Pindolol powder is a non-selective beta-adrenergic antagonist (beta-blocker) which possesses intrinsic sympathomimetic activity (ISA) in therapeutic dosage ranges but does not possess quinidine-like membrane stabilizing activity. Pindolol impairs AV node conduction and decreases sinus rate and may also increase plasma triglycerides and decrease HDL-cholesterol levels. Pindolol is nonpolar and hydrophobic, with low to moderate lipid solubility. Pindolol has little to no intrinsic sympathomimetic activity and, unlike some other beta-adrenergic blocking agents, pindolol has little direct myocardial depressant activity and does not have an anesthetic-like membrane-stabilizing action
02 Pindolol powder (13523-86-9) video
03 Pindolol powder (13523-86-9) Base Information
|Synonyms||Indapamide, Noranat, Fludex, Natrilix, Tertensif|
|Molecular Weight||365.8345 g/mol|
|Melting Point||168 – 172°C|
|Appearance||White to Off-White Solid|
|Solubility||Soluble in DMSO, not in water|
|Storage Condition||Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).|
|Application||Mixed β-adrenergic blocker and serotonin 5HT1A-receptor antagonist. Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.|
04 Pindolol powder General Description
Pindolol powder is a moderately lipophilic beta blocker.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. Pindolol is a SR-1A/SR-1B antagonist with similar affinity for each subtype. Pindolol acts as a partial agonist at mouse and human β3-AR (β3-adrenoceptors). Pindolol is an inhibitor of β1-AR.Pindolol is an aryloxypropanolamine derivative with antihypertensive property. Pindolol competitively binds to beta-adrenergic receptors, resulting in a decrease in beta-adrenergic activities In addition, this agent blocks serotonin (5-HT) 1A receptors, thereby increasing the available serotonin in the brain. Increased serotonin levels augment the antidepressant action of selective serotonin reuptake inhibitors and monoamine oxidase inhibitors.
05 Pindolol powder (13523-86-9) History
Pindolol powder has been investigated as an add-on drug to antidepressant therapy with SSRIs like fluoxetine in the treatment of depression since 1994. The rationale behind this strategy has its basis in the fact that pindolol is an antagonist of the serotonin 5-HT1A receptor.Presynaptic and somatodendritic 5-HT1A receptors act as inhibitory autoreceptors, inhibit serotonin release, and are pro-depressive in their action.
06 Pindolol (13523-86-9) Mechanism Of Action
Pindolol is a beta-adrenoceptor antagonist equally effective on beta 1- and beta 2-adrenoceptors which has a relatively long duration of action. It is practically completely absorbed and, unlike most other beta-adrenoceptor blockers, is only metabolized to a small extent during the first passage through the liver. Pindolol possesses partial agonist activity (intrinsic sympathomimetic activity, ISA). This means that apart from blocking beta-adrenoceptors it produces some stimulation. Pindolol therefore only slightly influences normal sympathetic drive at rest but effectively reduces the effects of elevated sympathetic activity. Various therapeutic advantages have been attributed to the partial agonist activity of pindolol: no or only slight alterations in normal cardiac output, heart rate and peripheral blood flow occur. Peripheral resistance is reduced during chronic oral therapy. No alteration of HDL/LDL cholesterol ratio has been observed. Rebound phenomena on sudden withdrawal of therapy and bronchoconstriction in susceptible patients are less likely than with drugs devoid of ISA
07 Pindolol (13523-86-9) Application
Pindolol 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.
Pindolol is a SR-1A/SR-1B antagonist with similar affinity for each subtype. Pindolol acts as a partial agonist at mouse and human β3-AR (β3-adrenoceptors). Pindolol is an inhibitor of β1-AR.
08 Pindolol (13523-86-9) More research
Pindolol is also an antagonist of the serotonin 5-HT1A receptor (Ki = 81.1 nM for inhibition of 5-HT-stimulated GTPgammaS binding). Pindolol inhibits isoproterenol-induced tachycardia in anesthetized cats (ED50 = 1.8 µg/kg). 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. Formulations containing pindolol have been used in the treatment of hypertension.Pindolol non-selectively blocks beta-1 adrenergic receptors mainly in the heart, inhibiting the effects of epinephrine and norepinephrine resulting in a decrease in heart rate and blood pressure. By binding beta-2 receptors in the juxtaglomerular apparatus, Pindolol inhibits the production of renin, thereby inhibiting angiotensin II and aldosterone production and therefore inhibits the vasoconstriction and water retention due to angiotensin II and aldosterone, respectively.
09 Pindolol (13523-86-9) Document Download
10 Pindolol (13523-86-9) Reference
1: Liu Y, Zhou X, Zhu D, Chen J, Qin B, Zhang Y, Wang X, Yang D, Meng H, Luo Q, Xie P. Is pindolol augmentation effective in depressed patients resistant to selective serotonin reuptake inhibitors? A systematic review and meta-analysis. Hum Psychopharmacol. 2015 May;30(3):132-42. doi: 10.1002/hup.2465. Epub 2015 Feb Review. PubMed PMID: 25689398.
2: Cumba LR, Smith JP, Brownson DA, Iniesta J, Metters JP, do Carmo DR, Banks CE. Electroanalytical detection of pindolol: comparison of unmodified and reduced graphene oxide modified screen-printed graphite electrodes. Analyst. 2015 Mar 7;140(5):1543-50. doi: 10.1039/c4an02005g. Epub 2015 Jan 22. PubMed PMID: 25610919.
3: Sassano-Higgins SA, Pato MT. Pindolol augmentation of selective serotonin reuptake inhibitors and clomipramine for the treatment of obsessive-compulsive disorder: A meta-analysis. J Pharmacol Pharmacother. 2015 Jan-Mar;6(1):36-8. doi: 10.4103/0976-500X.149144. PubMed PMID: 25709352; PubMed Central PMCID: PMC4319248.
4: Kim K, Cho E, Choi JM, Kim H, Jang A, Choi Y, Lee IS, Yu JH, Jung S. Intermolecular complexation of low-molecular-weight succinoglycans directs solubility enhancement of pindolol. Carbohydr Polym. 2014 Jun 15;106:101-8. doi: 10.1016/j.carbpol.2014.02.017. Epub 2014 Feb 15. PubMed PMID: 24721056.
- 01. Overview
- 02. Pindolol powder (13523-86-9) video
- 03. Pindolol powder (13523-86-9) Base Information
- 04. Pindolol powder General Description
- 05. Pindolol powder (13523-86-9) History
- 06. Pindolol (13523-86-9) Mechanism Of Action
- 07. Pindolol (13523-86-9) Application
- 08. Pindolol (13523-86-9) More research
- 09. Pindolol (13523-86-9) Document Download
- 10. Pindolol (13523-86-9) Reference