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| Targets |
Drobuline hydrochloride targets cardiac ion channels and receptors involved in the regulation of heart rhythm. As a cardiac depressant, it reduces the excitability of cardiac muscle cells, thereby slowing conduction velocity and prolonging the refractory period. The compound's mechanism of action likely involves modulation of sodium, potassium, or calcium channels in cardiac myocytes, similar to other Class I or Class III anti-arrhythmic agents. However, the specific molecular targets of drobuline hydrochloride have not been fully elucidated, and it is generally classified under "Others" in terms of target classification. The compound's cardiac depressant activity suggests that it may interact with voltage-gated ion channels, potentially inhibiting the rapid sodium current (INa) or prolonging the action potential duration through potassium channel blockade. Further research is needed to identify the precise molecular targets and to understand the structure-activity relationships that govern its anti-arrhythmic effects.
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| ln Vitro |
In vitro studies of drobuline hydrochloride have demonstrated its cardiac depressant activity in isolated cardiac tissue preparations. The compound reduces the contractility of cardiac muscle and slows the rate of spontaneous beating in isolated heart models. Electrophysiological studies using patch-clamp techniques on isolated cardiac myocytes would be expected to show that drobuline hydrochloride modulates ion channel currents, consistent with its anti-arrhythmic classification. The compound's effects on action potential parameters, such as maximum diastolic potential, action potential amplitude, and duration, can be measured in vitro using standard electrophysiological recording techniques. However, detailed in vitro activity data, including specific IC₅₀ values or potency comparisons, are not extensively documented in the available literature. The compound is primarily characterized by its functional activity as a cardiac depressant rather than by detailed mechanistic studies.
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| ln Vivo |
In vivo, drobuline hydrochloride has been used to manage abnormal heart rhythms through its cardiac depressant activity. The compound exerts its anti-arrhythmic effects by reducing cardiac excitability and slowing conduction, which helps to restore normal sinus rhythm in various arrhythmic conditions. Animal models of cardiac arrhythmia, such as those induced by coronary artery ligation or pharmacological agents, would be expected to show that drobuline hydrochloride reduces the incidence and severity of arrhythmias. However, specific in vivo efficacy data, including dose-response relationships and comparative studies with other anti-arrhythmic agents, are not extensively documented in the available literature. The compound's cardiac depressant activity suggests that it may have a narrow therapeutic index, requiring careful dose optimization to achieve anti-arrhythmic effects without causing excessive depression of cardiac function.
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| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for drobuline hydrochloride are not standard, as the compound's mechanism of action is believed to involve ion channel modulation rather than direct enzyme inhibition or receptor binding. However, radioligand binding studies could be performed using membrane preparations from cardiac tissue or cells expressing specific ion channel subunits to assess the compound's affinity for these targets. For example, binding assays using [³H]-batrachotoxin or [³H]-saxitoxin could evaluate interactions with sodium channels, while [³H]-diltiazem or [³H]-nitrendipine could assess calcium channel binding. Functional assays using isolated membrane patches or lipid bilayers could measure the direct effects of drobuline hydrochloride on ion channel conductance. These assays would provide valuable information about the compound's molecular mechanism of action and its selectivity for different ion channel subtypes.
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| Cell Assay |
In vitro cell-based assays for drobuline hydrochloride typically use cardiac myocytes or cell lines expressing cardiac ion channels. Primary cardiomyocytes isolated from animal hearts or immortalized cell lines such as HL-1 atrial cardiomyocytes can be used to study the compound's electrophysiological effects. Cells are treated with drobuline hydrochloride at various concentrations, and parameters such as action potential characteristics, ion channel currents, and cell viability are assessed. Patch-clamp electrophysiology in whole-cell or single-channel configurations provides detailed information about the compound's effects on specific ion currents. MTT or similar assays can be used to assess cytotoxicity, while calcium imaging can evaluate the compound's effects on intracellular calcium handling. These studies help to characterize the compound's cellular mechanism of action and its potential for cardiotoxicity.
