Acamprosate calcium Struktur

Calcium(2+)-3-(acetylamino)propansulfonat

Bezeichnung:Calcium(2+)-3-(acetylamino)propansulfonat

CAS-Nr77337-73-6

Englisch Name:Acamprosate calcium

CBNumberCB4310705

SummenformelC10H20CaN2O8S2

Molgewicht400.48

MOL-Datei77337-73-6.mol

Synonyma

Calcium(2+)-3-(acetylamino)propansulfonat

Calcium(2+)-3-(acetylamino)propansulfonat physikalisch-chemischer Eigenschaften

Schmelzpunkt	>300°C
storage temp.	2-8°C
Löslichkeit	H2O: >5mg/mL
Aggregatzustand	powder
Farbe	White to Off-White
Wasserlöslichkeit	Soluble in water (100mM)
Merck	14,17
CAS Datenbank	77337-73-6(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-36/37/39-36
WGK Germany	3
RTECS-Nr.	TZ6357000
HS Code	29241990
Toxizität	LD50 i.p. in male mice: 1.87 g/kg (Durlach, 1982)

Gefahreninformationscode (GHS)

Acamprosate calcium Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Acamprosate is an acetylated derivative of the GABA analog homotaurine (tramiprosate; ). Despite its structural similarity to GABA, acamprosate does not act at GABA_A receptors but does decrease paired-pulse inhibition of GABA_A inhibitory post-synaptic currents (IPSCs) at short inter-stimulus intervals when used at a concentration of 300 μM, indicating that it may inhibit GABA_B autoreceptor-mediated inhibition of GABA release. It is an NMDA receptor modulator with antagonist or agonist effects depending on brain region, receptor subunit composition, and other factors. Acamprosate (0.26 and 0.52 mmol/kg per day, i.p.) reduces voluntary intake of ethanol in rats, an effect that can be blocked by the GABA antagonist bicuculline . Formulations containing acamprosate have been used for the maintenance of alcohol abstinence.
Chemische Eigenschaften
Acamprosate calcium is White Crystalline Solid
Originator
Campral,Merck
Verwenden
glucocortcoid, antiinflammatory
Verwenden
Acamprosate calcium is a synthetic amino acid and a neurotransmitter analogue that is used as an alcohol deterrent in management of alcohol dependence and abuse. Acamprosate calcium was approved for use in the therapy of alcohol dependence and abuse in the United States in 2004.
Verwenden
Of interest for the treatment of alcoholism and other neurochemical disorders.
Verwenden
Of interest for the treatment of alcoholism. Store at -20°C
Definition
ChEBI: Acamprosate calcium is an organic calcium salt. It contains an acamprosate(1-).
Manufacturing Process
In a 4 liter flask provided with stirring means, a bromine funnel and a thermometer, 17.5% sodium hydroxide solution and aminopropanesulfonic acid (homotaurine) are added.
After complete dissolution, at a temperature of between 25°-40°C, acetic anhydride are added so as not to exceed a temperature of between 30°-40°C. The mixture is then maintained at this temperature by heating for at least 1 h.
The solution is then concentrated in vacuum, the residue is redissolved in 2.5 L of distilled water and the mixture is concentrated again. The residue is then dissolved in 1.6 L of distilled water, filtered, then concentrated almost completely. Drying is terminated in an oven in vacuum. A colorless crystalline powder of 3-acetylaminopropanesulfonate of sodium (sodium Nacetylhomotaurinate) is obtained.
The 3-acetylaminopropanesulfonic acid may be produced by treatment of 3- acetylaminopropanesulfonate of sodium with hydrochloric acid.
In practice it is usually used as calcium salt.
Trademarks
Campral (Forest).
Therapeutic Function
Psychotropic
Biologische Aktivität
GABA receptor agonist and modulator of glutamatergic systems. Reduces alcohol consumption in animal models of alcohol addiction.
Biochem/physiol Actions
Acamprosate calcium is a GABA γ-aminobutyric acid agonist.
Clinical Use
Maintenance of abstinence in alcohol dependence
Stoffwechsel
Acamprosate is excreted in the urine and is not metabolised significantly.
Lager
Room temperature (desiccate)
Einzelnachweise
1. wilde m i, wagstaff a j. acamprosate. drugs, 1997, 53(6): 1038-1053.

Acamprosate calcium Upstream-Materialien And Downstream Produkte

Calcium(2+)-3-(acetylamino)propansulfonat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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