TABLE 1

In Vitro Profiles of TASP699, TASP0434299, and Candidate Metabolites of TASP699

3H-AVP binding
Compound/peptideHuman V1B receptorHuman V1A receptorHuman V2 receptor3H-oxytocin binding, human oxytocin receptor[Ca2+]i assay, human V1B receptor
TASP6990.165>10,000>10,000>10,0000.381
Metabolite candidate 1>1,000
Metabolite candidate 21.87
TASP04342990.526>10,000>10,000>10,0000.639
AVP0.7760.4401.24
Oxytocin0.731
  • — = not determined.

  • IC50 values (nM) are expressed as geometric means (n = 3–6).