Ligand id: 56

Name: terguride

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 2
Rotatable bonds 5
Topological polar surface area 47.61
Molecular weight 340.23
XLogP 2.52
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Full marketing authorisation in Japan only.
The EMA has granted orphan designation for the tretament of pulmonary arterial hypertension (PAH) and chronic thromboembolic pulmonary hypertension, and systemic sclerosis.
Mechanism Of Action and Pharmacodynamic Effects
Terguride is a serotonin receptor antagonist, with highest affinity for 5-HT2B and 5-HT2A receptor subtypes. In the treatment of PAH, terguride binds to serotonin receptors in blood vessel walls and inhibits its actions on the smooth muscle cells. Thus counter-acts PAH. The MMOA in systemic sclerosis appears to involve inhibition of the serotonin-induced abnormal growth of fibrous connective tissue associated with this disease.