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| Targets |
CGP 36742 targets the GABAB receptor, a G protein-coupled receptor that mediates the inhibitory effects of GABA in the central nervous system. By acting as a selective antagonist, CGP 36742 blocks GABAB receptor-mediated signaling, which can modulate neurotransmitter release and neuronal excitability.
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| ln Vitro |
In vitro, CGP 36742 blocks GABAergic transmission with an IC50 of 36 μM. It is selective for GABAB over a panel of 11 receptors, including GABAA, at 1 mM. The compound inhibits baclofen-induced neuronal depression in vitro.
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| ln Vivo |
In vivo, CGP 36742 blocks baclofen-induced neuronal depression in rats, and reduces learning deficit and passive avoidance in an olfactory bulbectomy depression model. It can be used to study depression, seizures, and metabolic diseases. The compound penetrates the blood-brain barrier after peripheral administration.
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| Enzyme Assay |
In vitro receptor binding assays for GABAB antagonists typically use radioligand binding with [³H]GABA or [³H]baclofen as labeled ligands. Membranes prepared from rat brain or cells expressing GABAB receptors are incubated with the radioligand and varying concentrations of CGP 36742. Specific binding is determined by subtracting non-specific binding. IC50 or Ki values are calculated from competition binding curves.
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| Cell Assay |
In vitro cellular assays for GABAB antagonists typically use neuronal cell cultures or brain slices. Cells are treated with CGP 36742 at various concentrations, and GABAB receptor-mediated responses (e.g., inhibition of cAMP accumulation, activation of GIRK channels) are measured. The compound's ability to block baclofen-induced effects is assessed.
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| Animal Protocol |
In vivo animal studies for GABAB antagonists typically use rodent models of depression, seizures, or cognitive function. Animals are administered CGP 36742 orally or intraperitoneally at various doses. Behavioral tests (e.g., passive avoidance, forced swim test) are performed to assess antidepressant and cognitive effects. Electrophysiological recordings may be used to assess GABAB receptor-mediated responses.
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| ADME/Pharmacokinetics |
Biological Half-Life
4 hours CGP 36742 is orally active and can penetrate the blood-brain barrier after peripheral administration. It has good oral bioavailability and distributes to the central nervous system. The compound is metabolized in the liver, and its metabolites are excreted via the kidneys. Detailed PK parameters such as half-life, Cmax, and AUC are available from preclinical studies. |
| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CGP 36742 would typically include acute and repeated-dose toxicity in rodents, as well as genotoxicity and safety pharmacology assessments. As a GABAB antagonist, potential effects on seizure threshold and neuronal excitability should be monitored. The compound is generally well-tolerated at therapeutic doses.
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| References | |
| Additional Infomation |
SGS-742 is being investigated for the treatment of epilepsy and metabolic disorders.
Drug Indications It has been studied for the treatment of Alzheimer's disease, attention deficit hyperactivity disorder (ADHD), memory loss, and schizophrenia and schizoaffective disorder.Mechanism of Action SGS-742 blocks late inhibitory postsynaptic potentials and paired impulse inhibition recorded in vitro and in vivo in rat hippocampal CA1 pyramidal neurons. SGS-742 significantly enhances the release of glutamate, aspartate, glycine, and somatostatin in vivo. Long-term administration of SGS-742 upregulates GABA(B) receptors in the rat frontal cortex. A single dose significantly increases the mRNA and protein levels of NGF and BDNF in the rat cortex and hippocampus. CGP 36742 is a selective GABAB receptor antagonist with an IC50 of 32-36 μM. It is orally active and can penetrate the blood-brain barrier. The compound has been used to study depression, seizures, and metabolic diseases. It is available for research use only. |
| Molecular Formula |
C7H18NO2P
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|---|---|
| Molecular Weight |
179.2
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| Exact Mass |
179.108
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| CAS # |
123690-78-8
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| PubChem CID |
130021
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| Appearance |
White to light yellow solid powder
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| LogP |
2.106
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
11
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| Complexity |
138
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ONNMDRQRSGKZCN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H18NO2P/c1-2-3-6-11(9,10)7-4-5-8/h2-8H2,1H3,(H,9,10)
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| Chemical Name |
3-aminopropyl(butyl)phosphinic acid
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| Synonyms |
CGP-36742; CGP36742; CGP 36742
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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) |
H2O : ~125 mg/mL (~697.54 mM)
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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 | 5.5804 mL | 27.9018 mL | 55.8036 mL | |
| 5 mM | 1.1161 mL | 5.5804 mL | 11.1607 mL | |
| 10 mM | 0.5580 mL | 2.7902 mL | 5.5804 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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