| Identification | Back Directory | [Name]
L-765,314 | [CAS]
189349-50-6 | [Synonyms]
1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (S)-
1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (2S)- | [Molecular Formula]
C27H34N6O5 | [MDL Number]
MFCD05664727 | [MOL File]
189349-50-6.mol | [Molecular Weight]
522.6 |
| Chemical Properties | Back Directory | [density ]
1.269±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Sealed in dry,2-8°C | [solubility ]
DMSO:75.0(Max Conc. mg/mL);143.51(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);191.35(Max Conc. mM) | [form ]
Solid | [pka]
14.99±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively. | [Biological Activity]
L-765314 is a potent and selective antagonist of the α1b adrenergic receptor with Ki values of 5.4 nM and 2.0 nM in rat and human, respectively. | [in vitro]
L-765314 exhibits two displacement sites. The high-affinity site accounts for approximately 25% of binding (IC 50 ) 1.90 nM and represents binding to the R1b sites. The low- affinity site accounts for the residual 75% of binding (IC 50 ) 790 nM and represents binding to the R1a sites. < /div> | [in vivo]
The results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean C max of L-765314 (A322312) is 1.05 μM and the t 1 /2 is 0.5 h. It shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD 25 >3 mg/kg for each). On the basis of the inhibition of pressor responses to the R1a subtype selective agonist A-61603, it appears to be selective versus the R1a receptor up to a dose of 0.3 mg/kg. The results of hypotensive potency in rats show that both L- 765314 and terazosin tend to decrease heart rate (about 25 bpm at 1 mg/kg iv). | [target]
Ki: 5.4±0.6 nM (rat α1b receptor ), 2.0±0.66 nM (human α1b receptor), 50±8 nM (rat α1d receptor), 34±6 nM (human α1d receptor), 500± 20 nM (rat α1b receptor ), 420±62 nM (human α1b receptor). | [storage]
Store at -20°C | [References]
[1] Patane MA, et al. 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
[2] Tobias B?hmer, et al. The α1B-adrenoceptor subtype mediates adrenergic vasoconstriction in mouse retinal arterioles with damaged endothelium. Br J Pharmacol. 2014 Aug; 171(16): 3858–3867. DOI:10.1111/bph.12743 |
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Rhawn Reagent
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