SML3509
F13714
≥95% (HPLC)
別名:
(3-Chloro-4-fluorophenyl)-(4-fluoro-4-{[(5-methyl-6-methylaminopyridin-2-ylmethyl)amino]methyl}piperidin-1-yl)methanone, 1-(3-Chloro-4-fluorobenzoyl)-4-fluoro-N-[[5-methyl-6-(methylamino)-2-pyridinyl]methyl]-4-piperidinemethanamine, F 13714, F13714
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生物化学的／生理学的作用
F13714 is an orally active, high-affinity, potent, biased serotonin receptor 5-HT1A agonist (pKi = 10.12 against 0.2 nM (±)-8-OH-DPAT binding to rat cortex tissue). F13714 inhibits 100 μM forskolin-induced cAMP accumulation in human 5-HT1A-expressing HeLa cells (pIC50 = 8.67) and displays antidepressant efficacy in vivo (ED50 = 0.05 mg/kg p.o., Emax >80%; rat forced swimming). F13714 and F15599 display differential biased agonism and, when administerd in vivo, F13714 preferentially activates raphe-located autoreceptors, while F15599 preferentially activates post-synaptic heteroreceptors.
Orally active, high-affinity, potent, biased serotonin receptor 5-HT1A agonist with a differential mode of action as F15599 in vitro and 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
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
SML3509-VAR:
SML3509-10MG:
SML3509-50MG:
SML3509-BULK:
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試験成績書（COA）
Lot/Batch Number
Adrian Newman-Tancredi et al.
Neurochemical research, 43(5), 1035-1046 (2018-03-25)
Peak-dose dyskinesia is associated with the dramatic increase in striatal dopamine levels that follows L-DOPA administration. The 'false neurotransmitter' hypothesis postulates that the latter is likely due to an aberrant processing of L-DOPA by serotonergic neurons. In keeping with this
H Iderberg et al.
Neuropharmacology, 93, 52-67 (2015-02-04)
Serotonin 5-HT1A receptor agonists reduce L-DOPA-induced dyskinesia (LID) in animal models of Parkinson's disease (PD). Here, we compared the effects of novel 5-HT1A receptor 'biased agonists' on LID in hemiparkinsonian rats. F13714 preferentially activates pre-synaptic 5-HT1A autoreceptors. F15599 preferentially activates
B Vacher et al.
Journal of medicinal chemistry, 42(9), 1648-1660 (1999-05-07)
The aim of this work was to improve the oral bioavailability of a recently discovered, novel structural class of 5-HT1A receptor agonists: aryl-{[4-(6-R-pyridin-2-ylmethyl)-amino]-methyl}-piperidin-1 -yl-metha none. Incorporation of a fluorine atom in the beta-position to the amino function in the side
Sietse F de Boer et al.
Psychopharmacology, 233(6), 937-947 (2015-12-24)
The serotonin (5-HT) deficiency hypothesis of aggression is being seriously challenged by pharmacological data showing robust anti-aggressive effects of 5-HT1A receptor agonists in dose ranges that concomitantly inhibit 5-HT neurotransmission. Hence, an adequate interpretation of the role of 5-HT activity
Peter Heusler et al.
Neuropharmacology, 49(7), 963-976 (2005-06-21)
The subject of the present study was the functional and pharmacological characterization of human 5-HT(1A) receptor regulation of ion channels in Xenopus oocytes. Activation of the heterologously expressed human 5-HT(1A) receptor induced two distinct currents in Xenopus oocytes, consisting of
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ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
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