Terguride

Terguride

Clinical data
AHFS/Drugs.com	International Drug Names
Routes of administration	Oral
ATC code	G02CB06 (WHO)
Legal status
Legal status	℞ (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
ChemSpider	392004
UNII	21OJT43Q88 Y
KEGG	D01348 Y
ECHA InfoCard	100.048.732
Chemical and physical data
Formula	C20H28N4O
Molar mass	340.46 g/mol
3D model (Jmol)	Interactive image
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
(verify)

Terguride (INN), also known as trans-dihydrolisuride, is a serotonin receptor antagonist and dopamine receptor agonist of the ergoline family. It is approved for and used in 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 worldwide rights for the drug.