Terguride

Terguride
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
ATC code	G02CB06 (WHO) ;
Legal status
Legal status	In general: ℞ (Prescription only);
Identifiers
	IUPAC name N,N-diethyl-N'-[(8α)-6-methylergolin-8-yl]urea;
CAS Number	37686-84-3;
PubChem CID	443951;
IUPHAR/BPS	56;
UNII	21OJT43Q88;
KEGG	D01348 ;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C20H28N4O
Molar mass	340.46 g/mol
3D model (JSmol)	Interactive image;
	SMILES CCN(CC)C(=O)N[C@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(C1)C;
(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

↑ 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
↑ Presseportal (Swiss press portal, in German)
↑ TheDay.com 5/10/2010

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[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

[1]

[2]

[3]

Clinical data

AHFS/Drugs.com	International Drug Names
Routes of administration	Oral
ATC code	G02CB06 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Identifiers
IUPAC name N,N-diethyl-N'-[(8α)-6-methylergolin-8-yl]urea
CAS Number	37686-84-3
PubChem CID	443951
IUPHAR/BPS	56
UNII	21OJT43Q88
KEGG	D01348^Y
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C₂₀H₂₈N₄O
Molar mass	340.46 g/mol
3D model (JSmol)	Interactive image
SMILES CCN(CC)C(=O)N[C@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(C1)C
(verify)

Terguride

References

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