18328-02-4Relevant academic research and scientific papers
Synthesis, SAR studies, and evaluation of 1,4-benzoxazepine derivatives as selective 5-HT1A receptor agonists with neuroprotective effect: Discovery of Piclozotan
Kamei, Katsuhide,Maeda, Noriko,Nomura, Kayoko,Shibata, Makoto,Katsuragi-Ogino, Ryoko,Koyama, Makoto,Nakajima, Mika,Inoue, Teruyoshi,Ohno, Tomochika,Tatsuoka, Toshio
, p. 1978 - 1992 (2007/10/03)
A new series of 1,4-benzoxazepine derivatives was designed, synthesized, and evaluated for binding to 5-HT1A receptor and cerebral anti-ischemic effect. A lot of compounds exhibited nanomolar affinity for 5-HT1A receptor with good selectivity over both dopamine D 2 and α1-adrenergic receptors. Among these compounds, 3-chloro-4-[4-[4-(2-pyridinyl)-1,2,3,6-tetrahydropyridin-1-yl]butyl]- 1, 4-benzoxazepin-5(4H)-one (50: SUN N4057 (Piclozotan) as 2HCl salt) showed remarkable neuroprotective activity in a transient middle cerebral artery occlusion (t-MCAO) model.
Fused 7-membered cyclic compound and antipsychotic preparation containing the same
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, (2008/06/13)
A fused cyclic compound having the formula (I) or salts thereof: ψψ ψwherein both of A and B are carbonyl groups, or one represents methylene group and the other carbonyl group, Z represents a sulfur atom, or a nitrogen atom which may be substituted, or a methylene group, R represents an aromatic or heterocyclic group, which may be substituted, X represents a hydrogen atom, a halogen atom, a C1 - C5 lower alkyl group, a C1 - C5 lower alkoxy group, a C7 - C9 arylalkoxy group, a C1 - C5 lower acyloxy group, a C7 - C10 arylcarbonyloxy group, a hydroxy group, a nitro group or an ester group, and n is an integer of 2 to 10. The compounds have affinity for serotonin receptor.ψ
