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Prucalopride

Product Name
Prucalopride
CAS No.
179474-81-8
Chemical Name
Prucalopride
Synonyms
CS-219;Resolor;R093877;R 093877;Prucalopride;Unii-0A09iuw5tp;Prucalopride, >=98%;Prucalopride(R-93877);Prucalopride USP/EP/BP;Prucalopride (R-108512, R-93877)
CBNumber
CB21179613
Molecular Formula
C18H26ClN3O3
Formula Weight
367.87
MOL File
179474-81-8.mol
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Prucalopride Property

Melting point:
90.7°
Boiling point:
481.4±45.0 °C(Predicted)
Density 
1.28
storage temp. 
2-8°C
solubility 
DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml; DMSO: 10 mg/ml; Ethanol: 10 mg/ml
pka
13.65±0.20(Predicted)
form 
powder
color 
white to beige
InChI
InChI=1S/C18H26ClN3O3/c1-24-9-2-6-22-7-3-12(4-8-22)21-18(23)14-11-15(19)16(20)13-5-10-25-17(13)14/h11-12H,2-10,20H2,1H3,(H,21,23)
InChIKey
ZPMNHBXQOOVQJL-UHFFFAOYSA-N
SMILES
O1C2=C(C(NC3CCN(CCCOC)CC3)=O)C=C(Cl)C(N)=C2CC1
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Safety

RIDADR 
UN 3077 9 / PGIII
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

H400Very toxic to aquatic life

Precautionary statements

P273Avoid release to the environment.

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.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1371
Product name
Prucalopride
Purity
≥98% (HPLC)
Packaging
10MG
Price
$70.5
Updated
2023/06/20
Sigma-Aldrich
Product number
SML1371
Product name
Prucalopride
Purity
≥98% (HPLC)
Packaging
50MG
Price
$273
Updated
2023/06/20
Cayman Chemical
Product number
24192
Product name
Prucalopride
Purity
≥98%
Packaging
10mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
24192
Product name
Prucalopride
Purity
≥98%
Packaging
50mg
Price
$193
Updated
2024/03/01
Cayman Chemical
Product number
24192
Product name
Prucalopride
Purity
≥98%
Packaging
100mg
Price
$330
Updated
2024/03/01
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Prucalopride Chemical Properties,Usage,Production

Description

Prucalopride is a potent and selective agonist of the serotonin (5-HT) receptor subtype 5-HT4 (Kis = 2.5 and 8 nM for human 5-HT4A and 5-HT4B, respectively). Prucalopride is greater than 250-fold selective for 5-HT4 over a panel of 53 overexpressed receptors, including 5-HT subtypes, but does bind to human dopamine D4 and sigma-1 (σ1) receptors and mouse 5-HT3 receptors (Kis = 2.3, 3.7, and 3.8 μM, respectively). It induces contractions in guinea pig colon with an EC50 value of 33 nM, an effect that is blocked by the 5-HT4 antagonist GR113808 but not the 5-HT2A and 5-HT3 antagonists ketanserin and granisetron , respectively. It also facilitates non-cholinergic contractions induced by electrical stimulation. In fasted dogs, oral administration of prucalopride increases colonic motility by inhibiting distal colon contractions (ED50 = 0.04 mg/kg), an effect that is blocked by pretreatment with the 5-HT4 antagonist GR125487. Prucalopride (5-10 mg/kg, s.c.) increases acetylcholine and histamine levels in the rat prefrontal cortex by 2.4-fold and 3-fold, respectively, and increases the power of hippocampal theta oscillations. Formulations containing prucalopride have been used in the treatment of chronic idiopathic constipation.

Definition

ChEBI: Prucalopride is a member of benzamides.

Biochem/physiol Actions

In healthy male individuals, prucalopride decreases the display of esophageal acid and promotes gastric emptying. It is effective, safe and shows good tolerance for the treatment of men with chronic constipation.

Mechanism of action

Prucalopride is a high affinity, highly selective 5-HT4 agonist. Its action in the treatment of chronic constipation is to stimulate intestinal peristalsis by specifically interacting with 5-HT4 receptors in the digestive tract, resulting in the release of acetylcholine, which further constricts the muscular layer of the colon, and the relaxation of the circular muscular layer promoting the expulsion of luminal contents.

Side effects

Prucalopride is usually well tolerated. The most common adverse reactions include: headache, nausea, abdominal pain and diarrhoea. Other adverse reactions that may occur include: abnormal stomach or bowel sounds, flatulence, decreased appetite, dizziness, unusual tiredness or weakness, pain in the extremities or chest, difficulty or inability to speak, difficulty breathing, and suicidal thoughts. Severe allergic reactions are rare and usually manifest as hives or lumps, itching, rash, redness of the skin, swelling of the face, and tightness in the chest.

Enzyme inhibitor

This novel enterokinetic drug (FW = 367.87 g/mol; CAS 179474-81-8), also known by the tradename Resolor? and its systematic name, 4-amino-5- chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7- carboxamide, is a selective, high affinity serotonin 5-HT4 receptor agonist with that stimulates colonic mass movements, which provide the main propulsive force for defecation. It exhibits high affinity to both 5-HT4 receptor isoforms, with respective pKi values of 8.60 and 8.10 for the human 5-HT4A and 5-HT4B receptors. Based on 50 other binding assays,tonly the human D4 receptor (pKi = 5.63), the mouse 5-HT3 receptor (pKi = 5.41) and the human s1 (pKi = 5.43) shown measurable affinity, resulting in >290x selectivity for 5-HT4 receptors. Prucalopride also differs from other 5-HT4 agonists, such as tegaserod and cisapride, that interact with other receptors (5-HT1B/D and cardiac human ether-a-go-go K+ or hERG channel, respectively).

Prucalopride Preparation Products And Raw materials

Raw materials

Preparation Products

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Prucalopride Suppliers

China 198 India 5 Japan 1 The Netherlands 1 United Kingdom 2 United States 12 USA 1 Global 220
Carbosynth
Tel
--
Fax
--
Email
sales@carbosynth.com
Country
United Kingdom
ProdList
6005
Advantage
58
Sequoia Research Products Ltd.
Tel
--
Fax
--
Email
sales@seqchem.com
Country
United Kingdom
ProdList
3113
Advantage
69
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View Lastest Price from Prucalopride manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Prucalopride 179474-81-8
Price
US $0.00-0.00/Kg/Drum
Min. Order
1KG
Purity
99%min
Supply Ability
100kg
Release date
2021-10-22
Shaanxi Haibo Biotechnology Co., Ltd
Product
Prucalopride 179474-81-8
Price
US $0.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
2000ton
Release date
2023-09-04
Zhuozhou Wenxi import and Export Co., Ltd
Product
Prucalopride 179474-81-8
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10

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  • CS-219
  • Resolor
  • Unii-0A09iuw5tp
  • Prucalopride(R-93877)
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  • 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide
  • Prucalopride, >=98%
  • Prucalopride, 99%, a 5-HT Receptor agonist
  • Prucalopride USP/EP/BP
  • Prucalopride (R-108512, R-93877)
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  • PrucaloprideQ: What is Prucalopride Q: What is the CAS Number of Prucalopride Q: What is the storage condition of Prucalopride Q: What are the applications of Prucalopride
  • 4-Amino-5-chloro-N-[1-(3-methoxypropyl)-4-piperidyl]-2,3-dihydrobenzofuran-7-carboxamide
  • 179474-81-8
  • Inhibitors
  • API