4749-61-5

• 常用中文名：ST91,α2激动剂
• 常用英文名：ST 91
• CAS号：4749-61-5
• 分子式：C₁₃H₂₀ClN₃
• 分子量：253.77100
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 肾上腺素能受体
• 发布时间：2019-01-25 12:50:56
• 更新时间：2024-01-30 18:03:23
• ST91是一种α2-肾上腺素受体(α2AR)激动剂。ST91激活α2AAR和非α2AAR亚型,产生脊髓镇痛感受[1][2][3]。

名称

• 中文名: 2-(2,6-二乙基苯胺)-2-咪唑烷盐酸盐
• 英文名: N-(2,6-diethylphenyl)-4,5-dihydro-1H-imidazol-3-ium-2-amine,chloride
• 英文别名: 5,7-Dichlorokynurenic acid; ST 91; St 91-Cl; C11H16N4

物化性质

• 沸点: 325.1ºC at 760 mmHg
• 分子式: C₁₃H₂₀ClN₃
• 分子量: 253.77100
• 闪点: 150.4ºC
• 精确质量: 253.13500
• PSA: 36.42000
• LogP: 2.82190
• 储存条件: -20°C

生物活性

• 描述: ST91是一种α2-肾上腺素受体(α2AR)激动剂。ST91激活α2AAR和非α2AAR亚型,产生脊髓镇痛感受[1][2][3]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
  研究领域 >> 神经疾病
• 靶点:

  α2-adrenergic receptor

• 体外研究: 第91页降低 第16页第10页细胞的活力、增殖和线粒体功能[2]。
• 体内研究: ST91(鞘内给药)在大鼠体内产生抗伤害作用[1]。
• 参考文献:

  [1]. Graham BA, et, al. Synergistic interactions between two alpha(2)-adrenoceptor agonists, dexmedetomidine and ST-91, in two substrains of Sprague-Dawley rats. Pain. 2000 Mar;85(1-2):135-43.

  [2]. Maccari S, et, al. α-Adrenoceptor stimulation attenuates melanoma growth in mice. Br J Pharmacol. 2022 Apr;179(7):1371-1383.

  [3]. Stone LS, et, al. ST91 [2-(2,6-diethylphenylamino)-2-imidazoline hydrochloride]-mediated spinal antinociception and synergy with opioids persists in the absence of functional alpha-2A- or alpha-2C-adrenergic receptors. J Pharmacol Exp Ther. 2007 Dec;323(3):899-906.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : NJ2635000 CHEMICAL NAME : 2-Imidazoline, 2-(2,6-diethylanilino)-, hydrochloride CAS REGISTRY NUMBER : 4749-61-5 LAST UPDATED : 199309 DATA ITEMS CITED : 3 MOLECULAR FORMULA : C13-H19-N3.Cl-H MOLECULAR WEIGHT : 253.81 WISWESSER LINE NOTATION : T5M CN BUTJ BMR BZ F2 &GH HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 220 ug/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - acute pulmonary edema Lungs, Thorax, or Respiration - dyspnea REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 11,67,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 2400 ug/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - convulsions or effect on seizure threshold Skin and Appendages - hair REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,786,1975 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 2800 ug/kg/4W-I TOXIC EFFECTS : Lungs, Thorax, or Respiration - changes in lung weight Blood - pigmented or nucleated red blood cells Blood - changes in erythrocyte (RBC) count REFERENCE : JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 11,67,1986