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| ln Vitro |
Similar alterations in cell shape are brought about by SKF 38393 Hydrobromic acid, which also raises cAMP levels in the culture medium [2]. Increased DA- and cAMP-regulated threonine phosphorylation of the Mr 32 kD (DARPP-32) phosphoprotein is induced in cultivated GC cells by 10 μM SKF-38393 hydrochloride administered for one hour [2].
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| ln Vivo |
SKF 38393 Hydrobromide (10 mg/kg; i.p.) blocks 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced glutathione depletion [ 3]. SKF 38393 hydrobromide attenuates MPTP-induced dopamine depletion [3]. SKF 38393 hydrobromide enhances superoxide dismutase activity, thereby mimicking the effects of selegiline [3]. SKF 38393 hydrobromide increases the frequency, but not the amplitude, of tetrodotoxin-resistant excitatory postsynaptic currents, suggesting that D1 action occurs at presynaptic sites [4].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: GC Cell Tested Concentrations: 10 μM Incubation Duration: 1 hour Experimental Results: Induced increased DARPP-32 threonine phosphorylation in cultured GC cells. |
| Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse (20-25 g) [3]
Doses: 5 mg/kg, 10 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Blocks MPTP-induced glutathione depletion and attenuates MPTP Induced dopamine depletion. |
| References |
[1]. Altar CA, et al. Picomolar affinity of 125I-SCH 23982 for D1 receptors in brain demonstrated with digital subtraction auto radiography. J Neurosci. 1987 Jan;7(1):213-222.
[2]. Mayerhofer A, et al. Functional Dopamine-1 Receptors and DARPP-32 Are Expressed in Human Ovary and Granulosa Luteal Cells in Vitro. J Clin Endocrinol Metab. 1999 Jan;84(1):257-64. [3]. Muralikrishnan D, et al. SKF-38393, a dopamine receptor agonist, attenuates 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-induced neurotoxicity. Brain Res. 2001 Feb 23;892(2):241-7. [4]. Bouron A, et al. The D1 dopamine receptor agonist SKF-38393 stimulates the release of glutamate in the hippocampus. Neuroscience. 1999;94(4):1063-70. |
| Molecular Formula |
C16H18BRNO2
|
|---|---|
| Molecular Weight |
336.229
|
| Exact Mass |
0
|
| Elemental Analysis |
C, 57.16; H, 5.40; Br, 23.76; N, 4.17; O, 9.52
|
| CAS # |
20012-10-6
|
| Related CAS # |
SKF 38393 hydrochloride;62717-42-4
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| SMILES |
OC1=C(O)C=C2C(C3=CC=CC=C3)CNCCC2=C1.[H]Br
|
| InChi Key |
INNWVRBZMBCEJI-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H17NO2.BrH/c18-15-8-12-6-7-17-10-14(13(12)9-16(15)19)11-4-2-1-3-5-11;/h1-5,8-9,14,17-19H,6-7,10H2;1H
|
| Chemical Name |
1-phenyl-2,3,4,5-tetrahydro-1H-benzo[d]azepine-7,8-diol hydrobromide
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| Synonyms |
67287-49-4 (free base), 62717-42-4 (HCl), 81702-42-3 (R-isomer HCl), 62751-59-1 (R-isomer), 20012-10-6 (HBr),
|
| 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9742 mL | 14.8708 mL | 29.7415 mL | |
| 5 mM | 0.5948 mL | 2.9742 mL | 5.9483 mL | |
| 10 mM | 0.2974 mL | 1.4871 mL | 2.9742 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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