西那卡塞
| 中文名称 | 西那卡塞 |
|---|---|
| 中文同义词 | 西那卡塞(晶型II);甲状旁腺激素(西那卡塞);西纳卡塞;甲状旁腺激素杂质;西那卡塞盐酸;西那卡塞-D3(R-对映体);西那卡塞/甲状旁腺激素;西那卡塞碱--液体98%不高,黑色液体不卖 |
| 英文名称 | CINACALCET |
| 英文同义词 | CINACALCET;(aR)-α-Methyl-N-[3-[3-(trifluoromethyl)phenyl)propyl]-1-napthalenemethanamine;AMG 073;(aR)-a-Methyl-N-[3-[3-(trifluoromethyl)phenyl)propyl]-1-napthalenemethanamine;N-((1R)-1-(1-Naphthyl)ethyl)-3-(3-(trifluoromethyl)phenyl)propan-1-amine;364782-34-3 (Hydrochloride);Cinacalcet [inn];Hsdb 7318 |
| CAS号 | 226256-56-0 |
| 分子式 | C22H22F3N |
| 分子量 | 357.42 |
| EINECS号 | 682-701-7 |
| 相关类别 | 高钙血症;甲状旁腺功能亢进症;信号转导通路激酶抑制剂;原料药;中间体;Intermediates & Fine Chemicals;Pharmaceuticals;Mimpara, Sensipar;抗癌类;拟钙剂;对照品-杂质对照品;医药原料;细胞生物学试剂;肠胃泌尿生殖系统类;原料;Chiral Reagents |
| Mol文件 | 226256-56-0.mol |
| 结构式 |  |
西那卡塞 性质
| 沸点 | 440.9±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.154±0.06 g/cm3(Predicted) |
| 储存条件 | Keep in dark place,Sealed in dry,2-8°C |
| 溶解度 | 可溶于氯仿（少许）、甲醇（少许） |
| 形态 | 油状 |
| 酸度系数(pKa) | 9.19±0.29(Predicted) |
| 颜色 | 粘黄色 |
| InChI | InChI=1/C22H22F3N/c1-16(20-13-5-10-18-9-2-3-12-21(18)20)26-14-6-8-17-7-4-11-19(15-17)22(23,24)25/h2-5,7,9-13,15-16,26H,6,8,14H2,1H3/t16-/s3 |
| InChIKey | VDHAWDNDOKGFTD-QEIABERDNA-N |
| SMILES | [C@H](C1=CC=CC2C=CC=CC1=2)(C)NCCCC1C=CC=C(C(F)(F)F)C=1 |&1:0,r| |
| CAS 数据库 | 226256-56-0(CAS DataBase Reference) |
甲状旁腺激素的主要生理功能有促进骨质溶解，动员骨钙入血，血钙增高，骨和血中碱性磷酸酶活力增加；抑制肾小管对磷酸盐的再吸收，促进尿磷排出增多，血磷降低；PTH通过活化维生素D3，间接促进肠粘膜吸收钙、镁以及磷。PTH分泌主要受血钙浓度的调节。血Ca2+升高，PTH分泌减少，血Ca2+降低则分泌增多。此外，血磷升高可通过降低血钙而刺激PTH分泌，降钙素大量释放也可促使PTH分泌增多。
血清甲状旁腺素的测定除用于研究甲状旁腺疾病外，对鉴别高钙血症和低钙血症的原因有一定价值。主要临床意义如下：
1．辅助诊断甲状旁腺疾病。甲状旁腺机能亢进或异位PTH分泌症时，PTH升高；甲状旁腺机能减退、手术或放疗损伤甲状旁腺等，PTH降低。
2．鉴别高钙血症和低钙血症。由于甲状旁腺功能紊乱引起的血钙异常，血钙多随血清PTH的升降而升降，而其他原因所致血钙异常，PTH则无变化。Cinacalcet (AMG 073) 是一种可口服的 Ca receptor (CaR) 激动剂，用于心血管疾病研究。
Cinacalcet HCl (5 and 10 mg/kg) results in a significant reduction in parathyroid gland weight in 5/6 nephrectomy animals. In sham animals, Cinacalcet HCl has no effect on parathyroid gland cell proliferation or parathyroid weight compared with vehicle treatment. There are no differences in serum phosphorus levels in Cinacalcet HCl (10, 5, or 1 mg/kg) treated 5/6 nephrectomized animals compared with vehicle-treated 5/6 nephrectomized animals. Cinacalcet HCl treatment significantly reduces blood ionized calcium levels in sham animals. Cinacalcet (30 mg/kg/24 h) leads to a marked reduction in circulating parathyroid hormone and a modest reduction in serum Ca. Cinacalcet does not alter UCa when the GHS rats are fed the normal Ca diet but lowers UCa when they are fed the low Ca diet. Cinacalcet does not alter U supersaturation with respect to either CaOx or CaHPO4 on either diet.