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.