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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Prazosin-d8 hydrochloride targets α-adrenergic receptors, specifically acting as an α-adrenergic blocker. Prazosin hydrochloride is an alpha-adrenergic blocker that can be used to treat hypertension, anxiety, and panic disorder. The deuterated form (d8) contains eight deuterium atoms replacing hydrogen atoms, which does not alter the pharmacological target but modifies the compound's metabolic stability and pharmacokinetic profile for research purposes.
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| ln Vitro |
In vitro activity of Prazosin-d8 hydrochloride is expected to be similar to that of Prazosin hydrochloride, as the deuterium substitution does not significantly affect receptor binding affinity. Prazosin hydrochloride acts as an α-adrenergic blocker. The deuterated form is used in research to study drug metabolism and pharmacokinetics. Detailed in vitro activity data for the deuterated form are not extensively documented, as it is primarily used as an internal standard or metabolic tracer.
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| ln Vivo |
In vivo activity of Prazosin-d8 hydrochloride is studied to investigate the drug's metabolism, pharmacodynamics, and pharmacokinetics. As a deuterated analog of Prazosin hydrochloride, it maintains the pharmacological activity of the parent compound while offering distinct metabolic profiles due to the kinetic isotope effect. The deuterium substitution can alter the rate of metabolic degradation, providing insights into the drug's behavior in the body.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Prazosin-d8 hydrochloride typically involves measuring its binding affinity to α-adrenergic receptors. Competitive binding assays are performed using radiolabeled ligands and membrane preparations from tissues expressing α-adrenergic receptors. The compound's ability to displace the radioligand is measured, and binding affinity (Ki) is determined. As a deuterated analog, its binding profile is expected to be similar to that of Prazosin hydrochloride.
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| Cell Assay |
In vitro cell-based assays for Prazosin-d8 hydrochloride are conducted using cell lines expressing α-adrenergic receptors. Cells are treated with the compound, and receptor activation or inhibition is measured by assessing downstream signaling pathways such as cAMP production, calcium mobilization, or reporter gene activity. The compound's ability to block α-adrenergic receptor-mediated responses is compared to that of Prazosin hydrochloride.
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| Animal Protocol |
In vivo animal studies for Prazosin-d8 hydrochloride are typically conducted to investigate pharmacokinetics and metabolism. Animals are administered the compound, and plasma and tissue samples are analyzed using mass spectrometry to quantify the drug and its metabolites. The deuterated form serves as a tracer to study metabolic pathways and the impact of deuteration on drug clearance. Standard pharmacokinetic parameters such as half-life, bioavailability, and clearance are determined.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Prazosin-d8 hydrochloride are studied to understand the impact of deuteration on drug metabolism. The compound has a molecular weight of 427.91 and a molecular formula of C19H14D8ClN5O4. Solubility includes DMSO: 7.14 mg/mL (16.69 mM). As a deuterated analog, it may exhibit altered metabolic stability compared to the non-deuterated form due to the kinetic isotope effect, which can slow down enzymatic degradation.
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| Toxicity/Toxicokinetics |
Toxicity information for Prazosin-d8 hydrochloride is expected to be similar to that of Prazosin hydrochloride. Prazosin hydrochloride is a clinically used medication with established safety profiles. As a research compound, standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only. No specific toxicity data for the deuterated form are available from the search results.
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| References |
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| Additional Infomation |
Prazosin-d8 hydrochloride is the deuterated form of Prazosin hydrochloride, an α-adrenergic blocker used to treat hypertension, anxiety, and panic disorder. The deuterated form is primarily used in research to investigate drug metabolism, pharmacodynamics, and pharmacokinetics. It has a molecular formula of C19H14D8ClN5O4 and a molecular weight of 427.91. It is intended for research use only.
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| Exact Mass |
427.186
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| CAS # |
1189508-34-6
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| PubChem CID |
46782778
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
544
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[2H]C1(C(N(C(C(N1C2=NC3=CC(=C(C=C3C(=N2)N)OC)OC)([2H])[2H])([2H])[2H])C(=O)C4=CC=CO4)([2H])[2H])[2H].Cl
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| InChi Key |
WFXFYZULCQKPIP-CADLHFACSA-N
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| InChi Code |
InChI=1S/C19H21N5O4.ClH/c1-26-15-10-12-13(11-16(15)27-2)21-19(22-17(12)20)24-7-5-23(6-8-24)18(25)14-4-3-9-28-14;/h3-4,9-11H,5-8H2,1-2H3,(H2,20,21,22);1H/i5D2,6D2,7D2,8D2;
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| Chemical Name |
[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2,2,3,3,5,5,6,6-octadeuteriopiperazin-1-yl]-(furan-2-yl)methanone;hydrochloride
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
Typically soluble in DMSO (e.g. 10 mM)
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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.) |
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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