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Lorediplon

Lorediplon Struktur
917393-39-6
CAS-Nr.
917393-39-6
Englisch Name:
Lorediplon
Synonyma:
Lorediplon;Thionorphine Hydrochloride;Acetamide, N-[2-fluoro-5-[3-(2-thienylcarbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methyl-;N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide;GABA Receptor,γ-Aminobutyric acid Receptor,inhibit,Inhibitor,Lorediplon,Gamma-aminobutyric acid Receptor
CBNumber:
CB83053906
Summenformel:
C20H15FN4O2S
Molgewicht:
394.42
MOL-Datei:
917393-39-6.mol

Lorediplon Eigenschaften

storage temp. 
Store at -20°C
L?slichkeit
DMF: 25 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 14 mg/ml
Aggregatzustand
A crystalline solid
Farbe
Light yellow to yellow

Sicherheit

Lorediplon Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Lorediplon is a non-benzodiazepine belonging to pyrazolopyrimidine family isunderdevelopment for the management for insomnia. Lorediplon acts by modulationof the GABAgreceptor. Its long plasma half-life has the potential of hypnotic effect. Ithas the potential for maintenance of sleep and the sleep architecture. In the phase Ipharmacodynamic study,it showed better efficacy in quality and maintenance ofsleep as compared with zolpidem. It has been shown to be well tolerated, safe with noresidual effects as compared with other sedative-hypnotic. Currently, the drug has completed Phase ll clinical trial. Results indicated strongefficacy in sleep maintenance with an acceptable safety profile. It also seems topreserve natural sleep architecture.

Verwenden

Lorediplon is GABAA receptor modulator and is used in the treatment of insomnia.

Biologische Aktivit?t

Lorediplon is a ligand for α1 subunit-containing GABAA receptors. In vivo, lorediplon inhibits spontaneous motor activity and increases duration of sleep in mice (ED50s = 0.13 and 1.2 mg/kg, respectively). It selectively inhibits spontaneous motor activity, which is driven by α1 subunit-containing GABAA receptors, over modification of muscular tone in mice, an α2 subunit-containing GABAA receptor-stimulated activity. Lorediplon (0.13 and 1.2 mg/kg) also decreases latency to slow wave sleep (SWS) and paradoxical sleep (PS) in mice. Formulations containing lorediplon have been used in the treatment of insomnia.

Lorediplon Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Lorediplon Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 67)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Dorne Chemical Technology co. LTD
+86-86-13583358881 +8618560316533
Ethan@dornechem.com China 3105 58
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32951 60
Career Henan Chemica Co
+86-0371-86658258 +8613203830695
laboratory@coreychem.com China 30241 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6391 58
TargetMol Chemicals Inc.

support@targetmol.com United States 38466 58
ShenZhen Trendseen Biological Technology Co.,Ltd.
13417589054
trendseenbio@gmail.com China 11681 58
Shanghai Acmec Biochemical Technology Co., Ltd.
+undefined18621343501
product@acmec-e.com China 33338 58
SHANGHAI KEAN TECHNOLOGY CO., LTD.
+8613817748580
cooperation@kean-chem.com China 40066 58
Amadis Chemical Company Limited
571-89925085
sales@amadischem.com China 131957 58
Haoyuan Chemexpress Co., Ltd. 021-58950125
info@chemexpress.com China 7552 61

  • Lorediplon
  • Thionorphine Hydrochloride
  • N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide
  • Acetamide, N-[2-fluoro-5-[3-(2-thienylcarbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methyl-
  • GABA Receptor,γ-Aminobutyric acid Receptor,inhibit,Inhibitor,Lorediplon,Gamma-aminobutyric acid Receptor
  • 917393-39-6
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