MK-3207

MK-3207 is an antagonist of the calcitonin gene-related peptide (CGRP) receptor (Ki = 22 pM for the recombinant human receptor). It is selective for the CGRP receptor over adrenomedullin receptor 1 (AM1) and AM2, calcitonin (CT) receptor, and amylin 3 receptor (AMY3, Kis = 16. 0. 1. and 0. µM, respectively) but does inhibit AMY1 to a lesser extent (Ki = 750 pM). MK-3207 inhibits CGRP-induced cAMP production in HEK293 cells expressing the human CGRP receptor (IC50 = 120 pM). It decreases capsaicin-induced forearm dermal vasodilation in rhesus monkeys in a dose-dependent manner.InChI: InChI=1S/C31H29F2N5O3/c32-21-10-19(11-22(33)13-21)25-16-35-31(7-1-2-8-31)29(41)38(25)17-26(39)36-23-6-5-18-14-30(15-20(18)12-23)24-4-3-9-34-27(24)37-28(30)40/h3-6,9-13,25,35H,1-2,7-8,14-17H2,(H,36,39)(H,34,37,40)/t25-,30+/m0/s1 InChIKey: AZAANWYREOQRFB-SETSBSEESA-N SMILES: O=C1[C@]2(CC3=CC(NC(CN4[C@H](C5=CC(F)=CC(F)=C5)CNC6(CCCC6)C4=O)=O)=CC=C3C2)C7=CC=CN=C7N1