盐酸曲普利啶 | 6138-79-0

• 物质功能分类: 原料药 - 抗变态反应药 - 抗组胺药
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 盐酸曲普利啶
• 中文别名: 2-(1-(4-甲基苯基)-3-(1-吡咯烷基)-1-丙烯基)吡啶盐酸盐
• 英文名称: hydron;2-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridine;chloride;hydrate
• CAS: 6138-79-0
• 化学式: C19H25ClN2O
• 分子量: 332.9
• InChiKey: CUZMOIXUFHOLLN-UMVVUDSKSA-N

物化性质

• 熔点：
  115-120°C
• 溶解度：
  酒精：溶于1.5的溶剂
• LogP：
  4.223 (est)
• 物理描述：
  Triprolidine hydrochloride monohydrate is an odorless white crystalline powder. Bitter taste. (NTP, 1992)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.32
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  18.3
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 危险品标志：
  Xn
• 安全说明：
  S26,S36
• 危险类别码：
  R22,R36/37/38
• WGK Germany：
  3
• 海关编码：
  2933399090
• 危险品运输编号：
  NONH for all modes of transport
• 危险标志：
  GHS07
• 危险性描述：
  H302,H315,H319,H335
• 危险性防范说明：
  P261,P305 + P351 + P338

SDS

---

Section 1. Chemical Product and Company Identification
Triprolidine HCl Catalog
T2856, T1127
Common Name/
Number(s).
Trade Name
CAS# 550-70-9
Manufacturer
RTECS Not available.
SPECTRUM CHEMICAL MFG. CORP.
TSCA TSCA 8(b) inventory:
Triprolidine HCl
Commercial Name(s) Not available.
CI# Not available.
Synonym 2[1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]pyridine
IN CASE OF EMERGENCY
hydrochloride
Chemical Name Not available.
Not available. CALL [phone]
Chemical Family
Chemical Formula C19H22N2.HCl
SPECTRUM CHEMICAL MFG. CORP.

---

Section 2.Composition and Information on Ingredients
Exposure Limits
TWA (mg/m3) STEL (mg/m3) CEIL (mg/m3)
Name CAS # % by Weight
1) Triprolidine HCl 550-70-9 100
Toxicological Data Triprolidine HCl:
on Ingredients ORAL (LD50): Acute: 840 mg/kg [Rat]. 495 mg/kg [Mouse].

---

Section 3. Hazards Identification
Potential Acute Health Effects Hazardous in case of ingestion. Slightly hazardous in case of skin contact (irritant), of eye contact (irritant), of
inhalation.
Potential Chronic Health Hazardous in case of ingestion.
Effects Slightly hazardous in case of skin contact (irritant), of eye contact (irritant), of inhalation.
CARCINOGENIC EFFECTS: Not available.
MUTAGENIC EFFECTS: Not available.
TERATOGENIC EFFECTS: Not available.
DEVELOPMENTAL TOXICITY: Not available.
Triprolidine HCl

---

Section 4. First Aid Measures
Eye Contact No known effect on eye contact, rinse with water for a few minutes.
Skin Contact After contact with skin, wash immediately with plenty of water. Gently and thoroughly wash the contaminated skin
with running water and non-abrasive soap. Be particularly careful to clean folds, crevices, creases and groin.
Cover the irritated skin with an emollient. If irritation persists, seek medical attention. Wash contaminated
clothing before reusing.
Serious Skin Contact Not available.
Inhalation Allow the victim to rest in a well ventilated area. Seek immediate medical attention.
Serious Inhalation Not available.
Ingestion Do not induce vomiting. Examine the lips and mouth to ascertain whether the tissues are damaged, a possible
indication that the toxic material was ingested; the absence of such signs, however, is not conclusive. Loosen
tight clothing such as a collar, tie, belt or waistband. If the victim is not breathing, perform mouth-to-mouth
resuscitation. Seek immediate medical attention.
Serious Ingestion Not available.

---

Section 5. Fire and Explosion Data
Flammability of the Product May be combustible at high temperature.
Auto-Ignition Temperature Not available.
Flash Points Not available.
Flammable Limits Not available.
Products of Combustion These products are carbon oxides (CO, CO2), nitrogen oxides (NO, NO2...).
Fire Hazards in Presence of Not available.
Various Substances
Explosion Hazards in Presence Risks of explosion of the product in presence of mechanical impact: Not available.
of Various Substances Risks of explosion of the product in presence of static discharge: Not available.
Fire Fighting Media SMALL FIRE: Use DRY chemical powder.
and Instructions LARGE FIRE: Use water spray, fog or foam. Do not use water jet.
Special Remarks on Not available.
Fire Hazards
Special Remarks on Explosion Not available.
Hazards

---

Section 6. Accidental Release Measures
Small Spill Use appropriate tools to put the spilled solid in a convenient waste disposal container. Finish cleaning by
spreading water on the contaminated surface and dispose of according to local and regional authority
requirements.
Large Spill Use a shovel to put the material into a convenient waste disposal container. Finish cleaning by spreading water
on the contaminated surface and allow to evacuate through the sanitary system.
Triprolidine HCl

---

Section 7. Handling and Storage
Precautions Keep away from heat. Keep away from sources of ignition. Empty containers pose a fire risk, evaporate the
residue under a fume hood. Ground all equipment containing material. Do not ingest. Do not breathe dust.
Wear suitable protective clothing If ingested, seek medical advice immediately and show the container or the
label.
Storage Keep container dry. Keep in a cool place. Ground all equipment containing material. Keep container tightly
closed. Keep in a cool, well-ventilated place. Combustible materials should be stored away from extreme heat
and away from strong oxidizing agents.

