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. 2008 Aug 11;155(6):906–912. doi: 10.1038/bjp.2008.318

Table 1.

Binding affinities for various α1-adrenoceptor antagonists estimated at [3H]-silodosin and [3H]-prazosin-binding sites in rabbit prostate

Drug [3H]-silodosin
[3H]-prazosin
  Segments
Membranes Membranes
  pKi high (% high) pKi low pKi pKi
Prazosin 8.8±0.1 7.1±0.2 9.9±0.2 9.8±0.2
  (42±4%)      
Bunazosin 9.1±0.1 7.8±0.2    
  (34±7%)      
Silodosin 9.5±0.1   9.8±0.1 10.1±0.1
Tamsulosin 9.7±0.1      
RS-17053 9.6±0.6 6.8±0.3    
  (27±8%)      
5-Methylurapidil 9.6±0.2 7.6±0.1 9.5±0.3 9.8±0.2
  (45±5%)      
         
         
BMY-7378   5.2±0.2    

Values from four or five experiments.

pKi high and pKi low: negative logarithm of equilibrium dissociation constants at high- and low-affinity sites for tested drugs.

% high: proportion of high-affinity sites.