Tyr-α-CGRP (human)

Description

Tyr-α-CGRP is an N-terminal extended tyrosinated analogue of α-calcitonin gene-related peptide (α-CGRP; ).¹ It binds to amylin receptors AMY₁ and AMY₃ in COS-7 cells expressing the human receptors (IC₅₀s = 141 and 1.86 nM, respectively).² Tyr-α-CGRP also binds to and stimulates cAMP accumulation in rat L6 myocytes (IC₅₀ = 4 nM; EC₅₀ = 12 nM).¹ It also binds to rat brain and spleen membrane preparations (IC₅₀s = 0.2 and 0.5 nM, respectively), induces positive chronotropic and inotropic effects in isolated right and left guinea pig atria (EC₅₀s = 282 and 74 nM, respectively), and inhibits the twitch response in rat vas deferens (EC₅₀ = 1.9 nM).³

References

1. Poyner, D.R., Andrew, D.P., Brown, D., et al. Pharmacological characterization of a receptor for calcitonin gene-related peptide on rat, L6 myocytes Br. J. Pharmacol. 105(2),441-447(1992).
2. Hay, D.L., Christopoulos, G., Christopoulos, A., et al. Pharmacological discrimination of calcitonin receptor: Receptor activity-modifying protein complexes Mol. Pharmacol. 67(5),1655-1665(2005).
3. Dennis, T., Fournier, A., St. Pierre, S., et al. Structure-activity profile of calcitonin gene-related peptide in peripheral and brain tissues. Evidence for receptor multiplicity J. Pharmacol. Exp. Ther. 251(2),718-725(1989).