Pharmacological Discrimination of Calcitonin Receptor: Receptor Activity-Modifying Protein Complexes

Debbie L. Hay, George Christopoulos, Arthur Christopoulos, David R. Poyner and Patrick M. Sexton
Molecular Pharmacology May 1, 2005, 67 (5) 1655-1665; DOI: https://doi.org/10.1124/mol.104.008615
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