咪洛克生

化合物

咪洛克生INN:imiloxan)是一種用於科學研究的藥物。它作為α2B英語Alpha-2B adrenergic receptor腎上腺素受體的選擇性拮抗劑[1]可用於區分不同α2腎上腺素亞型的作用。[2][3]

咪洛克生
臨床資料
ATC碼
  • 未分配
識別資訊
  • (RS)-2-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-1-ethylimidazole
CAS號81167-16-0  checkY
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
化學資訊
化學式C14H16N2O2
摩爾質量244.29 g·mol−1
3D模型(JSmol英語JSmol
  • CCN1C=CN=C1CC2COC3=CC=CC=C3O2
  • InChI=1S/C14H16N2O2/c1-2-16-8-7-15-14(16)9-11-10-17-12-5-3-4-6-13(12)18-11/h3-8,11H,2,9-10H2,1H3 ☒N
  • Key:UXABARREKCJULM-UHFFFAOYSA-N ☒N

合成

 
咪洛克生合成:[4]

咪洛克生的咪唑部分是通過亞胺酸酯與氨基乙醛的二乙縮醛反應製備的。咪唑與碘乙烷N-烷基化可得到咪洛克生。

參考資料

  1. ^ Michel AD, Loury DN, Whiting RL. Assessment of imiloxan as a selective alpha 2B-adrenoceptor antagonist. British Journal of Pharmacology. March 1990, 99 (3): 560–4. PMC 1917331 . PMID 1970500. doi:10.1111/j.1476-5381.1990.tb12968.x. 
  2. ^ Cobos-Puc LE, Villalón CM, Sánchez-López A, Lozano-Cuenca J, Pertz HH, Görnemann T, Centurión D. Pharmacological evidence that alpha2A- and alpha2C-adrenoceptors mediate the inhibition of cardioaccelerator sympathetic outflow in pithed rats. European Journal of Pharmacology. January 2007, 554 (2–3): 205–11. PMID 17109851. doi:10.1016/j.ejphar.2006.09.068. 
  3. ^ Romero TR, de Castro Perez A, de Francischi JN, Gama Duarte ID. Probable involvement of alpha(2C)-adrenoceptor subtype and endogenous opioid peptides in the peripheral antinociceptive effect induced by xylazine. European Journal of Pharmacology. April 2009, 608 (1–3): 23–7. PMID 19236861. doi:10.1016/j.ejphar.2009.02.019 . 
  4. ^ Caroon JM, Clark RD, Kluge AF, Olah R, Repke DB, Unger SH, et al. Structure-activity relationships for 2-substituted imidazoles as alpha 2-adrenoceptor antagonists. Journal of Medicinal Chemistry. June 1982, 25 (6): 666–70. PMID 6124635. doi:10.1021/jm00348a012. 

外部連結