Pirenzepine hydrochloride
- Product Name
- Pirenzepine hydrochloride
- CAS No.
- 29868-97-1
- Chemical Name
- Pirenzepine hydrochloride
- Synonyms
- Tabe;Maghen;Leblon;l-s519;Ulcosan;Renzepin;Gasteril;ls519cl2;Bisvanil;Gastricur
- CBNumber
- CB1245572
- Molecular Formula
- C19H22ClN5O2
- Formula Weight
- 387.87
- MOL File
- 29868-97-1.mol
Pirenzepine hydrochloride Property
- Melting point:
- 248-250°C
- storage temp.
- Inert atmosphere,2-8°C
- solubility
- H2O: 50 mg/mL
- form
- powder
- color
- white
- Water Solubility
- Soluble to 100 mM in water
- Sensitive
- Hygroscopic
- CAS DataBase Reference
- 29868-97-1(CAS DataBase Reference)
Safety
- WGK Germany
- 2
- RTECS
- UU7883000
- HS Code
- 2933.99.7500
- Toxicity
- dog,LD50,intravenous,62500ug/kg (62.5mg/kg),Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 19, Pg. 544, 1988.
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H317May cause an allergic skin reaction
H319Causes serious eye irritation
H402Harmful to aquatic life
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P272Contaminated work clothing should not be allowed out of the workplace.
P273Avoid release to the environment.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P333+P313IF SKIN irritation or rash occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- P7412
- Product name
- Pirenzepine dihydrochloride
- Purity
- ≥98% (TLC), powder
- Packaging
- 500mg
- Price
- $113
- Updated
- 2024/03/01
- Product number
- P7412
- Product name
- Pirenzepine dihydrochloride
- Purity
- ≥98% (TLC), powder
- Packaging
- 1g
- Price
- $200
- Updated
- 2024/03/01
- Product number
- P2457
- Product name
- Pirenzepine Dihydrochloride
- Packaging
- 200MG
- Price
- $42
- Updated
- 2024/03/01
- Product number
- P2457
- Product name
- Pirenzepine Dihydrochloride
- Packaging
- 1G
- Price
- $165
- Updated
- 2024/03/01
- Product number
- J62252
- Product name
- Pirenzepine dihydrochloride, 99%
- Packaging
- 1g
- Price
- $172
- Updated
- 2024/03/01
Pirenzepine hydrochloride Chemical Properties,Usage,Production
Description
Pirenzepine is an antagonist of M1 muscarinic acetylcholine receptors (Ki = 11.48 nM). It is selective for M1 over M2, M3, and M4 receptors (Kis = 602.56, 151.36, and 199.53 nM, respectively). Pirenzepine inhibits ascending reflex contraction of the circular smooth muscle in isolated guinea pig ileal segments induced by intraluminal balloon inflation (IC50 = 501.19 nM). It inhibits methacholine-induced increases in ileal pressure in guinea pigs (ID50 = 724.44 nmol/kg). Pirenzepine inhibits oxotremorine-induced gastric ulcer, gastric acid secretion, and salivation in rats (ED50s = 13, 37.5, and 620 μg/kg i.v., respectively). It prevents form-deprivation myopia (FDM) in a chick model of experimental myopia.
Chemical Properties
Solid
Originator
Microsules Bernabo, Microsules Bernabo
Uses
Antiulcerative;M1 antagonist
Uses
An antiulcerative. Tricyclic gastric-acid inhibitor.
Manufacturing Process
48.4 g of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzo-diazepin-6-one were refluxed in 900 ml of absolute dioxane for 15 minutes. Thereafter, over a period of 45 minutes, 28 ml of chloroacetyl chloride and 52 ml of triethylamine were simultaneously added dropwise to the mixture. The mixture was refluxed for eight hours and then vacuum-filtered after having cooled. The filtrate was evaporated in vacuum. The crystalline residue was recrystallized from acetonitrile in the presence of activated charcoal. MP: 212°-213°C (with decomposition). Yield: 85% of theory.
