| Size | Price | Stock | Qty |
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| Targets |
FAUC-213 targets the human dopamine D4.4 receptor with high affinity, exhibiting a Ki value of 2.2 nM. It acts as a complete antagonist at this receptor, blocking dopamine-mediated signaling. The compound shows markedly lower activity at D2 and D3 receptors, with Ki values of 3.4 μM and 5.3 μM for hD2 and hD3, respectively. FAUC-213 also displays inhibitory activity at serotonin 5-HT1 (Ki = 1.2 μM), 5-HT2 (Ki = 0.52 μM), and α1-adrenergic (Ki = 0.27 μM) receptors. This high selectivity for D4 over D2/D3 and other targets underpins its utility as a specific D4 receptor antagonist for pharmacological studies.
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| ln Vitro |
p5-HT1 (Ki=1.2 μM), p5-HT2 (Ki=0.52 μM), and pα1 (Ki=0.27 μM) are all inhibited by FAUC 213[1].
FAUC-213 demonstrates potent antagonist activity at the human dopamine D4.4 receptor (Ki = 2.2 nM) in radioligand binding assays. It exhibits minimal activity at other dopamine receptor subtypes, as reflected in its significantly higher Ki values for D2 (3.4 μM) and D3 (5.3 μM) receptors. The compound also shows moderate binding affinity for serotonin and adrenergic receptors, but its primary and most potent activity is at the D4 receptor, making it a highly selective tool for studying D4 receptor-mediated signaling. |
| ln Vivo |
Even at just 30 mg/kg before treatment, FAUC 213 (7.5–30 mg/kg; oral; single dosage) dramatically decreased AMPH-induced elevations in hyperkinesia. The reduction in prepulse inhibition (PPI) caused by apomorphine (APO) administration at a dose of 30 mg/kg was dramatically recovered by FAUC 213 [1].
In vivo, FAUC-213 displays atypical antipsychotic activity in behavioral and neurochemical models of schizophrenia. At oral doses of 7.5–30 mg/kg, it significantly reduces amphetamine (AMPH)-induced hyperlocomotion in rats, with a marked effect observed even at 30 mg/kg. Additionally, at 30 mg/kg, FAUC-213 dramatically reverses apomorphine-induced disruptions in prepulse inhibition (PPI), a model of sensorimotor gating deficits associated with schizophrenia. These effects are consistent with an atypical antipsychotic profile, distinguishing it from typical D2 receptor antagonists. |
| Enzyme Assay |
Non-cellular enzyme/receptor binding assays for FAUC-213 typically involve competitive radioligand binding displacement studies using membrane preparations from cells expressing recombinant human dopamine receptors (D2L, D2S, D3, and D4.4). The membrane preparations are incubated with a radiolabeled D4-selective ligand (e.g., [³H]spiperone or [³H]YM-09151-2) and varying concentrations of FAUC-213. Following incubation and filtration to separate bound from free radioligand, the radioactivity is measured by scintillation counting. Binding displacement curves are generated to determine IC50 values, which are then converted to Ki values using the Cheng-Prusoff equation.
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| Cell Assay |
In vitro cellular assays for FAUC-213 involve treating cells expressing the human dopamine D4.4 receptor with the compound to assess its functional antagonist activity. Typically, cells are pre-incubated with FAUC-213 at various concentrations, followed by stimulation with a D4 receptor agonist such as dopamine. The inhibition of agonist-induced signaling, such as the reduction in cAMP accumulation (as D4 receptors are coupled to Gi proteins), is measured using a cAMP ELISA or HTRF-based assay. The IC50 for antagonism is determined from dose-response curves, and the compound's full antagonist nature is confirmed by its ability to completely block the agonist response.
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| Animal Protocol |
Animal/Disease Models: Male adult Wistar rats, body weight 300-350 g[1]
Doses: 7.5, 15, 30 mg/kg Route of Administration: oral; single dose Experimental Results: pretreatment with only 30 mg/kg can Dramatically Reduces the increase in amphetamine (AMPH)-induced hyperkinesia. In vivo animal experiments for FAUC-213 are conducted in adult male Wistar rats (300-350 g body weight). The compound is administered orally as a single dose at 7.5, 15, or 30 mg/kg. Behavioral assessments include the measurement of amphetamine-induced hyperlocomotion, where rats are pretreated with FAUC-213 before amphetamine administration and their locomotor activity is monitored. In prepulse inhibition (PPI) studies, apomorphine is administered to disrupt PPI, and the ability of FAUC-213 to restore PPI is measured using startle response equipment. These models evaluate the compound's antipsychotic-like effects and its impact on sensorimotor gating. |
| ADME/Pharmacokinetics |
FAUC-213 has a molecular weight of 326.82 and a molecular formula of C18H19ClN4. It is an orally bioavailable compound that can cross the blood-brain barrier (BBB), making it suitable for central nervous system studies. The compound has a calculated LogP of 3.312, indicating moderate lipophilicity conducive to BBB penetration. It is typically stored as a powder at -20°C for up to 3 years or at 4°C for 2 years. FAUC-213 is soluble in DMSO (~24 mg/mL) with warming to 60°C and is supplied as a white to off-white solid powder.
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| Toxicity/Toxicokinetics |
FAUC-213 is a research compound for laboratory use only and is not intended for human therapeutic or veterinary applications. In preclinical studies, it has been generally well-tolerated at the doses used for behavioral experiments (7.5–30 mg/kg). Standard laboratory safety precautions should be followed when handling the compound, as it may cause skin, eye, and respiratory irritation. The compound's high selectivity for D4 receptors over D2 and D3 receptors suggests a reduced potential for extrapyramidal side effects compared to typical antipsychotics that act on D2 receptors.
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| 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.
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| Additional Infomation |
FAUC-213 (CAS 337972-47-1) is a highly selective dopamine D4 receptor full antagonist developed as a research tool to investigate the role of D4 receptors in neuropsychiatric disorders. It exhibits atypical antipsychotic properties in behavioral and neurochemical models of schizophrenia, characterized by the ability to reduce amphetamine-induced hyperlocomotion and reverse apomorphine-induced PPI deficits. The compound has been cited in the literature for its utility in studying D4 receptor function and its potential as a lead for developing novel antipsychotic agents. It is available from various commercial suppliers for research applications.
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| Molecular Formula |
C18H19CLN4
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| Molecular Weight |
326.82
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| Exact Mass |
326.13
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| CAS # |
337972-47-1
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| PubChem CID |
10336538
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| Appearance |
White to off-white solid powder
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| Density |
1.28g/cm3
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| Index of Refraction |
1.667
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| LogP |
3.312
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
377
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=CC(=NN2C=C1)CN3CCN(CC3)C4=CC=C(C=C4)Cl
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| InChi Key |
DTRXURJDKOYCCD-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
2-[[4-(4-chlorophenyl)piperazin-1-yl]methyl]pyrazolo[1,5-a]pyridine
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| Synonyms |
FAUC213; FAUC 213; FAUC-213
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~305.98 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (3.82 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0598 mL | 15.2989 mL | 30.5979 mL | |
| 5 mM | 0.6120 mL | 3.0598 mL | 6.1196 mL | |
| 10 mM | 0.3060 mL | 1.5299 mL | 3.0598 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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