---

Section 8. Exposure Controls/Personal Protection
Engineering Controls Use process enclosures, local exhaust ventilation, or other engineering controls to keep airborne levels below
recommended exposure limits. If user operations generate dust, fume or mist, use ventilation to keep exposure to
airborne contaminants below the exposure limit.
Personal Protection Safety glasses. Lab coat. Dust respirator. Be sure to use an approved/certified respirator or equivalent. Gloves.
Personal Protection in Case of Splash goggles. Full suit. Dust respirator. Boots. Gloves. A self contained breathing apparatus should be used
a Large Spill to avoid inhalation of the product. Suggested protective clothing might not be sufficient; consult a specialist
BEFORE handling this product.
Exposure Limits Not available.

---

Section 9. Physical and Chemical Properties
Physical state and appearance Solid. Odor Not available.
Taste Not available.
314.86 g/mole
Molecular Weight
Color Not available.
pH (1% soln/water) Not available.
Boiling Point Decomposes.
Melting Point 115°C (239°F)
Critical Temperature Not available.
Specific Gravity Not available.
Not applicable.
Vapor Pressure
Vapor Density Not available.
Volatility Not available.
Odor Threshold Not available.
Water/Oil Dist. Coeff. Not available.
Not available.
Ionicity (in Water)
Dispersion Properties Not available.
Not available.
Solubility

---

Section 10. Stability and Reactivity Data
The product is stable.
Stability
Instability Temperature Not available.
Not available.
Conditions of Instability
Incompatibility with various Not available.
substances
Triprolidine HCl
Corrosivity Non-corrosive in presence of glass.
Special Remarks on Not available.
Reactivity
Special Remarks on Not available.
Corrosivity
Polymerization No.

---

Section 11. Toxicological Information
Routes of Entry Ingestion.
Toxicity to Animals Acute oral toxicity (LD50): 495 mg/kg [Mouse].
Chronic Effects on Humans Not available.
Other Toxic Effects on Hazardous in case of ingestion.
Humans Slightly hazardous in case of skin contact (irritant), of inhalation.
Special Remarks on Not available.
Toxicity to Animals
Special Remarks on Not available.
Chronic Effects on Humans
Special Remarks on other Not available.
Toxic Effects on Humans

---

Section 12. Ecological Information
Ecotoxicity Not available.
BOD5 and COD Not available.
Products of Biodegradation Possibly hazardous short term degradation products are not likely. However, long term degradation products may
arise.
Toxicity of the Products The products of degradation are less toxic than the product itself.
of Biodegradation
Special Remarks on the Not available.
Products of Biodegradation

---

Section 13. Disposal Considerations
Waste Disposal

---

Section 14. Transport Information
DOT Classification Not a DOT controlled material (United States).
Identification Not applicable.
Special Provisions for Not applicable.
Transport
Triprolidine HCl
DOT (Pictograms)

---

Section 15. Other Regulatory Information and Pictograms
TSCA 8(b) inventory: Triprolidine HCl
Federal and State
Regulations
California California prop. 65: This product contains the following ingredients for which the State of California has found
to cause cancer which would require a warning under the statute: No products were found.
Proposition 65
Warnings
California prop. 65: This product contains the following ingredients for which the State of California has found
to cause birth defects which would require a warning under the statute: No products were found.
Other Regulations OSHA: Hazardous by definition of Hazard Communication Standard (29 CFR 1910.1200).
WHMIS (Canada) CLASS D-1B: Material causing immediate and serious toxic effects (TOXIC).
Other Classifications
DSCL (EEC) R22- Harmful if swallowed.
Health Hazard
HMIS (U.S.A.) 2 National Fire Protection
1 Flammability
1 Association (U.S.A.)
Fire Hazard
2 0 Reactivity
Health
Reactivity
0
Specific hazard
Personal Protection
E
WHMIS (Canada)
(Pictograms)
DSCL (Europe)
(Pictograms)
TDG (Canada)
(Pictograms)
ADR (Europe)
(Pictograms)
Protective Equipment
Gloves.
Lab coat.
Dust respirator. Be sure to use an
approved/certified respirator or
equivalent. Wear appropriate respirator
when ventilation is inadequate.
Triprolidine HCl

---

SECTION 16 - ADDITIONAL INFORMATION
N/A

制备方法与用途

生物活性

Triprolidine hydrochloride monohydrate 属于第一代抗组胺试剂，是一种具有口服活性的组胺 H1 (histamine H1) 拮抗剂，可用于过敏性鼻炎的研究。在大鼠中，Triprolidine hydrochloride monohydrate 能阻滞脊髓运动和知觉。

