endo-3-(Diphenylmethoxy)-8-methyl-8-azoniabicyclo[3.2.1]octanmethansulfonat Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R23/24/25:Giftig beim Einatmen, Verschlucken und Berührung mit der Haut.
S-Sätze Betriebsanweisung:
S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S45:Bei Unfall oder Unwohlsein sofort Arzt zuziehen (wenn möglich, dieses Etikett vorzeigen).
Chemische Eigenschaften
Benztropine mesylate is a synthetic compound containing structural features found in atropine and diphenhydramine.
Benztropine mesylate is a crystalline white powder, very soluble in water, and has a molecular weight of 403.54. COGENTIN (benztropine mesylate) is supplied as a sterile injection for intravenous and intramuscular use.
Verwenden
Benztropine mesylate is an anti-histamine and dopamine re-uptake inhibitor. It has been used to study its target identification and mode of action against ebolavirus infection. It has also been used in pharmacological animal studies to evaluate its effect on SLC6A19 (solute carrier family 6 member 19; B0AT1).
Definition
ChEBI: The methanesulfonate salt of benzatropine. An acetylcholine receptor antagonist, it is used in the treatment of Parkinson's disease, and to reduce parkinsonism and akathisia side effects of antipsychotic treatments.
Allgemeine Beschreibung
Benztropine mesylate,3α-(diphenylmethoxy)-1αH,5αH-tropane methanesulfonate(Cogentin), has anticholinergic, antihistaminic, and localanesthetic properties. Its anticholinergic effect makes it applicableas an antiparkinsonian agent. It is about as potent ananticholinergic as atropine and shares some of the side effectsof this drug, such as mydriasis and dryness of mouth.Importantly, however, it does not produce central stimulationbut instead exerts the characteristic sedative effect ofthe antihistamines.
Biologische Aktivität
Benztropine mesylate is a centrally acting muscarinic acetylcholine receptor antagonist and dopamine transporter (DAT) inhibitor (IC50 = 118 nM). Benztropine mesylate has been used to treat the symptoms of Parkinson′s disease and is currently in clincial trials for chronic back pain.
Benztropine mesylate serves as an inhibitor of breast cancer stem cells (BCSCs) in vitro and in vivo. It can help in improving the efficacy of chemotherapy in vitro. It is considered as an anti-cancer stem cell (CSC) drug, which can modify tumorigenic properties.
Clinical Use
The tremor and rigidity characteristic of parkinsonismare relieved by benztropine mesylate, and it is particularlyvaluable for those patients who cannot tolerate central excitation(e.g., aged patients). It may also have a useful effectin minimizing drooling, sialorrhea, masklike facies, oculogyriccrises, and muscular cramps.
The usual caution exercised with any anticholinergic inglaucoma and prostatic hypertrophy is observed with thisdrug.
Sicherheitsprofil
Poison by ingestion,
intravenous, subcutaneous, and
intraperitoneal routes. Human systemic
effects by ingestion: psychotropic effects.
Mutation data reported. When heated to
decomposition it emits very toxic fumes of
NOx and SOx. See also ETHERS.
endo-3-(Diphenylmethoxy)-8-methyl-8-azoniabicyclo[3.2.1]octanmethansulfonat Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
