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Bopindolol Malonate (CTK-8F8315; LS-120081; HE-393689; D-01794) is a potent beta adrenoceptor antagonist with the potential to be used for essential and renovascular hypertension.
| Targets |
Adrenergic receptor, Renin, 5-HT receptors
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|---|---|
| ln Vitro |
Bopindolol, a non-selective antagonist of beta 1- and beta 2-adrenoceptors (ARs), has been found by pharmacological, molecular biological techniques and molecular modeling to have several unique properties. Bopindolol produces sustained blockade of beta 1- and beta 2-ARs, has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Also, our recent molecular modeling studies identified possible interaction sites between bopindolol and beta-AR subtypes. The reviewed studies support our findings that bopindolol is non-selective for beta 1- and beta 2-ARs, has low affinity for beta 3-AR subtype and has pharmacological properties that are likely to be beneficial in the treatment of cardiovascular diseases [4].
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| ln Vivo |
Bopindolol (intravenous injection; 8, 16, and 32 μg/kg) is four times more potent than propranolol in dogs under anesthesia, and it inhibits isoprenaline-induced tachycardia in a dose-dependent manner[1].
Bopindolol (0.3, 1 and 3 mg/kg; IP; single dosage) lowers heart rate and diastolic blood pressure in a dose-dependent manner[2]. 1. Effects of bopindolol, a beta adrenoceptor antagonist with partial agonist activity, on the diastolic blood pressure and heart rate of pithed rats were compared with those of pindolol. 2. Both bopindolol and pindolol reduced the diastolic blood pressure (DBP) in pithed rats. Bopindolol (3.0 mg/kg) and pindolol (1.0 mg/kg) produced similar decreases in DBP of about 8 mmHg; thus pindolol had a 3-fold higher hypotensive potency when compared with bopindolol. 3. Both drugs also produced a dose-dependent decrease in heart rate. 4. Propranolol (5 mg/kg) had no antagonistic effect on the decrease in DBP produced by either bopindolol or pindolol. 5. These results suggest that both bopindolol and pindolol reduce DBP and heart rate in pithed rats through some mechanism independent of beta-adrenoceptors [2]. |
| Animal Protocol |
Male Wistar rats (260-300 g)
0.3, 1 and 3 mg/kg IP; single dosage |
| ADME/Pharmacokinetics |
Popipolol is a non-selective β-adrenergic receptor antagonist with partial agonist activity used to treat hypertension. The drug is rapidly metabolized to its active hydrolytic form. A once-daily dose of 0.5 to 4 mg of popipolol can maintain its antihypertensive effect for more than 24 hours. In the treatment of mild to moderate hypertension, its efficacy is similar to that of propranolol, metoprolol, atenolol, pinilolol, and sustained-release nifedipine. In limited clinical trials, popipolol has also successfully reduced symptoms in patients with angina, anxiety, and essential tremor. Therefore, popipolol is an effective and well-tolerated β-adrenergic receptor antagonist. [1]
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| Toxicity/Toxicokinetics |
636368 rat oral LD50 824 mg/kg Sensory organs and special senses: ptosis; Behavior: seizures or impact on epileptic threshold; Gastrointestinal tract: gastric ulcer or bleeding. Kiso and Clinical, Clinical Reports, 23(4369), 1989.
636368 rat subcutaneous LD50 481 mg/kg Behavior: ataxia; Lungs, pleura, or respiration: cyanosis; Skin and appendages (skin): hair: other. Kiso to Rinsho. Clinical Reports, 23(4369), 1989 636368 Mice oral LD50 228 mg/kg Japanese Pharmaceuticals, -(1293), 1995 636368 Rabbit oral LD50 318 mg/kg Japanese Pharmaceuticals, -(1293), 1995 636368 Rat intravenous LD50 9200 ug/kg Sensory organs and special senses: Pupil dilation: eyes; Behavior: seizures or effects on epileptic threshold; Lungs, pleural cavity or respiration: other changes Kiso to Rinsho. Clinical Reports, 23(4369), 1989 |
| References | |
| Additional Infomation |
Bopindolol malonate is a benzoic acid ester.
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| Molecular Formula |
C26H32N2O7
|
|---|---|
| Molecular Weight |
484.54
|
| Exact Mass |
380.21
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| Elemental Analysis |
C, 64.45; H, 6.66; N, 5.78; O, 23.11
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| CAS # |
82857-38-3
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| Related CAS # |
Bopindolol; 62658-63-3; 79125-22-7 (furamate); 82857-38-3 (malonate)
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| PubChem CID |
636368
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| Appearance |
Solid powder
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| LogP |
4.859
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
35
|
| Complexity |
582
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)OC(=O)C3=CC=CC=C3.C(C(=O)O)C(=O)O
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| InChi Key |
LDOONRJGLKHGJI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H28N2O3.C3H4O4/c1-16-13-19-20(25-16)11-8-12-21(19)27-15-18(14-24-23(2,3)4)28-22(26)17-9-6-5-7-10-17;4-2(5)1-3(6)7/h5-13,18,24-25H,14-15H2,1-4H3;1H2,(H,4,5)(H,6,7)
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| Chemical Name |
[1-(tert-butylamino)-3-[(2-methyl-1H-indol-4-yl)oxy]propan-2-yl] benzoate;propanedioic acid
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| Synonyms |
Bopindolol hydrogen malonate; LS-120081; D01794; Sandonorm; Bopindolol malonate; Bopindolol Malonate; AC1LCS45; SCHEMBL348872; CTK8F8315; HE393689; Wandonorm; Sandonorm (TN); Bopindolol hydrogen malonate; Bopindolol malonate [JAN];
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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 | 2.0638 mL | 10.3191 mL | 20.6381 mL | |
| 5 mM | 0.4128 mL | 2.0638 mL | 4.1276 mL | |
| 10 mM | 0.2064 mL | 1.0319 mL | 2.0638 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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