L-765314 is a potent and selective α1badrenergic receptor antagonist with Kis of 5.4±0.6 nM and 2.0±0.66 nM for rat and human α1b adrenergic receptor, respectively.
The α1 adrenergic receptors (α1a, α1b, and α1c) are abundant in the prostate, bladder neck, and urethra. The α1 adrenergic receptor antagonist has been shown to relax vascular smooth muscles that contain high concentrations of α1 receptors. L-765314 is a potent and selective α1b adrenergic receptor antagonist with Ki values of 5.4 ± 0.6 and 2.0 ± 0.66nM for rat and human α1b adrenergic receptor, respectively. It exhibited two displacement sites. The high-affinity site accounted for approximately 25% of binding (IC50 = 1.90nM), while the low-affinity site accounted for the residual 75% of binding (IC50 = 790nM). L-765314 at doses of 0.01 – 5mg/kg (i.v.) decreased the mean arterial pressure of Sprague-Dawley rats in a dose-dependent manner but was 80-fold less potent than terazosin (AD50 = 0.89mg/kg). L-765314 also decreased the heart rate of rats about 25 bpm at a dose of 1mg/kg (i.v.).[1]
作用机制
L-765314 is a potent and selective α1b adrenergic receptor antagonist.[1]
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