Lidanserin

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Lidanserin (INN; ZK-33,839) is a serotonergic and adrenergic receptor antagonist developed for the treatment of hypertension. It acts as a dual antagonist at the 5-HT2A and α1-adrenergic receptors, making it pharmacologically similar to ketanserin.

Pharmacology[edit | edit source]

Lidanserin exerts its effects by blocking key receptors involved in vasoconstriction and platelet aggregation, leading to vasodilation and blood pressure reduction. Its primary actions include:

  • 5-HT2A receptor antagonism – Reduces vascular smooth muscle contraction, preventing serotonin-induced vasoconstriction.
  • α1-adrenergic receptor antagonism – Lowers peripheral vascular resistance by inhibiting norepinephrine-induced vasoconstriction.

These mechanisms suggest its potential as an antihypertensive agent, but it was never marketed.

Potential Clinical Uses[edit | edit source]

Although not commercially available, Lidanserin was investigated for:

  • Hypertension – As a vasodilator to lower blood pressure.
  • Thrombosis prevention – Due to its anti-platelet effects.
  • Vascular disorders – Such as Raynaud’s phenomenon and migraine prophylaxis, owing to its serotonergic modulation.

Comparison to Ketanserin[edit | edit source]

Lidanserin shares pharmacological similarities with ketanserin, another 5-HT2A and α1-adrenergic antagonist, which was approved for hypertension treatment in some regions. However, Lidanserin never progressed beyond clinical trials.

Chemical Structure[edit | edit source]

Lidanserin belongs to several chemical classes:

  • Piperidine derivatives – Contributing to receptor binding affinity.
  • Pyrrolidone structure – Involved in metabolic stability.
  • Organofluoride compounds – Modifying lipophilicity and receptor interactions.

See also[edit | edit source]

Antihypertensive agents



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