Description
YM 218 is a novel, potent, nonpeptide vasopressin V1A receptor-selective antagonist.
Uses
YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a Ki value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with Ki values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease[1].
IC 50
Rat liver V1a Receptor: 0.5 nM (Ki); Rat pituitary V1b receptor: 1510 nM (Ki); Rat kidney V2 receptor: 72.2 nM (Ki)
References
[1] Tsukada J, et al. Pharmacologic properties of YM218, a novel, potent, nonpeptide vasopressin V1A receptor-selective antagonist[J]. Vascular pharmacology, 2005, 42(2): 47-55. DOI:
10.1016/j.vph.2005.01.002
