TABLE 1

Affinity (pKB) of BIBN4096BS for antagonizing agonist-induced cAMP accumulation at WT human AMY, CT, CGRP1, and AM2 receptors Data are presented as mean ± S.E.M. The values in parentheses represent the number of individual experiments performed.




AMY1(a)

AMY3(a)

CT(a)

CGRP1

AM2
hCT <5 (4) a <5 (6)
rAmy 7.44 ± 0.2 (7) ≥5 (11)b <5 (6)
hβCGRP 7.67 ± 0.17 (12) 10.14 ± 0.44 (3) 6.29 ± 0.16 (4)
hαCGRP 7.49 ± 0.27 (10) 9.73 ± 0.24 (3)
Tyr0- hαCGRP 8.74 ± 0.33 (4)*
hAM




6.39 ± 0.25 (4)
  • * p < 0.05, Tyr0- hαCGRP versus rAmy, hβCGRP, and hαCGRP by one-way ANOVA followed by Tukey's test.

  • a BIBN4096BS pKB values were only determined for peptides for which full dose-response curves at a specific receptor could be achieved.

  • b For 8 of 11 experiments, a pKB value could not be determined, but on three occasions the pKB was equal to 5.4.