로레디플론

로레디플론
로레디플론 구조식 이미지
카스 번호:
917393-39-6
한글명:
로레디플론
동의어(한글):
로레디플론
상품명:
Lorediplon
동의어(영문):
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
분자식:
C20H15FN4O2S
포뮬러 무게:
394.42
MOL 파일:
917393-39-6.mol

로레디플론 속성

저장 조건
Store at -20°C
용해도
DMF: 25 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 14 mg/ml
물리적 상태
결정성 고체
색상
Light yellow to yellow

안전

로레디플론 C화학적 특성, 용도, 생산

개요

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.

용도

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

생물학적 활성

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.

로레디플론 준비 용품 및 원자재

원자재

준비 용품


로레디플론 공급 업체

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Haoyuan Chemexpress Co., Ltd. 021-58950125
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MedChemexpress LLC 021-58955995
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Nanjing Chalf-Pharm Technology Co., Ltd. 025-57018978 18251899859
sales@chalf-pharm.com China 5870 50

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