The calcitonin receptor-like receptor/receptor activity-modifying protein 1 heterodimer can function as a calcitonin gene-related peptide-(8-37)-sensitive adrenomedullin receptor

Eur J Pharmacol. 2002 Aug 30;450(3):237-43. doi: 10.1016/s0014-2999(02)02184-2.

Abstract

The receptor activity-modifying protein (RAMP)/calcitonin receptor-like (CRL) receptor heterodimer is thought to function as a receptor for either a calcitonin gene-related peptide (CGRP) (CRL receptor/RAMP1) or adrenomedullin (CRL receptor/RAMP2 or -3), depending on the RAMP isoform present. We examined the receptor specificity of adrenomedullin-induced increases in cAMP in human embryonic kidney (HEK)293 cells coexpressing human CRL receptor and human RAMP1 or RAMP2. In cells expressing CRL receptor/RAMP1, adrenomedulin-induced increases in cAMP were comparable to those induced by alpha-CGRP, and the CGRP receptor antagonist alpha-CGRP-(8-37), but not the adrenomedullin receptor antagonist adrenomedullin-(22-52), blocked the adrenomedullin-evoked responses. Cells expressing CRL receptor/RAMP2 responded more selectively to adrenomedullin; in this case, the effect was blocked by adrenomedullin-(22-52) but not by alpha-CGRP-(8-37). Real-time quantitative polymerase chain reaction confirmed that cotransfection of CRL receptor and RAMP1 had no effect on the endogenous expression of RAMP2. Thus, CRL receptor/RAMP1 likely functions as an adrenomedullin receptor as well as a CGRP receptor, which may explain why many of the actions of adrenomedullin are potently antagonized by alpha-CGRP-(8-37).

MeSH terms

  • Adrenomedullin
  • Calcitonin Gene-Related Peptide / pharmacology*
  • Calcitonin Receptor-Like Protein
  • Cells, Cultured
  • Cyclic AMP / biosynthesis
  • Humans
  • Intracellular Signaling Peptides and Proteins
  • Membrane Proteins / genetics
  • Membrane Proteins / metabolism*
  • Peptide Fragments / pharmacology*
  • RNA, Messenger / metabolism
  • Receptor Activity-Modifying Protein 1
  • Receptor Activity-Modifying Protein 2
  • Receptor Activity-Modifying Proteins
  • Receptors, Adrenomedullin
  • Receptors, Calcitonin / metabolism*
  • Receptors, Peptide / metabolism*
  • Transfection

Substances

  • CALCRL protein, human
  • Calcitonin Receptor-Like Protein
  • Intracellular Signaling Peptides and Proteins
  • Membrane Proteins
  • Peptide Fragments
  • RAMP1 protein, human
  • RAMP2 protein, human
  • RNA, Messenger
  • Receptor Activity-Modifying Protein 1
  • Receptor Activity-Modifying Protein 2
  • Receptor Activity-Modifying Proteins
  • Receptors, Adrenomedullin
  • Receptors, Calcitonin
  • Receptors, Peptide
  • adrenomedullin (22-52)
  • calcitonin gene-related peptide (8-37)
  • Adrenomedullin
  • Cyclic AMP
  • Calcitonin Gene-Related Peptide