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100mg | ||
250mg | ||
500mg |
ln Vitro |
(+)-DiHydrexidine HydroHClide (DHX) is a highly powerful, bioavailable D1 dopamine receptor agonist. (+)-DiHydrexidine was evaluated for activity against 40 additional binding sites and was inert against all receptors except the D2 dopamine receptor (IC50=130 nM) and the alpha2 adrenergic receptor (IC50=230 nM) Activity (IC50 greater than 10 µM). DiHydrexidine stereoselectively and efficiently competes for D1 binding sites in [3H]SCH23390-labeled rat striatal membranes with an IC50 of around 10 nM, whereas the archetypal D1 agonist SKF38393 has an IC50 of roughly 30 nM [2].
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ln Vivo |
In order to investigate the functional state of striatal neurons upon D1 receptor activation, D1 agonist (+)-DiHydrexidine (30 mg/kg, i.p.) was administered into AC5+/+ and AC5-/- animals, resulting in the formation of dorsolateral striations. Forty-five minutes later, the bodies underwent RT-PCR analysis. These studies demonstrated that the immediate early genes c-fos, egr-1, and junB were considerably more inducibly induced in the NAc by (+)-dioxysidine in AC5-/-mice as opposed to AC5+/+ mice. However, AC5-/-mice exhibit inhibition of induction in the dorsolateral striatum [3].
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References |
[1]. Lewis MM, et al. Homologous desensitization of the D1A dopamine receptor: efficacy in causing desensitizationdissociates from both receptor occupancy and functional potency. J Pharmacol Exp Ther. 1998 Jul;286(1):345-53.
[2]. Mottola DM, et al. Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. J Pharmacol Exp Ther. 1992 Jul;262(1):383-93. [3]. Kim KS, et al. Adenylyl cyclase-5 activity in the nucleus accumbens regulates anxiety-related behavior. J Neurochem. 2008 Oct;107(1):105-15 |
Molecular Formula |
C17H18CLNO2
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Molecular Weight |
303.783323764801
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CAS # |
158704-02-0
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Related CAS # |
Dihydrexidine hydrochloride;137417-08-4;Dihydrexidine;123039-93-0
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SMILES |
OC1=C(O)C=C(CC[C@]2([H])[C@]3([H])C4=C(C=CC=C4)CN2)C3=C1.Cl
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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 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 | 3.2919 mL | 16.4593 mL | 32.9186 mL | |
5 mM | 0.6584 mL | 3.2919 mL | 6.5837 mL | |
10 mM | 0.3292 mL | 1.6459 mL | 3.2919 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.