| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
CGP36216 hydrochloride targets the GABAB receptor, a G protein-coupled receptor (GPCR) that mediates slow inhibitory neurotransmission in the central nervous system. It binds to the GABAB receptor with a Ki value of 0.3 microM. Importantly, CGP36216 is selective for presynaptic GABAB receptors and is ineffective at postsynaptic GABAB receptors, allowing researchers to selectively block presynaptic inhibitory feedback mechanisms.
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| ln Vitro |
CGP36216 is inactive at postsynaptic GABA receptors but more active at presynaptic receptors. CGP36216 (100 µM) increases the frequency of spontaneous firing of VTA-DA neurons.
CGP36216 hydrochloride binds to GABAB receptor with a Ki of 0.3 microM. CGP36216 is ineffective at GABA postsynaptic receptors but is appreciably more active at presynaptic receptors. At 100 microM, CGP36216 can increase the frequency of spontaneous firing in VTA-DA (ventral tegmental area dopamine) neurons. This effect is likely due to blockade of presynaptic GABAB receptors that normally inhibit glutamate release onto these neurons, resulting in disinhibition and increased firing. |
| ln Vivo |
Animal Model: Rats[3]. Dosage: 20 μg/Rat. Administration: Intra-VTA injection (ventral tegmental area). Result: Abolishes CPP induced by intra-VTA injection of morphine.
No specific in vivo data was found for CGP36216 hydrochloride. However, based on its mechanism as a selective presynaptic GABAB receptor antagonist, it would be expected to enhance glutamatergic transmission in specific brain circuits by blocking presynaptic feedback inhibition. This could have complex effects on anxiety and fear-related behaviors, consistent with its indication for anxiety and trauma-related disorder research. Specific in vivo efficacy data is not provided. |
| Enzyme Assay |
Standard GABAB receptor radioligand binding assay: Rat brain cortical or cerebellar membranes (100-200 ug protein) are prepared by homogenization in 50 mM Tris-HCl buffer (pH 7.4) containing 2.5 mM CaCl2. Membranes are incubated with 1-2 nM [3H]-CGP54626A (a selective GABAB antagonist) and varying concentrations of CGP36216 hydrochloride (0.001-1000 microM) in assay buffer at 4degC for 60-90 minutes. Nonspecific binding is determined with 100 uM GABA or 100 uM CGP55845. Bound radioactivity is separated by rapid filtration through GF/B filters and quantified by scintillation counting. Ki value (0.3 microM) is calculated.
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| Cell Assay |
Standard electrophysiological assay for presynaptic GABAB receptor function: Whole-cell patch-clamp recordings are performed on ventral tegmental area dopamine (VTA-DA) neurons in acute rat brain slices (250-300 um thickness). Neurons are voltage-clamped at -70 mV. Excitatory postsynaptic currents (EPSCs) are evoked by electrical stimulation (0.1 Hz) in the presence of picrotoxin (50 microM) to block GABAA receptors. CGP36216 (100 microM) is bath-applied. The frequency and amplitude of spontaneous EPSCs are recorded. The ability of CGP36216 to increase spontaneous firing frequency is measured.
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| Animal Protocol |
No specific animal protocol was found. To study the role of presynaptic GABAB receptors in anxiety, male Sprague-Dawley rats (200-300 g) may be administered CGP36216 hydrochloride (e.g., 1-10 mg/kg) via intracerebroventricular (ICV) injection or systemic administration. Behavioral tests including elevated plus maze, open field test, and fear conditioning are conducted 30-60 minutes post-dosing. Parameters measured include time spent in open arms, locomotor activity, and freezing behavior. Comparison to vehicle-treated and positive control (e.g., diazepam) groups is performed.
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| ADME/Pharmacokinetics |
No specific PK data was found. CGP36216 hydrochloride is a small molecule with molecular weight 187.6. As a phosphinic acid derivative, it is expected to have moderate water solubility and limited blood-brain barrier penetration. The compound is typically used in ex vivo brain slice preparations or local administration (ICV) for central nervous system studies. Systemic pharmacokinetic parameters (half-life, oral bioavailability) are not reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data was found. As a selective GABAB antagonist, CGP36216 hydrochloride is expected to have low acute toxicity at research doses. However, GABAB antagonists can have proconvulsant effects and may increase anxiety-like behaviors, depending on the dosing regimen and brain region. The compound is for research use only and should be handled with standard laboratory safety precautions. Not for human consumption.
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| References |
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| Additional Infomation |
CGP36216 hydrochloride (CAS: 1781834-71-6) has molecular formula C₅H1₅ClNO2P and molecular weight 187.6. Its chemical name is 3-aminopropyl(methyl)phosphinic acid hydrochloride. It is a selective antagonist at GABA presynaptic receptors, binding to GABAB receptor with Ki = 0.3 microM. It is effective at presynaptic receptors but inactive at postsynaptic receptors. For research use only in anxiety and trauma-related disorder studies.
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| Molecular Formula |
C5H15CLNO2P
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|---|---|
| Molecular Weight |
187.60
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| Exact Mass |
187.053
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| CAS # |
1781834-71-6
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| Related CAS # |
CGP36216;123691-29-2
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| PubChem CID |
90488815
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| Appearance |
Typically exists as solids at room temperature
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| LogP |
0
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| Hydrogen Bond Donor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
10
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| Complexity |
116
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| Defined Atom Stereocenter Count |
0
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| SMILES |
P(O)(=O)(CC)CCCN.Cl
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| InChi Key |
CFQFXUJBWMPODB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H14NO2P.ClH/c1-2-9(7,8)5-3-4-6;/h2-6H2,1H3,(H,7,8);1H
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| Chemical Name |
3-aminopropyl(ethyl)phosphinic acid;hydrochloride
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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 | 5.3305 mL | 26.6525 mL | 53.3049 mL | |
| 5 mM | 1.0661 mL | 5.3305 mL | 10.6610 mL | |
| 10 mM | 0.5330 mL | 2.6652 mL | 5.3305 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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