CGP 35348 |
| カタログ番号GC11153 |
CGP 35348 は、選択的、脳浸透性、中枢活性 GABAB 受容体アンタゴニストであり、EC50 は 34 μM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 123690-79-9
Sample solution is provided at 25 µL, 10mM.
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CGP 35348 is a selective antagonist of γ-aminobutyric acidB (GABAB) receptor with IC50 value of 34 μM [1].
The GABAB receptor is a metabotropic transmembrane receptors for GABA that is linked via G-protein to potassium channel. It stimulates the opening of K+ channel and hyperpolarize the neuron.
CGP 35348 is a selective GABAB receptor antagonist that can penetrate the blood-brain barrier. In rat cortex slices, CGP 35348 inhibited the potentiating effect of L-baclofen on adenylate cyclase stimulated by noradrenaline. In the hippocampal slice, CGP 35348 (10, 30, 100 μM) inhibited membrane hyperpolarization induced by L-baclofen (10 μM) and the inhibitory postsynaptic potential [1].
In the spinal cord of the rat, CGP 35348 (3-30 μg) inhibited L-baclofen-induced antinociception in a dose-dependent way [2]. In the rat, CGP 35348 induced pain-like response to mechanical stimulation in a dose-dependent way and reduced the paw withdrawal threshold to pressure [3]. In rats, CGP 35348(500 mg/kg) significantly reduced food consumption by the blockade of central GABAB receptors [4].
References:
[1]. Olpe HR, Karlsson G, Pozza MF, et al. CGP 35348: a centrally active blocker of GABAB receptors. Eur J Pharmacol, 1990, 187(1): 27-38.
[2]. Hammond DL, Washington JD. Antagonism of L-baclofen-induced antinociception by CGP 35348 in the spinal cord of the rat. Eur J Pharmacol, 1993, 234(2-3): 255-262.
[3]. Hao JX, Xu XJ, Wiesenfeld-Hallin Z. Intrathecal gamma-aminobutyric acidB (GABAB) receptor antagonist CGP 35348 induces hypersensitivity to mechanical stimuli in the rat. Neurosci Lett, 1994, 182(2): 299-302.
[4]. Patel SM, Ebenezer IS. The effects of intraperitoneal and intracerebroventricular administration of the GABAB receptor antagonist CGP 35348 on food intake in rats. Eur J Pharmacol, 2004, 503(1-3): 89-93.
| Cas No. | 123690-79-9 | SDF | |
| Chemical Name | (S)-(3-aminopropyl)(diethoxymethyl)phosphinic acid | ||
| Canonical SMILES | O[P@@](CCCN)(C(OCC)OCC)=O | ||
| Formula | C8H20NO4P | M.Wt | 225.22 |
| 溶解度 | DMSO: 0.1 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 10 mg/ml | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.4401 mL | 22.2005 mL | 44.401 mL |
| 5 mM | 0.888 mL | 4.4401 mL | 8.8802 mL |
| 10 mM | 0.444 mL | 2.2201 mL | 4.4401 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)
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