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ST91,α2激动剂

ST91,α2激动剂用途

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]。

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ST91,α2激动剂名称

[ CAS 号 ]:
4749-61-5

[ 中文名 ]:
2-(2,6-二乙基苯胺)-2-咪唑烷盐酸盐

[ 英文名 ]:
ST 91

[英文别名 ]:

5,7-Dichlorokynurenic acid
ST 91
St 91-Cl
C11H16N4

ST91,α2激动剂生物活性

[ 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.

ST91,α2激动剂物理化学性质

[ 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

ST91,α2激动剂毒性和生态

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