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terguride is an approved drug
Compound class: Synthetic organic
Comment: Terguride is an ergoline type serotonin receptor antagonist/dopamine receptor agonist.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|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.|