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| Animal Protocol |
In vivo animal studies for drobuline hydrochloride would likely employ rodent or larger animal models of cardiac arrhythmia. Standard models include coronary artery occlusion-induced arrhythmias, ouabain-induced arrhythmias, or electrically induced ventricular fibrillation. The compound is administered intravenously or orally, and electrocardiographic parameters such as heart rate, PR interval, QRS duration, and QT interval are monitored. The incidence and duration of arrhythmic episodes are recorded to assess anti-arrhythmic efficacy. Hemodynamic parameters such as blood pressure and cardiac output may also be measured to evaluate the compound's cardiac depressant effects on overall cardiovascular function. Pharmacokinetic studies in these models provide information about the compound's absorption, distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
Drobuline hydrochloride has a molecular weight of 319.87 g/mol and a molecular formula of C₁₉H₂₆ClNO. It has a density of 1.027 g/cm³ and is soluble in DMSO at concentrations up to 150 mg/mL (468.94 mM). The compound should be stored as a powder at -20°C for up to three years or in solvent at -80°C for one year. For in vivo studies, formulations can be prepared using 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline or PBS. Detailed pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion have not been extensively characterized in the available literature. As a small lipophilic molecule with a molecular weight below 500 g/mol, drobuline hydrochloride is expected to have reasonable oral bioavailability, though its cardiac depressant activity suggests that intravenous administration may be preferred for acute management of arrhythmias.
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| Toxicity/Toxicokinetics |
The toxicity profile of drobuline hydrochloride is consistent with its classification as a cardiac depressant. Overdose or excessive dosing may lead to severe bradycardia, hypotension, and cardiac arrest, similar to other anti-arrhythmic agents. The compound should be used with caution in patients with pre-existing cardiac conduction abnormalities or heart failure. As a research compound, drobuline hydrochloride is not intended for human therapeutic use without appropriate regulatory approval. Standard laboratory safety precautions should be followed when handling the compound, including the use of appropriate personal protective equipment and working in a well-ventilated area. Comprehensive toxicological data, including acute, subchronic, and chronic toxicity studies, are not extensively documented in the available literature.
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| Additional Infomation |
Drobuline hydrochloride is an anti-arrhythmic agent with cardiac depressant activity, used to manage abnormal heart rhythms. It is the hydrochloride salt form of drobuline (free base CAS 58473-73-7), a synthetic small-molecule cardiac depressant. The compound is also known by its Chinese name 盐酸羟布林. As an anti-arrhythmic agent, drobuline hydrochloride belongs to a class of compounds that modulate cardiac electrophysiology to restore normal sinus rhythm. It is available as a research-grade reagent and is not intended for human therapeutic use without appropriate regulatory approval. The compound's mechanism of action is believed to involve modulation of cardiac ion channels, though specific molecular targets have not been fully elucidated. Drobuline hydrochloride is typically stored as a powder at -20°C and is soluble in DMSO at concentrations up to 150 mg/mL. It is used in research settings to study cardiac arrhythmias and the pharmacology of anti-arrhythmic agents.
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| Molecular Formula |
C19H26CLNO
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| Molecular Weight |
319.8688
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| Exact Mass |
319.17
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| CAS # |
68162-52-7
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| Related CAS # |
68162-52-7 (HCl);58473-73-7;
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| PubChem CID |
24198611
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.027g/cm3
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| Boiling Point |
434.8ºC at 760mmHg
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| Flash Point |
102.1ºC
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| LogP |
4.76
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
22
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| Complexity |
249
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl[H].O([H])C([H])(C([H])([H])N([H])C([H])(C([H])([H])[H])C([H])([H])[H])C([H])([H])C([H])(C1C([H])=C([H])C([H])=C([H])C=1[H])C1C([H])=C([H])C([H])=C([H])C=1[H]
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| InChi Key |
YKYKDSHUKOVMBU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H25NO.ClH/c1-15(2)20-14-18(21)13-19(16-9-5-3-6-10-16)17-11-7-4-8-12-17;/h3-12,15,18-21H,13-14H2,1-2H3;1H
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| Chemical Name |
4,4-diphenyl-1-(propan-2-ylamino)butan-2-ol;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 |
| 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 | 3.1263 mL | 15.6314 mL | 31.2627 mL | |
| 5 mM | 0.6253 mL | 3.1263 mL | 6.2525 mL | |
| 10 mM | 0.3126 mL | 1.5631 mL | 3.1263 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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