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DANTROLENE

DANTROLENE Structure
CAS No.
85008-71-5
Chemical Name:
DANTROLENE
Synonyms
DANTROLENE;DANTROLENE USP/EP/BP;Dantrolene free base;DANTROLENE FREE BASE (FOR R&D ONLY);2,4-Imidazolidinedione,1-[[[4-(4-nitrophenyl)-2-furanyl]meth...
CBNumber:
CB2158286
Molecular Formula:
C14H10N4O5
Molecular Weight:
314.25
MOL File:
85008-71-5.mol
Modify Date:
2023/4/23 13:52:06

DANTROLENE Properties

Melting point >236°C (dec.)
Density 1.57±0.1 g/cm3(Predicted)
storage temp. Hygroscopic, Refrigerator, under inert atmosphere
solubility DMSO (Slightly), Methanol (Very Slightly, Sonicated)
form Solid
pka pKa 7.5 (Uncertain)
color Yellow to Dark Yellow
Stability Hygroscopic

DANTROLENE Chemical Properties,Uses,Production

Description

Dantrolene is a drug that causes spastic muscle contraction. Unlike other muscle relaxants, it has a direct effect on the contractile mechanism by interfering in the process of calcium ion release from the sarcoplasmic reticulum. This results in a lack of coordination in the mechanism of excitation––contraction of skeletal muscle, which has a greater effect on fast muscle fibers than on slow muscle fibers.

Uses

Dantrolene is used for controlling the onset of clinical spasticity resulting from serious clinical cases such as wounds, paralysis, cerebral palsy, and disseminated sclerosis. Synonyms of this drug are dantrium and danlen.

Biological Functions

The site of action of dantrolene is believed to be at the sarcoplasmic reticulum in skeletal muscle cells. Dantrolene binds to a calcium channel protein (ryanodine receptor) on the sarcoplasmic reticulum to close the channel and inhibit the release of calcium; the alkaloid ryanodine activates the same receptor to open the channel.

Mechanism of action

Dantrolene is believed to act directly on the contractile mechanism of skeletal muscle to decrease the force of contraction in the absence of any demonstrated effects on neural pathways, on the neuromuscular junction, or on the excitable properties of the muscle fiber membranes. Cardiac muscle and smooth muscle are minimally affected by dantrolene, likely because calcium release from sarcoplasmic reticulum of these muscle cell types occurs via a mechanism that differs from skeletal muscle. The muscle relaxant effect of dantrolene on skeletal muscle, however, is not specific, and generalized muscle weakness occurs as a major adverse side effect. Like other hydantoins, dantrolene is a weak base (pKa = 7.5) that can cross the blood-brain barrier; thus, CNS depressant side effects (e.g., sedation) are common. Dantrolene sodium salt is slowly absorbed from the gastrointestinal tract. The mean half-life of the drug in adults is approximately 9 hours after a 100-mg dose. It is slowly metabolized by the liver to give the 5-hydroxy and acetamido (nitro reduction and acetylation) metabolites, as well as unchanged drug, excreted in the urine.

Clinical Use

Dantrolene is a hydantoin derivative that acts peripherally to reduce spasticity and is indicated for use in spinal cord injury, stroke, cerebral palsy, and multiple sclerosis.

DANTROLENE Preparation Products And Raw materials

Raw materials

Preparation Products

DANTROLENE Suppliers

Global( 19)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
SynZeal Research Pvt Ltd +1 226-802-2078 Gujarat, India 6522 58 Inquiry
Dideu Industries Group Limited +86-29-89586680 +86-15129568250 China 24099 58 Inquiry
Hefei TNJ Chemical Industry Co.,Ltd. +86-0551-65418684 +8618949823763 China 25363 58 Inquiry
Auschemicals Pty Ltd +61406202619 Australia 431 58 Inquiry
Hunan Furui Biopharma Technology Co., Ltd. 15902102743 China 452 55 Inquiry
CiVentiChem (919) 678-0702 ext. 227 United States 1342 55 Inquiry
3B Scientific Corporation 847.281.9822 United States 6744 47 Inquiry
2A PharmaChem USA (630) 737-0988 United States 6148 39 Inquiry
Yick-Vic Chemicals & Pharmaceuticals (HK) Ltd (852)2541 2772 China 6214 58 Inquiry
UK GREEN SCIENTIFIC CO.,LIMITED +44(0)870 432 4488 United Kingdom 6107 47 Inquiry
DANTROLENE DANTROLENE FREE BASE (FOR R&D ONLY) Dantrolene free base DANTROLENE USP/EP/BP 2,4-Imidazolidinedione,1-[[[4-(4-nitrophenyl)-2-furanyl]meth... 85008-71-5 C14H10N4O5