P118
法洛芬
solid
别名:
3-氨基-2-（4-氯苯基）丙烷膦酸
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关于此项目
经验公式（希尔记法）:
C9H13ClNO3P
化学文摘社编号:
分子量:
249.63
NACRES:
NA.32
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI key
VSGNGLJPOGUDON-UHFFFAOYSA-N
SMILES string
NCC(CP(O)(O)=O)c1ccc(Cl)cc1
InChI
1S/C9H13ClNO3P/c10-9-3-1-7(2-4-9)8(5-11)6-15(12,13)14/h1-4,8H,5-6,11H2,(H2,12,13,14)
form
solid
impurities
≥97% (NMR)
color
white
solubility
0.1 M HCl: 13.3 mg/mL, methanol: 19.3 mg/mL, DMSO: insoluble
Quality Level
Gene Information
human ... GABBR1(2550), GABBR2(9568)
General description
法克罗芬是巴氯芬的膦酸衍生物。
Application
法克罗芬已用于阻断 GABAB 受体。
Biochem/physiol Actions
法克罗芬在鉴定与 GABA 和（−）巴氯芬相互作用的中枢和外周荷包牡丹碱不敏感受体的生理重要性的研究中起着重要作用。法克罗芬可作为 GABAB 受体拮抗剂。法克罗芬具有可逆性阻断已记录在猫和大鼠背外侧膝状核的投射细胞中和大鼠海马 CA1 锥体神经元中的晚的、荷包牡丹碱耐药性、K+ 依赖性抑制性突触后电位（IPSP）的能力。
signalword
Warning
hcodes
Hazard Classifications
Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
target_organs
Respiratory system
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
dust mask type N95 (US), Eyeshields, Gloves
Phaclofen: a peripheral and central baclofen antagonist
Kerr D I, et al.
Brain Research, 405(1), 150-154 (1987)
D I Kerr et al.
Brain research, 405(1), 150-154 (1987-03-03)
Phaclofen, the phosphonic acid derivative of baclofen, reversibly antagonized the depression of the cholinergic twitch response of the guinea pig ileum and distal colon by either baclofen or GABA. When administered microelectrophoretically, phaclofen reversibly blocked the presumed presynaptic reduction by
Christof Geigerseder et al.
Reproductive biology and endocrinology : RB&E, 2, 13-13 (2004-03-26)
The neurotransmitter gamma-aminobutyric acid (GABA) and subtypes of GABA receptors were recently identified in adult testes. Since adult Leydig cells possess both the GABA biosynthetic enzyme glutamate decarboxylase (GAD), as well as GABA(A) and GABA(B) receptors, it is possible that
Luminal administration ex vivo of a live Lactobacillus species moderates mouse jejunal motility within minutes.
Wang B, et al.
Faseb Journal, 24(10), 4078-4088 (2010)
Mohammad Nasehi et al.
Brain research bulletin, 130, 101-106 (2017-01-24)
Activation of the GABA
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