3-(1′-Cyclobutylspiro[4H-1,3-benzodioxine-2,4′-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist
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- 作者：Robert L. Hudkins ; robert.hudkins@tevapharm.com" class="auth_mail" title="E-mail the corresponding author ; John A. Gruner1 ; Rita Raddatz ; Joanne R. Mathiasen ; Lisa D. Aimone ; Michael J. Marino2 ; Edward R. Bacon3 ; Michael Williams3 ; Mark A. Ator
- 关键词：Histamine H3 receptor ; H3R inverse agonist ; CEP-32215 ; Sleep wake activity
- 刊名：Neuropharmacology
- 出版年：2016
- 出版时间：July 2016
- 年：2016
- 卷：106
- 期：Complete
- 页码：37-45
- 全文大小：713 K
文摘
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CEP-32215 is a new, potent and selective H3R inverse agonist.
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Human H3R Ki = 2.0 with potent functional and inverse agonist activity (EC50 = 0.6 nM).
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Functional antagonism in the rat dipsogenia model (ED50 = 0.92 mg/kg p.o.).
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Active in the rat EEG model from 3 to 30 mg/kg p.o. with no undesirable events.