A mixture of 67.5 g of 11-chloroacetyl-5,11-dihydro-6H-pyrido[2,3b][1,4]benzodiazepin-6-one, 183 ml of N-methylpiperazine and 1.37 liters of absolute benzene was refluxed for 18 hours. Thereafter, the crystalline precipitate was vacuum filtered off, dissolved in aqueous 20% hydrochloric acid, the solution was evaporated in vacuum, the crystalline residue wasdissolved in 250 ml of water while heating, the solution was admixed with 150 ml of isopropanol and active charcoal, filtered, and 2.5 liters of isopropanol were added to the filtrate. After cooling, the precipitate was vacuum filtered off, yielding 70% of theory of the 5,11-dihydro-11-[(4'-methyl-1'-piperazinyl)acetyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one dihydrochloride, M.P. 257259°C (decomp.).
The free base of pirenzepine, obtained from the dihydrochloride by making an aqueous solution thereof alkaline with dilute sodium hydroxide and extracting it with chloroform, had MP: 226°-228°C after recrystallization from methanol/ether.
Therapeutic Function
Antiulcer, Antiemetic
General Description
Pirenzepine dihydrochloride is an anticholinergic agent. It is also considered as an antiulcer drug. It is used to treat myopia, gastric and duodenal ulcers. Pirenzepine dihydrochloride induces the dimerization of muscarinic M1 receptors.
Biochem/physiol Actions
Selective M1 muscarinic acetylcholine receptor antagonist.
storage
Store at RT
Pirenzepine hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
Pirenzepine hydrochloride Suppliers
- Tel
- 0512-82780333-8506
- Fax
- 0512-82782911,82780556
- wangchunhua@homesunpharm.com
- Country
- China
- ProdList
- 57
- Advantage
- 50
- Tel
- 021-50182298 021-50180596
- Fax
- +86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2210
- Advantage
- 55
- Tel
- 010-82848833 400-666-7788
- Fax
- 86-10-82849933
- jkinfo@jkchemical.com
- Country
- China
- ProdList
- 96815
- Advantage
- 76
- Tel
- 821-50328103-801 18930552037
- Fax
- 86-21-50328109
- 3bsc@sina.com
- Country
- China
- ProdList
- 15848
- Advantage
- 69
- Tel
- 001-857-928-2050 or 1-888-588-9418
- Fax
- 001-617-206-9595
- sales@chemreagents.com
- Country
- United States
- ProdList
- 10194
- Advantage
- 62
- Tel
- 021-50135380
- shchemsky@sina.com
- Country
- China
- ProdList
- 32344
- Advantage
- 50
- Tel
- 0712-0712-2580635 15527768850
- 1791901229@qq.com
- Country
- China
- ProdList
- 8849
- Advantage
- 52
- Tel
- +86 (21) 6435-5022
- Country
- China
- ProdList
- 4271
- Advantage
- 65
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Country
- China
- ProdList
- 4647
- Advantage
- 58
- Tel
- 010-56205725
- Fax
- 010-65763397
- waley188@sohu.com
- Country
- China
- ProdList
- 12338
- Advantage
- 58
View Lastest Price from Pirenzepine hydrochloride manufacturers
- Product
- Pirenzepine hydrochloride 29868-97-1
- Price
- US $1.00-1.00/KG
- Min. Order
- 1g
- Purity
- 99%
- Supply Ability
- 50tons
- Release date
- 2020-05-06
- Product
- Pirenzepine hydrochloride 29868-97-1
- Price
- US $0.00/Kg/Bag
- Min. Order
- 100g
- Purity
- 98.5%-101%; JP
- Supply Ability
- 50kg
- Release date
- 2021-09-22
- Product
- Pirenzepine hydrochloride 29868-97-1
- Price
- US $30.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 1000tons
- Release date
- 2023-08-23