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Domperidone

Gastro-kinetic drugs Chemical Properties Uses Production method
Domperidone
Domperidone structure
CAS No.
57808-66-9
Chemical Name:
Domperidone
Synonyms
Evoxin;Euciton;kw-5338;Peridon;Peridys;R-33812;MOTILIUM;Nauzelin;Gastronorm;Moperidone
CBNumber:
CB8699080
Molecular Formula:
C22H24ClN5O2
Formula Weight:
425.91
MOL File:
57808-66-9.mol

Domperidone Properties

Melting point:
240-244°C
Density 
1.2904 (rough estimate)
refractive index 
1.5400 (estimate)
storage temp. 
Store at RT
solubility 
DMSO: >10 mg/mL
form 
solid
pka
pKa 7.90 (Uncertain)
color 
white
Water Solubility 
Slightly soluble in water.
Merck 
14,3418
Stability:
Stable. Incompatible with strong oxidizing agents.
InChIKey
FGXWKSZFVQUSTL-UHFFFAOYSA-N
CAS DataBase Reference
57808-66-9(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  Xn
Risk Statements  62-63
Safety Statements  26-36
WGK Germany  3
RTECS  DE2275900
Symbol(GHS):
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H360 May damage fertility or the unborn child Reproductive toxicity Category 1A, 1B Danger
H361 Suspected of damaging fertility or the unborn child Reproductive toxicity Category 2 Warning P201, P202, P281, P308+P313, P405,P501
Precautionary statements:
P201 Obtain special instructions before use.
P202 Do not handle until all safety precautions have been read and understood.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P281 Use personal protective equipment as required.
P308+P313 IF exposed or concerned: Get medical advice/attention.
P405 Store locked up.
P501 Dispose of contents/container to..…

Domperidone price More Price(13)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich D122 Domperidone powder, ≥98% (HPLC) 57808-66-9 25mg $50 2018-11-22 Buy
Sigma-Aldrich D122 Domperidone powder, ≥98% (HPLC) 57808-66-9 100mg $153 2018-11-22 Buy
TCI Chemical D4125 Domperidone >98.0%(HPLC)(T) 57808-66-9 1g $502 2018-11-22 Buy
TCI Chemical D4125 Domperidone >98.0%(HPLC)(T) 57808-66-9 200mg $144 2018-11-22 Buy
Alfa Aesar J63681 Domperidone 57808-66-9 100mg $98.2 2018-11-13 Buy

Domperidone Chemical Properties,Uses,Production

Gastro-kinetic drugs

Domperidone is a commonly used antiemetic and gastro-kinetic drug with its appearance being white to light yellow powder and bitter taste. It is almost insoluble in water, slightly soluble in ethanol, easily soluble in lactic acid as well as soluble in citrate. This product is a kind of peripheral dopamine receptor antagonists with strong action. Domperidone can block the DA1 and DA2 receptor next to the synapses, antagonizing the inhibitory effect of dopamine on the postsynaptic cholinergic neurons of myenteric plexus and causing the stomach contractions. It can promote the motility and tension of digestive tract motility to return to normal function, promoting the emptying of stomach, increasing the motility of gastric antral and duodenum, coordinating the contraction of the pylorus as well as enhancing the esophageal peristalsis and the tension of the lower esophageal sphincter. Because it has a poor penetration capability through the blood-brain barrier with almost no antagonism on the dopamine receptor, you can rule out the side effects of spirit and the central nervous system side. It has rapid absorption after oral administration with the plasma concentration reaching peak after 15~30 min. In addition to the central nervous system, it is also widely distributed in other parts of the body. Owing to the presence of "first pass" hepatic metabolism and intestinal metabolism, it has a low oral bioavailability. The half-life of this product is 7h with 30% excreted through the urine at 24 h after the oral administration and about 60% excreted through faeces within 4 days.
Indications
1, Digestion dysfunction symptoms caused by delayed gastric emptying, gastroesophageal reflux, chronic gastritis and esophagitis including nausea, vomiting, belching, abdominal fullness, abdominal pain, regurgitation caused burning sensation of mouth and stomach.
2, Parkinson's disease and nausea and vomiting caused by various kinds of reasons such as functional, infection, dietary, radiotherapy or drug therapy and dopamine receptor agonists (such as levodopa, bromocriptine) therapy.
3, it is suitable for treating migraine, dysmenorrhea, traumatic brain injury and intracranial lesions, radiation therapy and the nausea and vomiting caused by levodopa, nonsteroidal anti-inflammatory drug.
4, it is effective in treating the nausea and vomiting caused by various organic or functional gastrointestinal disorders in elderly people.
5, Domperidone is not effective in treating the vomiting caused by surgery or anesthesia and chemotherapy.
The above information is edited by the Chemicalbook of Dai Xiongfeng.

