CLOZAPINE N-OXIDE Struktur

CLOZAPINE N-OXIDE

Bezeichnung:CLOZAPINE N-OXIDE

CAS-Nr34233-69-7

Englisch Name:CLOZAPINE N-OXIDE

CBNumberCB4759216

SummenformelC18H19ClN4O

Molgewicht342.82

MOL-Datei34233-69-7.mol

CLOZAPINE N-OXIDE physikalisch-chemischer Eigenschaften

Schmelzpunkt	190-248°C
Flammpunkt	9℃
storage temp.	-20°C Freezer, Under Inert Atmosphere
Löslichkeit	Soluble in DMSO.
Aggregatzustand	powder
pka	6.86±0.20(Predicted)
Farbe	Yellow
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
InChIKey	OGUCZBIQSYYWEF-UHFFFAOYSA-N

Sicherheit

Kennzeichnung gefährlicher	Xn,T,F
R-Sätze:	22-36/37/38-39/23/24/25-23/24/25-11
S-Sätze:	26-36-45-36/37-16-7
RIDADR	UN 2811 6.1/PG 3
WGK Germany	3
RTECS-Nr.	HP1760000
HazardClass	6.1(b)
PackingGroup	III
HS Code	29335990

Gefahreninformationscode (GHS)

CLOZAPINE N-OXIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
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:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
Beschreibung
Clozapine-N-oxide (34233-69-7) is a clozapine?metabolite1?which is pharmacologically inert2. Agonist at human muscarinic designer receptors known as DREADDs, (designer receptors exclusively activated by designer drug).2?May be used to control grafted human pluripotent stem cell-derived neurons engineered to express DREADDs.3,4??Numerous other applications.5,6
Chemische Eigenschaften
Yellow Solid
Verwenden
Clozapine N-oxide has been used:
- for the activation of human M4 muscarinic (hM4Di) in primary motor cortex
- for inducing in vivo chemogenetic manipulation and impairing locomotor activity in Th-cre transgenic mice
- in behavioral testing in mice and for stimulating (HEK293) cells
Verwenden
A 5-HT2 antagonist. A major metabolite of clozapine that can be monitored by HPLC. Possesses little or no activity towards serotonin receptors
Definition
ChEBI: Clozapine N-oxide is a dibenzodiazepine.
Allgemeine Beschreibung
Clozapine N-oxide (CNO), inactive from of clozapine drug, activates G-protein-coupled receptors (GPCRs). CNO serves as a synthetic ligand for engineered human muscarinic receptor. It elicits clozapine-like effects upon metabolic conversion. Clozapine conversion to CNO favors its passage through blood-brain barrier.
Biochem/physiol Actions
5-HT2 serotonin receptor antagonist; major metabolite of clopazine that can be monitored by HPLC.
Lager
Room temperature (desiccate)
Einzelnachweise
1) Eiermann?et al.?(1997),?The involvement of CYP1A2 and CYP3A4 in the metabolism of clozapine; Br. J. Clin. Pharmacol.,?44?439 2) Armbruster?et al.?(2007),?Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand; Proc. Natl. Acad. Sci. USA,?104?5163 3) Chen?et al.?(2016),?Chemical Control of Grafted Human PSC-Derived Neurons in a Mouse Model of Parkinson’s Disease; Cell Stem Cell,?18?817 4) Vazey and Aston-Jones (2014),?Designer receptors: therapeutic adjuncts to cell replacement therapy in Parkinson’s disease: J. Clin. Invest.,?124?2858 5) Gomez?et al.?(2017)?Chemogenetics revealed: DREADD occupancy and activation via converted clozapine; Science?357?503 6) Marcinkiewcz?et al. (2016)?Serotonin engages an anxiety and fear-promoting circuit in the extended amygdala; Nature?537?97

CLOZAPINE N-OXIDE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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