2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione
| 中文名称 | 2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione |
|---|---|
| 中文同义词 | 化合物PA-8;PA 8,PAC1受体拮抗剂 |
| 英文名称 | 2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione |
| 英文同义词 | 2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione;2-Amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione;Pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione, 2-amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]-;2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-1H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione |
| CAS号 | 878437-15-1 |
| 分子式 | C17H18N4O4 |
| 分子量 | 342.35 |
| EINECS号 | 825-313-7 |
| 相关类别 | |
| Mol文件 | 878437-15-1.mol |
| 结构式 | ![2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione 结构式](CAS/20200119/GIF/878437-15-1.gif) |
2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione 性质
| 密度 | 1.44±0.1 g/cm3(Predicted) |
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| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 酸度系数(pKa) | 14.74±0.40(Predicted) |
| 颜色 | 白色至黄色 |
2-amino-5-[3-methoxy-4-(prop-2-en-1-yloxy)phenyl]-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidine-4,7-dione 用途与合成方法
PA-8 是一种有效的，选择性的，具有口服活性的 PACAP I 型 (PAC1) 受体拮抗剂。PA-8 抑制 PAC1受体中 PACAP 诱导的 CREB 的磷酸化，但不抑制 VPAC1 或 VPAC2 受体。PA-8 还抑制 PACAP 诱导的 cAMP 升高，IC50 为 2 nM。
In PAC1/CHO cells, PA-8 (10 pM to 10 nM; 30 minutes) dose dependently inhibits PACAP (1 nM)-induced CREB phosphorylation. In VPAC1/CHO and VPAC2/CHO cells, PACAP (1 nM) also induced CREB phosphorylation; however, PA-8 (10 pM to 10 nM) does not inhibit PACAP (1 nM)-induced CREB phosphorylation.
PA-8 (100 pmol/5 µL; intrathecal injection; once; male ddY mice) treatment inhibits PACAP-induced aversive responses and mechanical allodynia in vivo.
PA-8 (3-30 mg/kg, p.o.) treatment results in the dose-dependent attenuation of the second phase of formalin-induced nociceptive responses. PA-8 also inhibits c-fos upregulation in the ipsilateral dorsal horn of the spinal cord.
| Animal Model: | Male ddY mice (6 weeks old) injected with PACAP (100 pmol) |
| Dosage: | 100 pmol/5 µL |
| Administration: | Intrathecal injection; once |
| Result: | Inhibited PACAP-induced aversive responses and mechanical allodynia in vivo. |