878437-15-1
中文名稱(chēng)
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
英文名稱(chēng)
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
CAS
878437-15-1
分子式
C17H18N4O4
分子量
342.35
MOL 文件
878437-15-1.mol
更新日期
2024/11/04 16:13:57
878437-15-1 結(jié)構(gòu)式
基本信息
英文別名
2-Amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione2-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
Pyrido[2,3-d]pyrimidine-4,7(3H,6H)-dione, 2-amino-5,8-dihydro-5-[3-methoxy-4-(2-propen-1-yloxy)phenyl]-
物理化學(xué)性質(zhì)
密度1.44±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)14.74±0.40(Predicted)
形態(tài)Solid
顏色White to yellow
常見(jiàn)問(wèn)題列表
生物活性
PA-8 是一種有效的，選擇性的，具有口服活性的 PACAP I 型 (PAC1) 受體拮抗劑。PA-8 抑制 PAC1受體中 PACAP 誘導(dǎo)的 CREB 的磷酸化，但不抑制 VPAC1 或 VPAC2 受體。PA-8 還抑制 PACAP 誘導(dǎo)的 cAMP 升高，IC50 為 2 nM。體外研究
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.
體內(nèi)研究
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. |