Propranolol

Propranolol (CAS No. 525-66-6) is a non-selective β-adrenergic receptor (β?/β?) blocker. Its core bioactivities involve cardiovascular regulation, anti-tremor effects, modulation of emotional memory, and metabolic improvement. Its targets include β?/β? receptors (β1AR and β2AR) in the myocardium and peripheral tissues. It can also modulate GABAergic outflow and cortical excitability via central noradrenergic pathways, inhibit hormone-sensitive lipase (HSL) activity in adipose tissue, and downregulate the inflammatory factor IL-6. Commonly used application concentrations: in vitro cell experiments (cortical excitability assessment) are designed around clinically equivalent doses; in animal experiments, oral doses of 40~80 mg/kg are used in emotional memory studies, and an initial dose of 10 mg per administration, four times daily (adjusted as needed), is used in burn models. Clinically effective therapeutic concentrations correspond to scenario-specific dosing: for hypertension, the initial oral dose is 40 mg/day, which can be doubled every 2 weeks, with a maximum dose up to 960 mg/day; when combined with diuretics, the average dose is 320~480 mg/day. For essential tremor, the median dose is 80 mg/day (IQR 50~80 mg/day). In emotional memory modulation experiments, 40~80 mg per administration is commonly used (memory tasks are performed 60~90 minutes after dosing). For burn patients, treatment is initiated at 10 mg per administration, four times daily, with dose adjustments targeting a heart rate ＜ 100 bpm, which can improve insulin sensitivity and reduce pro-inflammatory fatty acid levels.

References:

[1] Ahlquist RP. Propranolol in hypertension. J Clin Pharmacol. 1977 Feb-Mar;17(2-3):93-4. doi: 10.1002/j.1552-4604.1977.tb04594.x. PMID: 13091.

[2] Lonergan MH, Olivera-Figueroa LA, Pitman RK, Brunet A. Propranolol's effects on the consolidation and reconsolidation of long-term emotional memory in healthy participants: a meta-analysis. J Psychiatry Neurosci. 2013 Jul;38(4):222-31. doi: 10.1503/jpn.120111. PMID: 23182304; PMCID: PMC3692719.

[3] Rehou S, de Brito Monteiro L, Auger C, Knuth CM, Abdullahi A, Stanojcic M, Jeschke MG. Propranolol Normalizes Metabolomic Signatures Thereby Improving Outcomes After Burn. Ann Surg. 2023 Oct 1;278(4):519-529. doi: 10.1097/SLA.0000000000005973. Epub 2023 Jun 30. PMID: 37389480.

[4] Vogelnik ?akelj K, Prezelj N, Gregori? Kramberger M, Kojovi? M. Mechanisms of tremor-modulating effects of primidone and propranolol in essential tremor. Parkinsonism Relat Disord. 2024 Nov;128:107151. doi: 10.1016/j.parkreldis.2024.107151. Epub 2024 Sep 14. PMID: 39321734.