64019-93-8

• 常用中文名：盐酸地匹福林
• 常用英文名：Dipivefrin HCl
• CAS号：64019-93-8
• 分子式：C₁₉H₃₀ClNO₅
• 分子量：387.89800
• 相关类别： 原料药 专科用药 眼科用药
• 发布时间：2018-09-14 11:48:01
• 更新时间：2024-01-06 07:48:23
• Dipivefrin hydrochloride (Dipivefrine hydrochloride) 是一种抗青光眼前体药物,通过角膜中的酯酶水解为其活性化合物肾上腺素。

名称

• 中文名: 盐酸地匹福林
• 英文名: dipivefrin hydrochloride
• 中文别名: 4-(1-羟基-2-(甲基氨基)乙基)-1,2-苯二醇二特戊酸酯盐酸盐
• 英文别名: Dipivefrin HCL; EINECS 264-609-5; AKPro; Dipivefrin hydrochloride; [2-(2,2-dimethylpropanoyloxy)-4-[1-hydroxy-2-(methylamino)ethyl]phenyl] 2,2-dimethylpropanoate,hydrochloride; (1)-4-(1-Hydroxy-2-(methylamino)ethyl)-1,2-phenylene dipivalate hydrochloride; Dipivalyl epinephrine hydrochloride; Dipivefrine hydrochloride

物化性质

• 沸点: 473.7ºC at 760 mmHg
• 熔点: 158-159°
• 分子式: C₁₉H₃₀ClNO₅
• 分子量: 387.89800
• 闪点: 240.3ºC
• 精确质量: 387.18100
• PSA: 84.86000
• LogP: 4.03530
• 储存条件: -20°C， 充氩
• 水溶解性: Freely soluble in water, very soluble in methanol, freely soluble in ethanol (96 per cent) and in methylene chloride.

生物活性

• 描述: Dipivefrin hydrochloride (Dipivefrine hydrochloride) 是一种抗青光眼前体药物,通过角膜中的酯酶水解为其活性化合物肾上腺素。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 体内研究: 盐酸二吡氟林(0.3-10μg/kg；i.p.；)诱导记忆增强涉及中枢β-而不是α肾上腺素能机制[3]。动物模型：雄性60日龄CFW小鼠(23-28g)[3]剂量：0.3μg/kg、1.0μg/kg、3.0μg/kg、10μg/kg；腹腔注射；训练后结果：抑制回避和Y迷宫辨别任务的保留率均显著提高,且呈剂量依赖性。
• 参考文献:

  [1]. Edgar DF, et al. Effects of dipivefrin and pilocarpine on pupil diameter, automated perimetry and LogMAR acuity. Graefes Arch Clin Exp Ophthalmol. 1999 Feb;237(2):117-24.

  [2]. Anderson JA, et al. Effects of echothiophate on enzymatic hydrolysis of dipivefrin. Arch Ophthalmol. 1984 Jun;102(6):913-6.

  [3]. Introini-Collison I, et al. Memory-enhancing effects of post-training dipivefrin and epinephrine: involvement of peripheral and central adrenergic receptors. Brain Res. 1992 Feb 14;572(1-2):81-6.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : UA2459550 CHEMICAL NAME : Propanoic acid, 2,2-dimethyl-, 4-(1-hydroxy-2-(methylamino)ethyl)-1,2-phenylene ester, hydrochloride, (+-)- CAS REGISTRY NUMBER : 64019-93-8 LAST UPDATED : 199212 DATA ITEMS CITED : 11 MOLECULAR FORMULA : C19-H29-N-O5.Cl-H MOLECULAR WEIGHT : 387.95 HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 183 mg/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,25,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 8500 ug/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,25,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 21200 ug/kg TOXIC EFFECTS : Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,25,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 224 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,25,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 32700 ug/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,25,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 35 mg/kg TOXIC EFFECTS : Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,25,1986 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 4 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,25,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 260 mg/kg/30D-I TOXIC EFFECTS : Endocrine - other changes Blood - changes in spleen Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,75,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 780 mg/kg/13W-I TOXIC EFFECTS : Cardiac - other changes Endocrine - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,75,1986 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 18900 ug/kg SEX/DURATION : male 4 week(s) pre-mating TOXIC EFFECTS : Reproductive - Paternal Effects - testes, epididymis, sperm duct REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 20,25,1986 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Subcutaneous DOSE : 13500 ug/kg SEX/DURATION : female 17-22 day(s) after conception lactating female 21 day(s) post-birth TOXIC EFFECTS : Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 31,1083,1986

安全

• 危险品运输编码: UN 2811 6.1 / PGIII