FAUC 213

Names

[ Name ]:
FAUC 213

[Synonym ]:
FAUC 213
2-[4-(4-Chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine

Biological Activity

[Description]:

FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[Target]

hD4.4 Receptor:2.2 nM (Ki)

hD2 Receptor:3.4 μM (Ki)

hD3 Receptor:5.3 μM (Ki)

[In Vitro]

FAUC 213 inhibits p5-HT1 (Ki=1.2 μM)，p5-HT2 (Ki=0.52 μM)，pα1 (Ki=0.27 μM)[1].

[In Vivo]

FAUC 213 (7.5-30 mg/kg; orally; single dose) significantly reduces this elevation in AMPH-induced locomotor hyper-activity only pre-treatment with 30 mg/kg. FAUC 213 significantly restores the prepulse inhibition (PPI) reduction caused by the apomorphine (APO) treatment with 30 mg/kg[1]. Animal Model: Male adult Wistar rats weighing 300-350 g[1] Dosage: 7.5, 15, 30 mg/kg Administration: Orally; single dose Result: Significantly reduced this elevation in amphetamin (AMPH)-induced locomotor hyper-activity only pre-treatment with 30 mg/kg.

[References]

[1]. Frank Boeckler, et al. FAUC 213, a highly selective dopamine D4 receptor full antagonist, exhibits atypical antipsychotic properties in behavioural and neurochemical models of schizophrenia. Psychopharmacology (Berl). 2004 Aug;175(1):7-17.

Chemical & Physical Properties

[ Density]:
1.28g/cm3

[ Molecular Formula ]:
C₁₈H₁₉ClN₄

[ Molecular Weight ]:
326.82300

[ Exact Mass ]:
326.13000

[ PSA ]:
23.78000

[ LogP ]:
3.31280

[ Index of Refraction ]:
1.667

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

Articles

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

Psychopharmacology 175 , 7-17 , (2004)

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 anta...

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).

J. Med. Chem. 44 , 2691-2694 , (2001)

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 co...