靶点

Target	Value
H1 receptor	()

体内研究

Triprolidine hydrochloride monohydrate（292.81-1467.20 μg/kg；鞘内注射）在大鼠中表现出剂量依赖性的脊髓运动和感觉阻滞效应。

实验细节

动物模型	雄性SD大鼠（300-350 g）
剂量	292.81 μg/kg, 488.02 μg/kg, 733.60 μg/kg, 1098.83 μg/kg, 1467.20 μg/kg
给药方式	鞘内注射
结果	剂量依赖性地引发脊髓阻滞效应

文献信息

• Use of a compound in providing refreshedness on waking and a method for the treatment of drowsiness therewith
  申请人：——

  公开号：US20030134878A1

  公开（公告）日：2003-07-17

  There is disclosed the use of triprolidine for enabling an individual to wake refreshed after sleep and the method of treating such an individual with triprolidine. The triprolidine is administered shortly before a person wishes to fall asleep, preferably orally and most commonly in the form of a tablet containing less than 5 mg, eg 0.1 mg, 1.25 mg or 2.5 mg, of the active ingredient. The triprolidine is also effective in enabling an individual to sleep more easily.

  本发明公开了使用曲普利定使个体在睡眠后清醒的方法，以及使用曲普利定治疗此类个体的方法。曲普利定在个体希望入睡前不久给予，最好是口服，通常以含有少于5毫克（例如0.1毫克、1.25毫克或2.5毫克）活性成分的片剂形式给予。曲普利定也能够有效地使个体更容易入睡。
• PROCESS FOR PREPARATION OF E-ISOMER OF 1-(4-METHYLPHENYL) - 1-(2-PYRID YL)-3-PYRROLIDINO PROP-1-ENE AND ACID ADDITION SALTS THEREOF
  申请人：Gupta Rajender Pershad

  公开号：US20110046384A1

  公开（公告）日：2011-02-24

  A process for preparation of E-isomer of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene of Formula-I, and acid addition salts thereof, said process comprising; dehydrating 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinopropan-1-ol of Formula III followed by adding a base solution to obtain a mixture of E and Z isomers of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene, and washing said mixture of E and Z isomers of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene with water to dissolve Z isomer and to obtain E-isomer of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene of Formula I, which is substantially free from Z isomer.

  一种制备公式I中1-(4-甲基苯基)-1-(2-吡啶基)-3-吡咯烷基丙烯酰胺的E异构体及其酸盐的过程，该过程包括：脱水公式III中的1-(4-甲基苯基)-1-(2-吡啶基)-3-吡咯烷基丙醇，然后加入碱溶液以获得1-(4-甲基苯基)-1-(2-吡啶基)-3-吡咯烷基丙烯酰胺的E和Z异构体混合物，并用水洗涤该混合物以溶解Z异构体并获得公式I中E异构体的制备方法，该方法中E异构体基本上不含Z异构体。
• Use of a compound in providing refreshedness on waking and a method for the treatment of grogginess therewith
  申请人：The Boots Company PLC

  公开号：US20040029927A1

  公开（公告）日：2004-02-12

  There is disclosed the use of triprolidine for enabling an individual to wake refreshed after sleep and the method of treating such an individual with triprolidine. The triprolidine is administered shortly before a person wishes to fall asleep, preferably orally and most commonly in the form of a tablet containing less than 5 mg, e.g. 0.1 mg, 1.25 mg or 2.5 mg, of the active ingredient. The triprolidine is also effective in enabling an individual to sleep more easily. There is also disclosed such uses of, and methods of treating with, consumable films comprising triprolidine, and triprolidine in combination with at least one further active pharmaceutical agent, and consumable films comprising triprolidine in combination with at least one further active pharmaceutical agent.

  本发明公开了曲普利啶用于使人在睡眠后神清气爽地醒来，以及用曲普利啶治疗这种人的方法。曲普利啶在一个人希望入睡前服用，最好是口服，最常见的形式是含活性成分少于 5 毫克的片剂，如 0.1 毫克、1.25 毫克或 2.5 毫克。曲普利啶还能有效地使人更容易入睡。此外，还公开了包含曲普利啶的可消耗薄膜、曲普利啶与至少一种其他活性药剂的组合物以及包含曲普利啶与至少一种其他活性药剂的组合物的可消耗薄膜的用途和治疗方法。
• Process for preparing ethylcellulose microcapsules
  申请人：Tanabe Seiyaku Co., Ltd.

  公开号：EP0038979B1

  公开（公告）日：1984-07-11
• USE OF A COMPOUND IN THE TREATMENT OF SLEEP DISORDERS AND THE LIKE IN PROVIDING REFRESHEDNESS ON WAKING AND A METHOD FOR THE TREATMENT OF GROGGINESS THEREWITH
  申请人：The Boots Company PLC

  公开号：EP1455786A1

  公开（公告）日：2004-09-15