Terguride

Terguride

Systematic (IUPAC) name
N,N-diethyl-N'-[(8α)-6-methylergolin-8-yl]urea
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	℞ (Prescription only)
Routes of administration	Oral
Identifiers
CAS Number	37686-84-3
ATC code	G02CB06 (WHO)
PubChem	CID: 443951
IUPHAR/BPS	56
ChemSpider	392004
UNII	21OJT43Q88 Y
KEGG	D01348 Y
Chemical data
Formula	C20H28N4O
Molecular mass	340.46 g/mol
SMILES CCN(CC)C(=O)N[C@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(C1)C
InChI InChI=1S/C20H28N4O/c1-4-24(5-2)20(25)22-14-10-16-15-7-6-8-17-19(15)13(11-21-17)9-18(16)23(3)12-14/h6-8,11,14,16,18,21H,4-5,9-10,12H2,1-3H3,(H,22,25)/t14-,16+,18+/m0/s1 Key:JOAHPSVPXZTVEP-YXJHDRRASA-N
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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.

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