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アッセイ
≥98% (HPLC)
形状
powder
保管条件
desiccated
色
white to beige
溶解性
H2O: 2 mg/mL, clear
保管温度
2-8°C
SMILES記法
[H][C@@]([C@]1([H])C2)(CCC1)CN2CCCOC3=CC=C(C(N)=O)C=C3.Cl
生物化学的／生理学的作用
S 38093 is an orally available compound with selective affinity toward histamine H3 receptor (human/mouse/rat H3R Ki = 0.2/1.44/8.8 μM), but not other histaminergic receptors, exhbiting both antagonist (KB = 652 nM against 300 nM (R)-α-Methylhistamine-induced GTPγS recruitment to mH3 CHO membrane; KB = 110 nM against 1 μM histamine-induced cAMP downregulation in hH3 CHO cells) and inverse agonist activity (hH3/rH3 HEK basal cAMP enhancing EC50 = 1.7/9 μM; 48% inhibition of ionomycin-induced hH3 or rH3 HEK AA reslease by 10 μM S 38093). S 38093 is reported to improve AD- and age-associated memory and cognition deficits in mice (0.1-3 mg/kg/day p.o.) and rats (0.1-10 mg/kg p.o. or i;p.), as well as display antiallodynic and antihyperalgesic efficacy in rat models of neuropathic pain in vivo.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
T Chaumette et al.
European journal of pain (London, England), 22(1), 127-141 (2017-09-07)
Histamine H3 receptors are mainly expressed on CNS neurons, particularly along the nociceptive pathways. The potential involvement of these receptors in pain processing has been suggested using H3 receptor inverse agonists. The antinociceptive effect of S 38093, a novel inverse
Aurore Sors et al.
Frontiers in pharmacology, 7, 492-492 (2017-01-10)
Donepezil, an acetylcholinesterase inhibitor, induces only moderate symptomatic effects on memory in Alzheimer's disease patients. An alternative strategy for treatment of cognitive symptoms could be to act simultaneously on both histaminergic and cholinergic pathways, to create a synergistic effect. To
Jean-Philippe Guilloux et al.
Scientific reports, 7, 42946-42946 (2017-02-22)
Strategies designed to increase adult hippocampal neurogenesis (AHN) may have therapeutic potential for reversing memory impairments. H3 receptor antagonists/inverse agonists also may be useful for treating cognitive deficits. However, it remains unclear whether these ligands have effects on AHN. The
Aurore Sors et al.
European journal of pharmacology, 803, 11-23 (2017-03-25)
Histaminergic H3 inverse agonists, by stimulating central histamine release, represent attractive drug candidates to treat cognitive disorders. The present studies aimed to describe the mechanistic profile of S 38093 a novel H3 receptors inverse agonist. S 38093 displays a moderate
Fany Panayi et al.
European journal of pharmacology, 803, 1-10 (2017-03-21)
S 38093, a novel histamine H3 receptor inverse agonist, was tested in a series of neurochemical and behavioral paradigms designed to evaluate its procognitive and arousal properties. In intracerebral microdialysis studies performed in rats, S 38093 dose-dependently increased histamine extracellular
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