| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
GABAB receptor[1]
Phaclofen targets the GABAB receptor, a type of GABA receptor that responds to the neurotransmitter GABA. It is a selective antagonist of the GABAB receptor. By blocking GABAB receptor activity, Phaclofen allows researchers to study mechanisms underlying motor control, pain processing, memory, and neural excitability. |
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| ln Vitro |
The effects of 1 µM of (R+) baclofen are somewhat inhibited by the GABAB antagonist phaclofen (500 µM)[5].
Phaclofen demonstrates potent in vitro antagonism of GABAB receptors. It antagonizes the depressant effect of baclofen on spinal reflex transmission in rats. Phaclofen also antagonizes baclofen or GABA-induced inhibition of cholinergic twitch responses in the guinea pig ileum and distal colon. |
| ln Vivo |
Less neuropeptide Y-like immunoreactive fibers are seen in the activated cuneate nucleus when phaclofen (2 mg/kg; ip) is administered[4]. In the dorsal striatum, phaclofen (2 mg/kg; sc) counteracts the effects of 6 mg/kg R(+) baclofen[5]. Intrathecal injection of phaclofen (100 nmol) counteracts the depressive effect of baclofen. There are no stimulatory or depressive effects of phaclofen (100 nmol) on spinal reflexes[3].
Phaclofen has been shown to antagonize the depressant effect of baclofen on spinal reflex transmission in rats in vivo. It can partially antagonize the sedative effects of (-)-baclofen. Phaclofen antagonizes post-tetanic disinhibition in the rat dentate gyrus. These in vivo studies demonstrate the compound's activity as a GABAB receptor antagonist. |
| Enzyme Assay |
The in vitro receptor binding assay for Phaclofen involves measuring its antagonism of GABAB receptor activity. The assay typically uses radioligand binding or electrophysiological techniques. Phaclofen is incubated with GABAB receptors at various concentrations. The IC50 or Ki value is determined by fitting the inhibition data to a dose-response curve.
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| Cell Assay |
In vitro cellular assays for Phaclofen typically use cell lines or tissue preparations expressing GABAB receptors. Cells are treated with Phaclofen at various concentrations. Receptor activity is measured using electrophysiological techniques or calcium imaging. The compound's ability to antagonize receptor function is quantified.
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| Animal Protocol |
Animal/Disease Models: Sprague–Dawley rats ( 180–250 g)[4]
Doses: 2 mg/kg Route of Administration: Ip. Experimental Results: Fewer neuropeptide Y-like immunoreactive fibers were detected in the stimulated cuneate nucleus. Animal/Disease Models: Male Wistar rats (280–320 g)[5] Doses: 2 mg/kg Route of Administration: Sc Experimental Results: Antagonized the effects of 6 mg/ kg R(+) baclofen in dorsal striatum. Phaclofen has been used in vivo in animal models to study GABAB receptor function. It has been shown to antagonize the depressant effect of baclofen on spinal reflex transmission in rats. Phaclofen also antagonizes post-tetanic disinhibition in the rat dentate gyrus. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Phaclofen are not extensively documented. As a small molecule with a molecular weight of 249.6, the compound is expected to have reasonable bioavailability. Its phosphonic acid structure may influence its absorption, distribution, metabolism, and excretion. Further pharmacokinetic studies are necessary to fully characterize its PK profile.
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| Toxicity/Toxicokinetics |
Toxicological data for Phaclofen are not extensively available in the public domain. As a research compound used for in vitro and in vivo studies, Phaclofen has not undergone extensive toxicological evaluation. Standard cytotoxicity assays in cell lines may have been performed to assess safety margins. Further preclinical toxicology studies would be required before clinical development.
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| References | |
| Additional Infomation |
Peripheral and central baclofen and GABA antagonists; structures are described in the first source.
Phaclofen is a selective antagonist of the GABAB receptor. It is a peripheral and central baclofen antagonist. Phaclofen is used in neuroscience research to study GABAB receptor function. The compound has a molecular weight of 249.6 and a purity of 98%. No clinical trials or regulatory approvals have been reported. |
| Molecular Formula |
C9H13CLNO3P
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|---|---|
| Molecular Weight |
249.63
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| Exact Mass |
249.032
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| CAS # |
114012-12-3
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| PubChem CID |
1641
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| Appearance |
White to off-white solid powder
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| Density |
1.432 g/cm3
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| Boiling Point |
467.1ºC at 760 mmHg
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| Flash Point |
236.3ºC
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| LogP |
2.26
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
15
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| Complexity |
238
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1C(CN)CP(=O)(O)O)Cl
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| InChi Key |
VSGNGLJPOGUDON-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
[3-amino-2-(4-chlorophenyl)propyl]phosphonic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0059 mL | 20.0296 mL | 40.0593 mL | |
| 5 mM | 0.8012 mL | 4.0059 mL | 8.0119 mL | |
| 10 mM | 0.4006 mL | 2.0030 mL | 4.0059 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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