| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Metabotropic glutamate receptors (mGluR)
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|---|---|
| ln Vitro |
Glutamate and L-AP4 inhibited forskolin-stimulated cyclic AMP (cAMP) production in baby hamster kidney (BHK) cells transfected with the type IV metabotropic receptor (mGluR4). In situ hybridization revealed a high level of mRNA for the mGluR4 in the entorhinal cortex, but not in the dentate gyrus. These data demonstrate that mGluR4 receptors are negatively coupled to the cAMP cascade, and suggest that the mGluR4 receptor may be the previously described presynaptic L-AP4 receptor [1].
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| ln Vivo |
Four experiments were performed to assess the effects of ON channel blockade with the glutamate analog 2-amino-4-phosphonobutyrate (APB) on brightness and contrast perception in monkeys. In Experiment 1, we demonstrate that stimuli brighter than background (incremental stimuli) appear less bright following ON channel blockade. This decrease in brightness is not enough to account for the previously observed threshold increase for detection of incremental stimuli following APB administration (Schiller et al., 1986; Dolan & Schiller, 1989). Experiment 2 examines the role of the ON and OFF channels in the interaction between local contrast and apparent brightness. The phenomenon of simultaneous contrast was examined under normal conditions and following APB administration. We find that even following ON channel blockade, the brightness of a stimulus is determined primarily by its contrast with its immediate background. This indicates that the lateral processes involved in simultaneous contrast can operate even when one channel has been compromised. In Experiment 3, we examined the role of the ON channel in detection of stimuli that appear by virtue of changes in background vs. foreground luminance. We find that the ON channel selectively conveys information pertaining not only to the temporal nature that defines the stimulus as incremental but also to the spatial features that define it as incremental. In Experiment 4, we test the hypothesis that incremental and decremental temporal luminance ramps are differentially processed by the ON and OFF channels to a higher degree than are step-luminance changes. We find that the detection of incremental ramps is no more affected than is the detection of incremental steps following APB administration [2].
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| References |
|
| Molecular Formula |
C4H9NNAO5P
|
|---|---|
| Molecular Weight |
205.08
|
| Exact Mass |
205.011
|
| CAS # |
1263093-79-3
|
| Related CAS # |
6323-99-5
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| PubChem CID |
124081039
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| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
12
|
| Complexity |
198
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[Na+].OC([C@@H](CCP([O-])(O)=O)N)=O
|
| InChi Key |
IGWPQOULJIILQQ-AENDTGMFSA-M
|
| InChi Code |
InChI=1S/C4H10NO5P.Na/c5-3(4(6)7)1-2-11(8,9)10;/h3H,1-2,5H2,(H,6,7)(H2,8,9,10);/q;+1/p-1/t3-;/m1./s1
|
| Chemical Name |
sodium;[(3R)-3-amino-3-carboxypropyl]-hydroxyphosphinate
|
| Synonyms |
2-Amino-4-phosphonobutyric acid sodium; 1263093-79-3; DL-2-Amino-4-phosphonobutyric acid sodium salt; Sodium;[(3R)-3-amino-3-carboxypropyl]-hydroxyphosphinate;
|
| 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 | 4.8761 mL | 24.3807 mL | 48.7615 mL | |
| 5 mM | 0.9752 mL | 4.8761 mL | 9.7523 mL | |
| 10 mM | 0.4876 mL | 2.4381 mL | 4.8761 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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