Discovery and characterization of NVP-QAV680, a potent and selective CRTh2 receptor antagonist suitable for clinical testing in allergic diseases.
第一作者:
David A,Sandham
第一单位:
Novartis Institutes for Biomedical Research, Horsham Research Centre, Wimblehurst Road, Horsham, West Sussex RH12 5AB, United Kingdom. Electronic address: david.sandham@novartis.com.
作者:
关键词
13,14-dihydro-15-keto-PGD(2)2-tert-butylimino-2-diethylamino-1,3-dimethyl-perhydro-1,3,2-diazaphosphorineAllergyBALBEMPCC chemokine receptor 3CCR-3CRTh2CRTh2 receptor antagonistDK-PGD(2)ELSDFITCGLPPGD(2)SCbronchoalveolar lavagechemoattractant receptor homologous expressed on Th2 cellsevaporative light scattering detectionfluorescein isothiocyanategood laboratory practiceprostaglandin D(2)shape change
医学主题词
投药, 口服(Administration, Oral);动物(Animals);CHO细胞(CHO Cells);仓鼠亚科(Cricetinae);仓鼠属(Cricetulus);皮炎, 接触性(Dermatitis, Contact);疾病模型, 动物(Disease Models, Animal);药物评价, 临床前(Drug Evaluation, Preclinical);嗜酸细胞(Eosinophils);半衰期(Half-Life);人类(Humans);超敏反应(Hypersensitivity);吲哚嗪类(Indolizines);小鼠(Mice);小鼠, 近交BALB C(Mice, Inbred BALB C);蛋白质结合(Protein Binding);大鼠(Rats);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);受体, 免疫(Receptors, Immunologic);受体, 前列腺素(Receptors, Prostaglandin);构效关系(Structure-Activity Relationship);Th2细胞(Th2 Cells)
DOI
10.1016/j.bmc.2013.08.025
PMID
24021582
发布时间
2019-01-15
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