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Open Access Articles- Top Results for Terguride

Terguride

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Terguride
File:Terguride.png
Systematic (IUPAC) name
N,N-diethyl-N'-[(8α)-6-methylergolin-8-yl]urea
Clinical data
AHFS/Drugs.com International Drug Names
  • (Prescription only)
Oral
Identifiers
37686-84-3
G02CB06
PubChem CID 443951
IUPHAR ligand 56
UNII 21OJT43Q88 7pxY
KEGG D01348 7pxY
Chemical data
Formula C20H28N4O
340.46 g/mol
 14pxY (what is this?)  (verify)

Terguride (INN) is a serotonin antagonist. It is used for the treatment of hyperprolactinemia. Terguride is an oral, potent antagonist of 5-HT2B and 5-HT2A (serotonin) receptors. Serotonin stimulates the proliferation of pulmonary artery smooth muscle cells, and induces fibrosis in the wall of pulmonary arteries. Together, this causes vascular remodeling and narrowing of the pulmonary arteries. These changes result in increased vascular resistance and PAH. Due to the potential anti-proliferative and anti-fibrotic activity of terguride, this potential medicine could offer the hope of achieving reversal of pulmonary artery vascular remodeling and attenuation of disease progression.[1]

In May 2008, terguride was granted orphan drug status for the treatment of pulmonary arterial hypertension.[2] In May 2010 Pfizer purchased world-wide rights for the drug.[3]


References

  1. ^ Janssen W, Schymura Y, Novoyatleva T, Kojonazarov B, Boehm M, Wietelmann A, Luitel H, Murmann K, Krompiec DR, Tretyn A, Pullamsetti SS, Weissmann N, Seeger W, Ghofrani HA, Schermuly RT. 5-HT2B Receptor Antagonists Inhibit Fibrosis and Protect from RV Heart Failure. Biomed Research International. 2015;2015:438403. doi 10.1155/2015/438403 PMID 25667920
  2. ^ Presseportal (Swiss press portal, in German)
  3. ^ TheDay.com 5/10/2010



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