Trequinsin hydrochloride

Biological Activity

Trequinsin hydrochloride is a highly potent inhibitor of cGMP-inhibited phosphodiesterase (PDE3; IC₅₀ = 250 pM). Potently inhibits arachidonic acid-induced aggregation of human platelets (IC₅₀ = 50 pM). Orally active antihypertensive agent; reduces systemic blood pressure in both normotensive and hypertensive animal models. Also activates CatSper channels, increases intracellular Ca²⁺ and cGMP levels, and decreases potassium channel activity in sperm.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. HL 725, an extremely potent inhibitor of platelet phosphodiesterase and induced platelet aggregation in vitro.
   Ruppert and Weithmann
   Life Sci., 1982;31:2037
2. Trequinsin, a potent new antihypertensive vasodilator in the series of 2-(arylimino)-3-alkyl-9,10-dimethoxy-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-ones.
   Lal et al.
   J.Med.Chem., 1984;27:1470
3. Role of plasma adenosine in the antiplatelet action of HL 725, a potent inhibitor of cAMP phosphodiesterase: species differences.
   Agarwal et al.
   Thromb.Res., 1987;47:191
4. Novel pharmacological actions of Trequinsin Hydrochloride improve human sperm cell motility and function.
   McBrinn et al.
   Br.J.Pharmacol., 2019;

Product Datasheets