Pindolol (Synonyms: DL-Pindolol) |
Katalog-Nr.GC17734
One-Click Copy Product Info
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Pindolol (LB-46) ist ein nicht-selektiver β-Blocker mit partieller agonistischer Wirkung auf den beta-adrenergen Rezeptor und wirkt auch als schwacher partieller 5-HT1A-Rezeptor-Antagonist (Ki = 33 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 13523-86-9
Sample solution is provided at 25 µL, 10mM.
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Pindolol is an antagonist of β1- and β2-adrenergic receptors (β1- and β2-ARs; Kis = 2.6 and 4.8 nM, respectively) and a partial agonist of the β3-AR, stimulating adenylyl cyclase in membranes of cells expressing the human receptor.[1],[2] It is also an antagonist of the serotonin 5-HT1A receptor (Ki = 81.1 nM for inhibition of 5-HT-stimulated GTPγS binding).[3] Pindolol inhibits isoproterenol-induced tachycardia in anesthetized cats (ED50 = 1.8 µg/kg).[4] It also decreases mean blood pressure in conscious spontaneously hypertensive rats when administered at a dose of 30 mg/kg per day, but concomitantly increases heart rate.[5] Formulations containing pindolol have been used in the treatment of hypertension.
Reference
[1]. Hicks, P.E., Cavero, I., Manoury, P., et al. Comparative analysis of beta-1 adrenoceptor agonist and antagonist potency and selectivity of cicloprolol, xamoterol and pindolol. J. Pharmacol. Exp. Ther. 242(3), 1025-1034 (1987).
[2]. Hoffmann, C., Leitz, M.R., Oberdorf-Maass, S., et al. Comparative pharmacology of human β-adrenergic receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch. Pharmacol. 369(2), 151-159 (2004).
[3]. Krushinski, J.H., Jr., Schaus, J.M., Thompson, D.C., et al. Indoloxypropanolamine analogues as 5-HT1A receptor antagonists. Bioorg. Med. Chem. Lett. 17(20), 5600-5604 (2007).
[4]. Lubawski, I., and Wale, J. Studies with LB 46, a new β-receptor blocking drug. Eur. J. Pharmacol. 6(3), 345-348 (1969).
[5]. Antonaccio, M.J., High, J., DeForrest, J.M., et al. Antihypertensive effects of 12 beta adrenoceptor antagonists in conscious spontaneously hypertensive rats: Relationship to changes in plasma renin activity, heart rate and sympathetic nerve function. J. Pharmacol. Exp. Ther. 238(1), 378-387 (1986).
| Cas No. | 13523-86-9 | SDF | |
| Überlieferungen | DL-Pindolol | ||
| Chemical Name | (R)-1-((1H-indol-4-yl)oxy)-3-(isopropylamino)propan-2-ol | ||
| Canonical SMILES | O[C@@H](COC1=C2C(NC=C2)=CC=C1)CNC(C)C | ||
| Formula | C14H20N2O2 | M.Wt | 248.32 |
| Löslichkeit | 15 mg/ml in DMF, 15 mg/ml in DMSO, 5 mg/ml in Ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.0271 mL | 20.1353 mL | 40.2706 mL |
| 5 mM | 805.4 μL | 4.0271 mL | 8.0541 mL |
| 10 mM | 402.7 μL | 2.0135 mL | 4.0271 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)