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Vol. 299, Issue 3, 1086-1094, December 2001
Department of Pharmacology (B.R.R., M.A.S., W.B.J., P.W.A.) and
Department of Biomedical Sciences (D.D.S.), Creighton University School
of Medicine, Omaha, Nebraska
Calcitonin gene-related peptide (CGRP) receptors are classified
into CGRP subtype 1 (CGRP1) and CGRP subtype 2 (CGRP2) based on the affinity of the antagonist, human 
(h)-CGRP8-37. h-CGRP8-37 antagonizes
CGRP1 receptor-mediated responses with high affinity
(KB < 100 nM) and antagonizes
CGRP2 receptor-mediated responses with low affinity
(KB > 1 µM). CGRP2
receptors have been previously reported to mediate relaxation of large
porcine coronary arteries because this action is antagonized with low affinity by h-CGRP8-37. 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
CGRP1 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 CGRP1 receptor were
highly similar. KI values for
h-CGRP8-37 were 6.6 and 5.7 nM in porcine coronary
arteries and the cloned CGRP1 receptor, respectively. The
affinities (KB) of
h-CGRP8-37 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 h-CGRP8-37 antagonizes CGRP-induced
relaxation of porcine coronary arteries with low affinity at the
CGRP1 receptor. Taken together, these data do not support
the existence of the CGRP2 receptor.
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