| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Practolol targets the β1-adrenergic receptor, a subtype of beta-adrenergic receptor found predominantly in the heart. It acts as a selective antagonist, blocking the effects of catecholamines such as norepinephrine and epinephrine at this receptor. By blocking β1 receptors, it reduces heart rate, cardiac contractility, and cardiac output.
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| ln Vitro |
After giving spontaneously contracting trachea to guinea pigs, pactolol (10 μM; 30 min) resists the contractile effects of R0363 in a preferred and selective manner [1]. Granulosa cells produce progesterone in response to a burst (-) dosage of pactolol (10 nM-100 μM) [2].
In vitro, practolol is a potent and selective β1-adrenergic receptor antagonist. Its affinity and selectivity for β1 over β2 receptors have been characterized in radioligand binding assays. It inhibits the effects of β1-receptor agonists in isolated tissue preparations. These activities confirm its profile as a selective β1-blocker. |
| ln Vivo |
Pracolol (0.5 mg/kg; intravenously) lowers heart rate, left ventricular dP/dt max, myocardial blood flow, and cardiac output in intact closed-chest dogs [3]. Pracolol (0.5 mg/kg; iv) lowers normal myocardial blood flow, while local regional blood flow stays unaffected following coronary artery ligation [3].
In vivo, practolol was used clinically to manage angina pectoris, cardiac arrhythmias, and hypertension. Its effects were mediated through its selective blockade of β1-adrenergic receptors in the heart. However, it was withdrawn from the market due to severe adverse effects, including oculomucocutaneous syndrome. |
| Enzyme Assay |
The in vitro receptor binding assay for practolol typically involves radioligand displacement studies using membrane preparations from cells expressing β1-adrenergic receptors. The compound's affinity is determined by measuring its ability to displace a specific radiolabeled ligand. Its selectivity for β1 over β2 receptors is assessed using similar assays.
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| Cell Assay |
In vitro cellular assays for practolol assess its functional antagonism at β1-adrenergic receptors. Cells expressing the β1 receptor are stimulated with a β-agonist, and the compound's ability to inhibit downstream signaling, such as cAMP accumulation, is measured. These assays demonstrate the compound's functional activity in a relevant cellular context.
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| Animal Protocol |
In vivo animal studies for practolol were conducted in animal models of hypertension and arrhythmias to evaluate its efficacy. However, its clinical development was halted due to severe adverse effects observed in humans. It is now used primarily as a research tool.
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| ADME/Pharmacokinetics |
Practolol is a small molecule that was administered orally. Its pharmacokinetic properties are characterized by good absorption and a relatively long half-life. It is metabolized in the liver and excreted in urine. Its pharmacokinetic profile supported once-daily dosing.
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| Toxicity/Toxicokinetics |
Practolol is associated with severe adverse effects, including oculomucocutaneous syndrome, which led to its withdrawal from the market. Other adverse effects include those common to beta-blockers, such as bradycardia, hypotension, and bronchospasm. Its toxicity is a key aspect of its research applications.
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| References |
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| Additional Infomation |
Pramolol is an n-(4-hydroxyphenyl)acetamide, in which the hydrogen atom on the phenolic hydroxyl group is replaced by a 3-(isopropylaminoamino)-2-hydroxypropyl group. It is a selective beta-blocker and has been used for the emergency treatment of arrhythmias. It has the effects of both a beta-adrenergic antagonist and an antiarrhythmic drug. It is a propanolamine, belonging to the ethanolamine, secondary alcohol, acetamide, and secondary amino compounds.
A beta-adrenergic antagonist, used for the emergency treatment of arrhythmias. A beta-1 adrenergic antagonist, used for the emergency treatment of arrhythmias. Indications For the emergency treatment of arrhythmias. Mechanism of Action Like other beta-adrenergic antagonists, pramolol competitively binds to sympathetic receptors with adrenergic neurotransmitters such as catecholamines. Similar to propranolol and timolol, pranolactone binds to β1-adrenergic receptors in cardiac and vascular smooth muscle, inhibiting the effects of catecholamines such as adrenaline and noradrenaline, thereby reducing heart rate, cardiac output, and systolic and diastolic blood pressure. Pranolactone is a β-adrenergic receptor antagonist used for the emergency treatment of arrhythmias. β-blockers inhibit normal adrenaline-mediated sympathetic activity but have little effect on the resting state. That is, they can reduce the effects of excitation/physical activity on heart rate and the ability of blood vessels to constrict and dilate. Practolol is a first-generation selective β1-adrenergic receptor blocker that was withdrawn from the market due to severe adverse effects. It is a potent and selective β1-adrenergic receptor antagonist. It is used as a research tool for studying beta-adrenergic receptor pharmacology. It is not approved for clinical use. |
| Molecular Formula |
C14H22N2O3
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|---|---|
| Molecular Weight |
266.34
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| Exact Mass |
266.163
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| CAS # |
6673-35-4
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| Related CAS # |
Practolol-d7;2714414-11-4
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| PubChem CID |
4883
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| Appearance |
White to off-white solid powder
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| Density |
1.0807 (rough estimate)
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| Boiling Point |
409.54°C (rough estimate)
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| Melting Point |
134-136° (BuOAc)
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| Index of Refraction |
1.5110 (estimate)
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| LogP |
1.846
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
19
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| Complexity |
263
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DURULFYMVIFBIR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H22N2O3/c1-10(2)15-8-13(18)9-19-14-6-4-12(5-7-14)16-11(3)17/h4-7,10,13,15,18H,8-9H2,1-3H3,(H,16,17)
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| Chemical Name |
N-[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl]acetamide
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| Synonyms |
Dalzic Eraldin Teranol ICI 50172 Eralzdin Practolol ICI 50172 ICI-50172 ICI50172 Practolol Practolol, Eralzdin
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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) |
DMSO : ~100 mg/mL (~375.46 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.39 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7546 mL | 18.7730 mL | 37.5460 mL | |
| 5 mM | 0.7509 mL | 3.7546 mL | 7.5092 mL | |
| 10 mM | 0.3755 mL | 1.8773 mL | 3.7546 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06149507 | Not yet recruiting | Drug: Acetaminophen Drug: Ibuprofen |
Celiac Disease in Children | Cairo University | 2024-03-01 | Phase 4 |
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