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F4429

FAUC 213

Name: FAUC 213
Brand: SIGMA

≥98% (HPLC), solid

Synonyme(s) :

2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine

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About This Item

Formule empirique (notation de Hill):

C₁₈H₁₉ClN₄

Numéro CAS:

337972-47-1

Poids moléculaire :

326.82

Numéro MDL:

MFCD06798338

Code UNSPSC :

12352200

ID de substance PubChem :

24894864

Nomenclature NACRES :

NA.77

Pureté

≥98% (HPLC)

Forme

solid

Couleur

white

Solubilité

DMSO: ~24 mg/mL (with warming up to 60 °C)
H₂O: insoluble

Température de stockage

2-8°C

Chaîne SMILES

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

Clé InChI

DTRXURJDKOYCCD-UHFFFAOYSA-N

Informations sur le gène

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

Actions biochimiques/physiologiques

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

Pictogrammes

GHS07

Mention d'avertissement

Warning

Mentions de danger

H315,H319,H335

Conseils de prudence

P261 - P264 - P271 - P280 - P302 + P352 - P305 + P351 + P338

Classification des risques

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Organes cibles

Respiratory system

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Équipement de protection individuelle

dust mask type N95 (US), Eyeshields, Gloves

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Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).

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

FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia.

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

Blocking alpha2A adrenoceptors, but not dopamine receptors, augments bupropion-induced hypophagia in rats.

Janhunen, et al.

Obesity (Silver Spring, Md.), 21, E700-E708 (2017)

Dopaminergic modulation of oscillatory network inhibition in the rat basolateral amygdala depends on initial activity state.

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

Functional Characterisation of Eel Dopamine D2 Receptors and Involvement in the Direct Inhibition of Pituitary Gonadotrophins.

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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