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盐酸地匹福林

盐酸地匹福林用途

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。

盐酸地匹福林名称

[ CAS 号 ]:
64019-93-8

[ 中文名 ]:
盐酸地匹福林

[ 英文名 ]:
Dipivefrin HCl

[中文别名 ]:

[英文别名 ]:

Dipivefrin HCL
EINECS 264-609-5
AKPro
Dipivefrin hydrochloride
Dipivalyl epinephrine hydrochloride
Dipivefrine hydrochloride

盐酸地匹福林生物活性

[ 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.

盐酸地匹福林物理化学性质

[ 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.

盐酸地匹福林毒性和生态

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

盐酸地匹福林安全信息

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

盐酸地匹福林文献

Bikini dermatitis due to mercaptobenzothiazole.

Contact Dermatitis 54(6) , 345-6, (2006)

[Radiation protective effect of beta-ketoanalogs of hydroxyphenyl ethanolamines].

Radiats. Biol. Radioecol. 37(6) , 914-7, (1997)

Experiments are carried out on 3400 mice, irradiated in dose 8 Gy (LD97/30). beta-Ketoanalogs of adrenaline (adrenalone, 50-150 mumol/kg), m,p-dipivaloyladrenaline (20 mumol/kg) and phenylephrine (but...

Effects of dipivefrin and pilocarpine on pupil diameter, automated perimetry and LogMAR acuity.

Graefes Arch. Clin. Exp. Ophthalmol. 237(2) , 117-24, (1999)

A study was carried out to ascertain, in ophthalmologically normal subjects, the short-term effects of dipivefrin hydrochloride 0.1% on visual performance and make comparisons with pilocarpine.Twelve ...

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