CGP 36742
Based on 1 publication(s) in Google Scholar
CGP 36742 (SGS-742) is an orally active and selective antagonist of GABAB receptor (IC50 = 36 µM). CGP 36742 is a brain-penetrant compound and improves cognitive performances. CGP 36742 can be used for depression study.
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- Pureza: 98.0%
- No. CAS: 123690-78-8
- Fòrmula: C7H18NO2P
- Peso molecular:179.20
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CGP 36742
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Actividad biológica
IC50: 32 μM (GABAB)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Oocyte | IC50 |
38 μM
Compound: 7, CGP-36742
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Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
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[PMID: 24900248] |
| Oocyte | IC50 |
508 μM
Compound: 7, CGP-36742
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Antagonist activity at human recombinant GABAA alpha1beta2gamma2L receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAA alpha1beta2gamma2L receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
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[PMID: 24900248] |
| Oocyte | IC50 |
62 μM
Compound: 2, SGS742
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Antagonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
Antagonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
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[PMID: 18528996] |
| Oocyte | IC50 |
62 μM
Compound: 7, CGP-36742
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Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
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[PMID: 24900248] |
CGP 36742 blocks the late inhibitory postsynaptic potential (i.p.s.p.) in CA1 pyramidal neurons[2].
CGP 36742 (1 μM) prevents kynurenate from antagonizing N-methyl-d-aspartate (NMDA) (HY-17551)-induced release of noradrenaline from rat brain slices potently[4].
CGP 36742 (1 μM) increases the somatostatin-like immunoreactivity (SRIF-LI) release from hippocampal slices exposed to NMDA[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CGP 36742 (10 mg/kg; i.p.; once daily for 14 d) are effective in an olfactory bulbectomy (OB) model of depression in rats[1].
CGP 36742 (30-200 mg/kg; p.o.; administered in a cumulative manner at intervals of 2.5-3 h) blocks the neuronal depression induced by iontophoretically applied baclofen in anaesthetized rats[2].
CGP 36742 (1-10 mg/kg; i.v.; 25-30 min before test) dose dependently attenuates paired-pulse inhibition measured at latencies of > 100 ms[2].
CGP 36742 (50-1000 mg/kg; i.v. or p.o.; once or twice) can penetrate the blood-brain barrier in male Sprague-Dawley rats [3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Albino Swiss mice (22-26 g)[1]
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Dosage:10, 30 mg/kg
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Administration:Intraperitoneal injection (i.p.); 30 min before test
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Result:Significantly reduced the immobility time in the forced swim test at both doses (10 mg/kg by 32% and 30 mg/kg by 40%).
Had no effect on the spontaneous locomotor activity in mice.
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Animal Model:Male Wistar rats (200-250 g), olfactory bulbectomy model[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.); once daily for 14 d
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Result:Single administration did not alter the olfactory bulbectomy (OB)-induced learning deficit, induced following bulbectomy.
Restored the learning deficit in OB rats (five trials) without affecting performance in sham-operated animals.
Reduced the OB-related increase in the number of rearings + peepings.
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Animal Model:Male rats (weighing 280-320 g)[2]
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Dosage:30-200 mg/kg
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Administration:Oral gavage (p.o.); administered in a cumulative manner at intervals of 2.5-3 h.
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Result:Antagonized baclofen-induced inhibitory effects on spontaneously firing cortical neurons in a dose-dependent manner.
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Animal Model:Male Sprague-Dawley rats (200-325 g)[3]
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Dosage:50, 100, 200, 500, 1000 mg/kg
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Administration:Intravenous injection (i.v.) via tail vein of 50, 100, 200 mg/kg, oral gavage (p.o.) of 500, 1000 mg.kg; in two rats given an i.v. injection of 100 mg/kg, a second i.v. injection of 100 mg/kg was given after 6 h and samples were collected for another 6 h.
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Result:The appearance in the rat brain frontal cortex after i.v. injection was seen in the first 30 min dialyzate collected and peaked in the 1 h dialysate.
Removed or metabolized from brain in dialyzates collected 3 h post-injection.
The presence was again seen 30 min after the second 100 mg/kg i.v. injection administered 6 h after the first injection.
Showed the appearance in the third ventricle of the rat brain after two i.v. injections of 100 mg/kg with an interval of 6 h.
Showed that the highest concentrations were seen 1.5 or 2 h after the p.o..
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 123690-78-8
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Appearance Solid
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Peso molecular 179.20
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Fòrmula C7H18NO2P
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Color White to light yellow
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SMILES
O=P(CCCN)(O)CCCC
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Synonyms
SGS-742
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
GABA production induced by imipridones is a targetable and imageable metabolic alteration in diffuse midline gliomas. [Abstract]2024 Jun 10:2024.06.07.597982. PMID: 38915617
Solvente y solubilidad
H2O : ≥ 100 mg/mL (558.04 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Nowak G, et al. Antidepressant-like activity of CGP 36742 and CGP 51176, selective GABAB receptor antagonists, in rodents. Br J Pharmacol. 2006 Nov;149(5):581-90. [Content Brief]
[2]. Olpe HR, et al. The actions of orally active GABAB receptor antagonists on GABAergic transmission in vivo and in vitro. Eur J Pharmacol. 1993 Mar 23;233(2-3):179-86. [Content Brief]
[3]. Andrén PE, et al. Blood-brain barrier penetration of 3-aminopropyl-n-butylphosphinic acid (CGP 36742) in rat brain by microdialysis/mass spectrometry. J Mass Spectrom. 1998 Mar;33(3):281-7. [Content Brief]
[4]. Pittaluga A, et al. Potentiation of NMDA receptor function through somatostatin release: a possible mechanism for the cognition-enhancing activity of GABA(B) receptor antagonists. Neuropharmacology. 2001 Sep;41(3):301-10. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 5.5804 mL | 27.9018 mL | 55.8036 mL | 139.5089 mL |
| 5 mM | 1.1161 mL | 5.5804 mL | 11.1607 mL | 27.9018 mL | |
| 10 mM | 0.5580 mL | 2.7902 mL | 5.5804 mL | 13.9509 mL | |
| 15 mM | 0.3720 mL | 1.8601 mL | 3.7202 mL | 9.3006 mL | |
| 20 mM | 0.2790 mL | 1.3951 mL | 2.7902 mL | 6.9754 mL | |
| 25 mM | 0.2232 mL | 1.1161 mL | 2.2321 mL | 5.5804 mL | |
| 30 mM | 0.1860 mL | 0.9301 mL | 1.8601 mL | 4.6503 mL | |
| 40 mM | 0.1395 mL | 0.6975 mL | 1.3951 mL | 3.4877 mL | |
| 50 mM | 0.1116 mL | 0.5580 mL | 1.1161 mL | 2.7902 mL | |
| 60 mM | 0.0930 mL | 0.4650 mL | 0.9301 mL | 2.3251 mL | |
| 80 mM | 0.0698 mL | 0.3488 mL | 0.6975 mL | 1.7439 mL | |
| 100 mM | 0.0558 mL | 0.2790 mL | 0.5580 mL | 1.3951 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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