The FDA-approved drug Losartan is used to treat high blood pressure. By preventing the blood vessels from narrowing, Losartan improves blood flow reducing hypertension. Losartan is also used to reduce kidney damage in type 2 diabetes patients with high blood pressure. Losartan is now considered an attractive therapeutical solution to prevent epilepsy associated with vascular injury.


Losartan belongs to a group of drugs called Angiotensin II Receptor Antagonists, aka Angiotensin Receptor Blockers (ARBs), AT 1-receptor antagonists or sartans.

IHC of AGTR1 in mouse kidney tissue with AGTR1 antibody GTX31793 Genetex - tebu-bio

IHC of mouse kidney tissue with AGTR1 antibody (Genetex).

Bar-Klien et al. have demonstrated that Losartan is a potent preventive agent against epilepsy in brain cellular populations following vascular injury and brain exposure to albumin.

The authors identified the molecular mechanisms of this effect. They came to the conclusion that AT-1-receptor antagonist indeed blocks the TGF-beta signalling pathway in the brain.

Sartan-related active molecules

  • Losartan potassium (CAS: 124750-99-8): Losartan is the potassium salt form of Losartan. Losartan is an Angiotensin II antagonist with antihypertensive activity that selectively  blocks the binding of Angiotensin II to the Angiotensin I (AT1) Receptor.
  • Valsartan (Angiotensin antagonist; CAS: 137862-53-4) is a high affinity and highly selective angiotensin AT1 receptor antagonist (Ki = 2.38 nM). Valsartan normalizes the increased production of inflammatory cytokines in adipose and liver tissue in LPS-infused mice. Valsartan is a clinically useful antihypertensive agent.

Source:

Human Cardiac Fibroblasts

Human Cardiac Fibroblasts (HCF) as primary cells for in vitro cell-based assays.

  • Bar-Klein, Guy et al. “Losartan Prevents Acquired Epilepsy via TGF-beta
    Signaling Suppression.” Annals of neurology 75.6 (2014): 864–875. PMC. Web. 17 Nov. 2015.

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Philippe Fixe, PhD
Written by Philippe Fixe, PhD
Philippe Fixe is a former Marketing Manager at tebu-bio, passionate about innovation and R&D in Life sciences, Biotechnology, Medical research, Drug discovery, and also a keen photographer.