F4429
FAUC 213
≥98% (HPLC), solid
别名:
2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine
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关于此项目
经验公式（希尔记法）:
C18H19ClN4
化学文摘社编号:
分子量:
326.82
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
InChI key
DTRXURJDKOYCCD-UHFFFAOYSA-N
SMILES string
Clc1ccc(cc1)N2CCN(CC2)Cc3cc4ccccn4n3
InChI
1S/C18H19ClN4/c19-15-4-6-17(7-5-15)22-11-9-21(10-12-22)14-16-13-18-3-1-2-8-23(18)20-16/h1-8,13H,9-12,14H2
assay
≥98% (HPLC)
form
solid
color
white
solubility
DMSO: ~24 mg/mL (with warming up to 60 °C), H2O: insoluble
storage temp.
2-8°C
Gene Information
human ... DRD2(1813), DRD3(1814), DRD4(1815)
Application
FAUC 213 has been used as a selective dopamine receptor D4-R antagonist:
- to test its effect on the expression of luteinizing hormone in eel pituitary primary cell culture
- to test its effect on bupropion induced hypophagia and locomotion in rats
- to test its modulatory effects on rat basolateral amygdala in the presence of dopamine
Biochem/physiol Actions
FAUC 213 displays antipsychotic properties and may be of use in studies related to behavioral neurobiology and neurochemistry.
Highly selective D4 dopamine receptor full antagonist
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
法规信息
新产品
此项目有
S Löber et al.
Journal of medicinal chemistry, 44(17), 2691-2694 (2001-08-10)
Structure dependent efficacy studies in the field of selective D4 ligands led to the 2-aminomethyl substituted azaindole 2 (FAUC 213) that displayed strong D4 binding, high subtype selectivity, and complete antagonist properties in ligand-induced mitogenesis experiments. According to our schematic
Blocking alpha2A adrenoceptors, but not dopamine receptors, augments bupropion-induced hypophagia in rats.
Janhunen, et al.
Obesity (Silver Spring, Md.), 21, E700-E708 (2017)
Hironori Ohshiro et al.
Neuropharmacology, 61(4), 857-866 (2011-06-21)
The amygdala receives dopaminergic innervation, and dopamine (DA) enhances various activities in cognitive and emotional behaviors. Periodic bursts of spontaneous inhibitory postsynaptic currents (IPSCs) with a low (<1 Hz) inter-event frequency have been observed in projection neurons of the basolateral
Frank Boeckler et al.
Psychopharmacology, 175(1), 7-17 (2004-03-10)
2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213) is a highly selective antagonist at the dopamine D(4) receptor subtype. It was designed as a derivative of two partial antagonists and has been proven to be a complete antagonist in mitogenesis assay. In the present study
C Jolly et al.
Journal of neuroendocrinology, 28(9) (2016-07-28)
In various vertebrate species, dopamine (DA) exerts an inhibitory action on reproduction. In the European eel, DA plays a pivotal role in the inhibitory control of gonadotroph function and the blockade of puberty. In vivo studies have suggested that this
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