Table 2

Comparative functional antagonistic potencies of fiduxosin and standard α1-adrenoceptor antagonists at α1-adrenoceptors in isolated smooth muscle in vitro

CompoundTissue and Receptor Subtype
Rat Vas Deferens α1ACanine Prostate α1ARabbit Urethra α1LRat Spleen α1BRat Aorta α1D
Fiduxosin2-a
 pA2(±S.E.M.)9.62 (±0.44)8.51 (±0.23)7.58 (±0.19)7.08 (±0.07)8.92 (±0.86)
 Slope (±S.E.M.)0.83 (±0.07)0.80 (±0.05)0.92 (±0.13)0.90 (±0.05)0.78 (±0.08)
 [n][18][20][15][14][20]
Terazosin2-b
 pA2(±S.E.M.)8.04 (±0.45)7.44 (±0.24)6.77 (±0.30)8.60 (±0.46)8.65 (±0.29)
 Slope (±S.E.M.)0.83 (±0.17)0.79 (±0.09)0.99 (±0.07)0.94 (±0.14)0.99 (±0.13)
 [n][12][35][13][12][9]
Tamsulosin2-c
 pA2(±S.E.M.)9.47 (±0.21)9.54 (±0.17)8.86 (±0.22)9.69 (±0.44)10.6 (±0.43)
 Slope (±S.E.M.)1.06 (±0.14)1.12 (±0.08)1.41 (±0.26)0.84 (±0.15)0.94 (±0.11)
 [n][22][20][8][16][10]

Isolated smooth muscle strips or rings were incubated in tissue baths in the presence or absence of various concentrations of fiduxosin and standard α1-adrenoceptor antagonists, as described underExperimental Procedures.

  • 2-a  One-way analysis of variance indicated the following potency order of statistically significant differences for fiduxosin: rat vas deferens > rat aorta ≅ canine prostate > rabbit urethra > rat spleen α1-adrenoceptor antagonism.

  • 2-b  One-way analysis of variance indicated the following potency order of statistically significant differences for terazosin: rat aorta ≅ rat spleen > rat vas deferens > canine prostate > rabbit urethra α1-adrenoceptor blockade.

  • 2-c  One-way analysis of variance indicated the following potency order of statistically significant differences for tamsulosin: rat aorta > canine prostate > rabbit urethra, but canine prostate ≅ rat vas deferens ≅ rat spleen and rat vas deferens ≅ rat spleen ≅ rabbit urethra α1-adrenoceptor antagonism.