Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT

Product Name : hydrochloride Catalog Number : T0812 CAS Number : 318-98-9 Molecular Formula : C16H22ClNO2 Molecular Weight : 295.81 Apprearence : Solid Melting Point : 163-165°C

Description: Propranolol hydrochloride is a widely used non-cardioselective beta- antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.

Storage: 2 years -80°C in solvent; 3 years -20°C powder;

DMSO 55 mg/mL (185.9 mM) Water 6 mg/mL (20.28 mM) Solubility Ethanol <1 mg/mL ( < 1 mg/ml refers to the product slightly soluble or insoluble )

Receptor (IC50) β- 12nM

In vitro Activity In cultured endothelial or tumor cells, propranolol has been shown to both reduce cAMP levels and simultaneously activate the mitogen-activated protein kinase (MAPK) pathway downstream of βAR inhibition[2]. It displays high affinity for 5-HT1B receptors (Ki= 17 nM), and milder affinity for 5HT1D receptors (Ki= 10.2 μM)[3]. In vivo Activity Chronic administration of propranolol increased the beta(1)-adrenoceptors but decreased the beta(2)-adrenoceptors without changing total amount of plasma membrane beta-adrenoceptors[4]. Animal Experiment Animal Model: Male Wistar rats

Reference 1. Briley M , Cavero I , Langer S Z , et al. EVIDENCE AGAINST β-ADRENOCEPTOR BLOCKING ACTIVITY OF , A DRUG WITH CALCIUM ANTAGONIST PROPERTIES[J]. British Journal of Pharmacology, 1980, 69(4):669-673. 2. Munabi NC, et al. Propranolol Targets Hemangioma Stem Cells via cAMP and Mitogen-Activated Protein Kinase Regulation. Stem Cells Transl Med. 2016 Jan;5(1):45-55. 3. Glennon RA, et al. The binding of propranolol at 5-hydroxytryptamine1D beta T355N mutant receptors may involve formation of two hydrogen bonds to asparagine. Mol Pharmacol. 1996 Jan;49(1):198-206. 4. Horinouchi T, et al. Different changes of plasma membrane beta-adrenoceptors in rat heart after chronic administrationof propranolol, and bevantolol. Life Sci. 2007 Jul 12;81(5):399-404. Epub 2007 Jun 16. 4. Horinouchi T, et al. Different changes of plasma membrane beta-adrenoceptors in rat heart after chronic administrationof propranolol, atenolol and bevantolol. Life Sci. 2007 Jul 12;81(5):399-40 Epub 2007 Jun 16. 5. Al-Majed AA, et al. Propranolol. Profiles Drug Subst Excip Relat Methodol. 2017;42:287-338.

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