Table 3

In vivo effects of KMD-3213 and reference compounds after i.v. administration in the anesthetized rat model

CompoundIncrease in IUP ID50MBP ED15Uroselectivity (ED15/ID50)Relative Selectivity to Prazosin
μg/kg i.v.
KMD-32131.4128.629.7
Tamsulosin0.670.701.03.4
Prazosin4.81.40.291
Terazosin497.30.150.52
WB410111.3NDNDND
5-Methyl urapidil6.8NDNDND
Urapidil110NDNDND

Data represent the active doses inhibiting by 50% the increase in IUP response to PHE and the active doses in lowering MBP pressure by 15% of the initial value. Uroselectivity indicates the ratio between doses (ED15 value of MBP/ID50 value of increase in IUP), and relative selectivity indicates the relative uroselectivity when the uroselectivity for prazosin is taken as 1.

  • ND, not determined.