Chemical Properties

From dimethylformamide-water to obtain its white crystalline powder; the melting points is 242.5 ℃

Uses

It is a kind of potent peripheral dopamine receptor antagonist with anti-vomiting and gastro-kinetic effects. It can affect the gastrointestinal motility to make the motility and tension of upper gastrointestinal tract return to normal and promote gastric emptying, enhancing the antral and duodenal motility, and coordinating the pyloric contraction. It can be used for the treatment of dyspepsia, and the nausea and vomiting induced by functional, organic, infection, dietary, radiation therapy or drug therapy. Because it almost has no inhibitory effect on dopamine receptor, there are no psychiatric and neurological side effects. And it can be used for treating the nausea caused by treating the Parkinson’s disease through taking dopamine agonists.
It can be used as anticholinergic antispasmodics.
Domperidone is a kind of phenyl imidazole compounds with a strong role in promoting gastric motility and antiemetic effect. It can strengthen the tension of the sphincter of the lower part of the esophagus, preventing the stomach-esophageal reflux, enhancing the gastric motility, promoting the gastric emptying, coordinating the stomach and duodenal motility, suppressing nausea, vomiting, and effectively preventing the bile reflux without affecting the secretion of gastric juice. This product is a kind of peripheral dopamine receptor antagonists which can directly block the gastrointestinal dopamine receptors and exhibit the stimulating effect of gastric motility. It can enhance the esophageal peristalsis and the tension of esophageal sphincter. Because of its poor penetration through the blood brain barrier, it has almost no antagonism against the dopamine receptor of the brain, and therefore can excluding the side effects of the spirit and the central nervous system.

Production method

2-nitro-1, 4-dichlorobenzene is reacted with 4-amino-cyclohexanecarboxylic acid ethyl ester and is further subject to hydrogenation reduction, urea cyclization, hydrolysis, to give 5-chloro-1-(piperidin-4-yl)-1,3-dihydro-benzimidazol-2-ketone.
Hydroxyl propylamine can have nucleophilic substitution of the chlorine of 2-nitro-chlorobenzene and then be subject to hydrogenation to reduce the nitro group to amino group; then have cyclization with potassium chloride and further chlorination to give 1-(3-chloropropyl)-2,3-dihydro-1H-benzimidazol-2-ketone.
The two benzimidazole derivative obtained above are processed as follows and can give domperidone. 2.3 parts of 1-(3-chloropropyl)-2,3-dihydro-1H-benzimidazol-2-ketone, 2.5 parts of 5--chloro-I-(piperidin-4-yl)-1,3-2H-dihydro-benzimidazol-2-one, 3.2 parts of sodium carbonate, 0.1 parts of potassium iodide and 80 parts of 4-methyl-2-pentanone were stirred and reflux for 24h. After being cooled to room temperature, add water, filter off the insolubles and purify it by silica gel column chromatography with the eluting solution being chloroform and 10% methanol mixture. The effluent containing the product were collected and concentrated. The residue was crystallized using 4-methyl-2-pentanone. After filtration, apply re-crystallization with the mixture of dimethylformamide and water to obtain 1.3 parts of domperidone with the yield being 30% and the mp being 242.5 ℃.

Chemical Properties

White or almost white powder.

Uses

COX2 inhibitor, antiinflammatory, antiarthritic

Uses

A novel peripheral dopamine receptor antagonist that does not cross the blood-brain barrier; anti-emetic. Domperidone(Motilium) is a dopamine blocker and an antidopaminergic reagent.

Uses

For management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.

Definition

ChEBI: 1-[3-(Piperidin-1-yl)propyl]-1,3-dihydro-2H-benzimidazol-2-one in which the 4-position of the piperidine ring is substituted by a 5-chloro-1,3-dihydro-2H-benzimidazol-2-on-1-yl group. A dopamine antagonist, it is used s an antiemetic for the short-term treatment of nausea and vomiting, and to control gastrointestinal effects of dopaminergic drugs given in the management of parkinsonism. The free base is used in oral suspensions, while the maleate salt is used in tablet reparations.

brand name

Motilium (Janssen);Evixub;Kw 5338;Moperidona;Neta662;R 33812;Tametil;Touristic.

World Health Organization (WHO)

Domperidone, a peripheral dopaminergic antagonist, was introduced in 1979 for the symptomatic relief of acute nausea and vomiting. The major manufacturer became aware that the injectable formulation was being used in some countries in much higher doses than those recommended to combat nausea and vomiting in cancer patients treated with cytostatic agents. Such use - which was not in conformity with the approved indications - was associated with cardiotoxicity, which in some cases was fatal, and the manufacturer decided to withdraw the injectable dosage form from the market worldwide in January 1985. Suppositories, tablets and a suspension remain available and the manufacturer continues to supply the injection for the treatment of a named patient at the written request of a doctor on the understanding that the appropriate dosage recommendations will be followed.

Biological Activity

Peripheral dopamine D 2 -like receptor antagonist that does not readily cross the blood brain barrier. Displays gastroprokinetic and antiemetic properties; increases the frequency and duration of antral and duodenal contractions and protects from apomorphine-induced emesis (ED 50 values are 0.003 and 0.03 mg/kg for i.v. and oral administration respectively).

Domperidone Preparation Products And Raw materials

Raw materials

Preparation Products


Domperidone Suppliers

Global( 247)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Hebei Guanlang Biotechnology Co., Ltd.
+86-0311-66562153 whatsapp +8615203118427
+86-0311-66562153 sales@crovellbio.com CHINA 416 50
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19954 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3217 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22043 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32651 55
Rixing Chemical CO.,LTD
13237129059
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PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2548 55
Hubei XinRunde Chemical Co., Ltd.
+8615102730682; +8618874586545
02783214688 bruce@xrdchem.cn CHINA 552 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 16534 60

View Lastest Price from Domperidone manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-04-17 Domperidone
57808-66-9
US $10.00 / KG 1KG 99% 10 mt Hebei Guanlang Biotechnology Co., Ltd.

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