L-765314

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Chemical Structure| 189349-50-6 同义名 : -
CAS号 : 189349-50-6
货号 : A484697
分子式 : C27H34N6O5
纯度 : 99%+
分子量 : 522.6
MDL号 : MFCD05664727
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.57mL

1.91mL

0.96mL

19.14mL

3.83mL

1.91mL
参考文献

[1]Patane MA, Scott AL, Broten TP, Chang RS, Ransom RW, DiSalvo J, Forray C, Bock MG. 4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist. J Med Chem. 1998 Apr 9;41(8):1205-8. doi: 10.1021/jm980053f