ATC 0175 Struktur

ATC 0175

Bezeichnung:ATC 0175

CAS-Nr510733-97-8

Englisch Name:ATC 0175

CBNumberCB5972935

SummenformelC23H25F2N5O.ClH

Molgewicht461.941

MOL-Datei510733-97-8.mol

ATC 0175 physikalisch-chemischer Eigenschaften

storage temp.	2-8°C
Löslichkeit	DMSO: soluble5mg/mL
Aggregatzustand	solid
Farbe	White to light yellow

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26
WGK Germany	3

Gefahreninformationscode (GHS)

ATC 0175 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.
Verwenden
ATC0175 is a MCHR1, SR-1A and SR-2B inhibitor.
Biologische Aktivität
Potent, selective and orally active melanin-concentrating hormone receptor 1 (MCH 1 ) antagonist (IC 50 values are 13.5 and > 10000 nM for MCH1 and MCH2 receptors respectively). Exhibits anxiolytic and antidepressant activity in rodents. Also displays affinity for 5-HT 2B and 5-HT 1A receptors (IC 50 values are 9.66 and 16.9 nM respectively).
in vitro
assays showed that this compound is a potent antagonist with a high affinity for mch1r. the receptor binding and the functional assay (mch-induced increase in [ca2+]) indicated that atc0175 is a noncompetitive antagonist at mch1rs 1.
in vivo
atc0175 displayed anxiolytic effects in numerous animal models of anxiety including the social interaction test, elevated plus-maze test, maternal separation-induced vocalization and stress-induced hyperthermia. in addition, atc0175 treatment also exhibited antidepressant effects in the forced swimming test 2.
Einzelnachweise
1. semple g, tran ta, kramer b, et al. pyrimidine-based antagonists of h-mch-r1 derived from atc0175: in vitro profiling and in vivo evaluation. bioorganic & medicinal chemistry letters. 2009;19(21):6166-6171.2. chaki s, yamaguchi j, yamada h, et al. atc0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety. cns drug reviews. 2005;11(4):341-352.

ATC 0175 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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