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Pindolol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pindolol图片
CAS NO:13523-86-9
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
Pindolol (LB-46) 是一种非选择性 β-受体阻滞剂,具有部分 β-肾上腺素能受体激动剂活性,也可用作 5-HT1A 受体弱部分拮抗剂 (Ki=33nM)。
Cas No.13523-86-9
别名吲哚洛尔; LB-46
化学名(R)-1-((1H-indol-4-yl)oxy)-3-(isopropylamino)propan-2-ol
Canonical SMILESO[C@@H](COC1=C2C(NC=C2)=CC=C1)CNC(C)C
分子式C14H20N2O2
分子量248.32
溶解度15 mg/ml in DMF, 15 mg/ml in DMSO, 5 mg/ml in Ethanol
储存条件Store at -80℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).