Fig. 1.
Antagonist affinities on CGRP receptors. a, apparent pA2 values for CGRP8–37 on human cells and tissues. For CGRP receptors (CLR/RAMP1), data have been combined from studies on recombinant receptors and also SK-N-MC cells. b, apparent pA2 values for BIBN4096BS on rat (▵) and human (•) cells and tissues. It should be noted that because BIBN4096BS is probably an allosteric antagonist (Hay et al., 2006), the apparent pA2 values are simply to give a guide as to its affinity at the preparations illustrated here. Data for both figures from Hay et al. (2004), updated to 2008 (Sheykhzade et al., 2004; Springer et al., 2004; Kawase et al., 2005; Nodin et al., 2005; Verheggen et al., 2005; Bailey and Hay, 2006; Gupta et al., 2006a,b; Takhshid et al., 2006; Edvinsson et al., 2007; De Mey et al., 2008; Wunder et al., 2008). In addition, an apparent pA2 for BIBN4096BS of 14 on human pial arteries has been reported (Moreno et al., 2002). Where no error bar is shown, the result is from a single study; otherwise n = 2 to 12. HUVEC, human umbilical vein endothelial cells.