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CGRP activates both the CGRP-R and structurally related amylin 1 receptor (AMY<jats:sub>1<\/jats:sub>-R). The relative effect of erenumab and the small-molecule CGRP-R antagonist, rimegepant, towards the CGRP-R and AMY-R needs to be further characterized.<\/jats:p>\n              <\/jats:sec><jats:sec>\n                <jats:title>Methods<\/jats:title>\n                <jats:p>The effect of CGRP and two CGRP-R antagonists were examined in <jats:italic>Xenopus laevis<\/jats:italic> oocytes expressing human CGRP-R, human AMY<jats:sub>1<\/jats:sub>-R and their subunits.<\/jats:p>\n              <\/jats:sec><jats:sec>\n                <jats:title>Results<\/jats:title>\n                <jats:p>CGRP administered to receptor expressing oocytes induced a concentration-dependent increase in current with the order of potency CGRP-R&gt;\u2009&gt;\u2009AMY<jats:sub>1<\/jats:sub>-R\u2009&gt;\u2009calcitonin receptor (CTR). There was no effect on single\u00a0components of the CGRP-R; calcitonin receptor-like receptor and receptor activity-modifying protein 1. Amylin was only effective on AMY<jats:sub>1<\/jats:sub>-R and CTR. Inhibition potencies (pIC<jats:sub>50<\/jats:sub> values) for erenumab on CGRP induced currents were 10.86 and 9.35 for CGRP-R and AMY<jats:sub>1<\/jats:sub>-R, respectively. Rimegepant inhibited CGRP induced currents with pIC<jats:sub>50<\/jats:sub> values of 11.30 and 9.91 for CGRP-R and AMY<jats:sub>1<\/jats:sub>-R, respectively.<\/jats:p>\n              <\/jats:sec><jats:sec>\n                <jats:title>Conclusion<\/jats:title>\n                <jats:p>Our results demonstrate that erenumab and rimegepant are potent antagonists of CGRP-R and AMY<jats:sub>1<\/jats:sub>-R with 32- and 25-times preference for the CGRP-R over the AMY<jats:sub>1<\/jats:sub>-R, respectively. It is discussed if this difference in affinity between the two receptors is the likely reason why constipation is a common and serious adverse effect during CGRP-R antagonism but less so with CGRP binding antibodies.<\/jats:p>\n              <\/jats:sec>","DOI":"10.1186\/s10194-022-01425-9","type":"journal-article","created":{"date-parts":[[2022,5,26]],"date-time":"2022-05-26T00:03:32Z","timestamp":1653523412000},"update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":20,"title":["Characterization of erenumab and rimegepant on calcitonin gene-related peptide induced responses in Xenopus Laevis oocytes expressing the calcitonin gene-related peptide receptor and the amylin-1 receptor"],"prefix":"10.1186","volume":"23","author":[{"given":"Sanne","family":"Hage La Cour","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Kiki","family":"Juhler","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lisette J. 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