| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
SKF 38393 HCl (SKF38393; SKF-38,393; SKF 38,393; SKF-38393A), the hydrochloride salt of SKF-38393, is a novel potent and selective dopamine D1 receptor agonist with IC50 of 110 nM, and the (+)-enantiomer is the active isomer. Desynchronization of electroencephalogram activity in rats is associated with SKF 38393-induced agonism of the D1DR. Additionally, serotonin SR-2C (5-HT1C receptor) agonism was demonstrated by SKF 38393. D5DR is triggered by SKF 38393 HCl. The intravenous administration of SKF 38393 significantly changed the activity of dopamine cells in rats treated with gallamine and locally anesthetized. Both rises and falls in the firing rate were noted in these rats.
| Targets |
dopamine D1 receptor; D5 receptor
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
SKF 38393 hydrochloride is an agonist of D1 with IC50 of 110 nM.
Iodinated SCH 23390, 125I-SCH 23982 (DuPont-NEN), was examined using quantitative autoradiography for its potency, selectivity, and anatomical and neuronal localization of binding to the dopamine D1 receptor in rat brain sections. 125I-SCH 23982 bound to D1 sites in the basal ganglia with very high affinity (Kd values of 55-125 pM), specificity (70-85% of binding was displaced by 5 microM cis-flupenthixol), and in a saturable manner (Bmax values of 65-176 fmol/mg protein). Specific 125I-SCH 23982 binding was displaced by the selective D1 antagonists SCH 23390 (IC50 = 90 pM) and cis-flupenthixol (IC50 = 200 pM) and the D1 agonist SKF 38393 (IC50 = 110 nM) but not by D2-selective ligands (I-sulpiride, LY 171555) or the S2 antagonist cinanserin. Compared with 3H-SCH 23390, the 5- to 10-fold greater affinity for the D1 site and 50-fold greater specific radioactivity of 125I-SCH 23982 makes it an excellent radioligand for labeling the D1 receptor. The concentrations of D1 sites were greatest in the medial substantia nigra and exceeded by over 50% the concentration of D1 sites in the lateral substantia nigra, caudoputamen, nucleus accumbens, olfactory tubercle, and entopeduncular nucleus. Lower concentrations of D1 sites were present in the internal capsule, dorsomedial frontal cortex, claustrum, and layer 6 of the neocortex. D1 sites were absent in the ventral tegmental area. Intrastriatal injections of the axon-sparing neurotoxin, quinolinic acid, depleted by 87% and by 46-58% the concentrations of displaceable D1 sites in the ipsilateral caudoputamen and medial and central pars reticulata of the substantia nigra, respectively. No D1 sites were lost in the lateral substantia nigra. Destruction of up to 94% of the mesostriatal dopaminergic projection with 6-hydroxydopamine did not reduce D1 binding nor, with one exception, increase striatal or nigral D1 receptor concentrations. 125I-SCH 23982 selectively labels D1 binding sites on striatonigral neurons with picomolar affinity, and these neurons contain the majority of D1 sites in rat brain[1]. |
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| Cell Assay |
Cell Line: GC cells
Concentration: 10 μmol/L Incubation Time: 1 hour Result: Induced increased threonine-phosphorylation of DA- and cAMP-regulated phosphoprotein of Mr 32 kD (DARPP-32) in cultured GC cells. |
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| Animal Protocol |
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| References |
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| Additional Infomation |
A selective D1 dopamine receptor agonist used primarily as a research tool.
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| Molecular Formula |
C16H18CLNO2
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| Molecular Weight |
291.77
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| Exact Mass |
291.102
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| Elemental Analysis |
C, 65.86; H, 6.22; Cl, 12.15; N, 4.80; O, 10.97
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| CAS # |
62717-42-4
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| Related CAS # |
SKF 38393 hydrobromide; 20012-10-6; (R)-SKF 38393 hydrochloride; 81702-42-3; 62751-59-1 (R-isomer); 67287-49-4; 62717-42-4 (HCl)
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| PubChem CID |
147514
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
3.506
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
291
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O([H])C1=C(C([H])=C2C([H])([H])C([H])([H])N([H])C([H])([H])C([H])(C3C([H])=C([H])C([H])=C([H])C=3[H])C2=C1[H])O[H]
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| InChi Key |
YEWHJCLOUYPAOH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H17NO2.ClH/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
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| Chemical Name |
5-phenyl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diol;hydrochloride
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| Synonyms |
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4274 mL | 17.1368 mL | 34.2736 mL | |
| 5 mM | 0.6855 mL | 3.4274 mL | 6.8547 mL | |
| 10 mM | 0.3427 mL | 1.7137 mL | 3.4274 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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