中文名 | L-765314 |
英文名 | L-765,314 |
别名 | 化合物L-765314 (S)-4-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-2-(叔丁基氨基甲酰基)哌嗪-1-甲酸苄酯 (2S)-4-(4-氨基-6,7-二甲氧基-2-喹唑啉基)-2-[[(1,1-二甲基乙基)氨基]羰基]-1-哌嗪甲酸苯甲酯 |
英文别名 | L-765314 L-765,314 Benzyl (S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate 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)- |
CAS | 189349-50-6 |
化学式 | C27H34N6O5 |
分子量 | 522.6 |
存储条件 | 2-8°C(protect from light) |
体外研究 | 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. |
体内研究 | 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. L-765314 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, L-765314 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). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.914 ml | 9.568 ml | 19.135 ml |
5 mM | 0.383 ml | 1.914 ml | 3.827 ml |
10 mM | 0.191 ml | 0.957 ml | 1.914 ml |
5 mM | 0.038 ml | 0.191 ml | 0.383 ml |
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