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Pindolol (Synonyms: DL-Pindolol)

Catalog No.GC17734 Copy One-Click Copy Product Info

β-adrenoceptor antagonist with partial agonist activity

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Pindolol Chemical Structure

Cas No.: 13523-86-9

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50mg
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100mg
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250mg
$187.00
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500mg
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Sample solution is provided at 25 µL, 10mM.



Description of Pindolol

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).

Chemical Properties of Pindolol

Cas No. 13523-86-9 SDF
Synonyms 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
Solubility 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Pindolol

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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
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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