Losartan (potassium salt)

Losartan is an antagonist of angiotensin II type 1b (AT_1b) receptor (IC₅₀ = 2.2 nM in COS-7 cells expressing the rat receptor).¹ It reduces U-46619-induced aggregation of platelets in isolated human platelet-rich plasma when used at a concentration of 5 µM.² It decreases 1-lipoxygenase (1-LO) levels in the endothelial layer of autologous vein grafts in rabbits fed a high-cholesterol diet when administered at a dose of 10 mg/kg per day.³ Losartan (15 mg/kg per day) decreases systolic blood pressure in a ouabain-induced mouse model of hypertension.⁴ It also increases the mechanical pain threshold in the von Frey test in a paclitaxel-induced rat model of neuropathic pain when administered at a dose of 50 mg/kg twice per day.⁵ Formulations containing losartan have been used in the treatment of hypertension and diabetic nephropathy.

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1. Ji, H., Leung, M., Zhang, Y., et al. Differential structural requirements for specific binding of nonpeptide and peptide antagonists to the AT₁ angiotensin receptor. Identification of amino acid residues that determine binding of the antihypertensive drug losartan. The Journal of Biological Chemisty 269(24), 16533-16536 (1994).

2. Núñez, A., Gómez, J., Zalba, L.R., et al. Losartan inhibits in vitro platelet activation: Comparison with candesartan and valsartan. J. Renin Angiotensin Aldosterone Syst. 1(2), 175-179 (2000).

3. Ge, J., Huang, D., Liang, C., et al. Upregulation of lectinlike oxidized low-density lipoprotein receptor-1 expression contributes to the vein graft atherosclerosis: Modulation by losartan. Atherosclerosis 177(2), 263-268 (2004).

4. Xavier, F.E., Rossoni, L.V., Alonso, M.J., et al. Ouabain-induced hypertension alters the participation of enothelial factors in α-adrenergic responses differently in rat resistance and conductance mesenteric arteries. Br. J. Pharmacol. 143(1), 215-225 (2004).

5. Kim, E., Hwang, S.-H., Kim, H.-K., et al. Losartan, an angiotensin II type 1 receptor antagonist, alleviates mechanical hyperalgesia in a rat model of chemotherapy-induced neuropathic pain by inhibiting inflammatory cytokines in the dorsal root ganglia. Mol. Neurobiol. 56(11), 7408-7419 (2019).