Table 1

KI values of CGRP analogs in pig coronary arteries and in pig CGRP1 receptor-transfected HEK 293 cells

LigandPig Coronary ArteriesTransfected CGRP1 Receptor
KIHill Slope1-aKIHill Slope1-a
nM nM
hα-CGRP0.11  ± .08−0.940.08  ± 0.01−0.85
[N-benzoyl]hα-CGRP8–37 0.271-b 0.072  ± 0.006−0.96
[N-acetyl]hα-CGRP8–37 1.3  ± 0.8−0.821.3  ± 0.05−0.82
hα-CGRP8–37 6.6  ± 6.3−0.905.7  ± 1.7−0.84
[Pro14]hα-CGRP9.0  ± 6.3−0.705.5  ± 1.3−0.80
[D-Pen2,7]hα-CGRP21.0  ± 5.9−0.9315.2  ± 2.7−0.95
Adrenomedullin19.9  ± 11.6−0.9719.9  ± 12.9−0.80
[Cys(ACM)2,7]hα-CGRP38.4  ± 25.2−0.8132.0  ± 5.8−0.82
[Cha37]hα-CGRP8–37 32.7  ± 13.6−0.9637.9  ± 4.3−0.90
[Pro34,Phe35]hα-CGRP27–37 50.7  ± 16.7−1.05118.2  ± 40.2−1.10
[Ala37]hα-CGRP8–37 499.9  ± 265−1.001021  ± 200−0.53
CalcitoninNo bindingNo binding

Each value represents the mean ± S.E.M. of three to five separate membrane preparations, each from a different pig or from a different group of cells. A two-tailed t test of pKI values found no significant differences (p < 0.05) for any of these peptides when comparing their affinities for membranes from pig coronary arteries to their affinities for membranes from the pig CGRP1 receptor clone.

  • 1-a  The 95% confidence intervals of the Hill slope included the value of −1.0 for each ligand except for h-αCGRP8–37, [Pro14]h-αCGRP, [Ala37]h-αCGRP8–37, and adrenomedullin in the pig CGRP1 receptor clone.

  • 1-b  From Smith et al. (2001).