Terguride
Also called Dironyl, Teluron, trans-Dihydrolisuride
Overview
Terguride (INN (International Nonproprietary Name), JAN (Japanese Accepted Name)), sold under the brand name Teluron, is a serotonin receptor antagonist and dopamine receptor agonist of the ergoline family. It is approved for and used as a prolactin inhibitor in the treatment of hyperprolactinemia (high prolactin levels) in Japan. Terguride is taken by mouth.[1]
Pharmacology
Pharmacodynamics
Terguride acts as an agonist of the dopamine D₂ receptor and as an antagonist of the serotonin 5-HT2A and 5-HT2B receptors, among other actions. WP⚠ Wikipedia itself has flagged this text: citation needed.
As an antagonist of the 5-HT2B receptor, terguride is not associated with cardiac valvulopathy.[3] WP⚠ A table follows this text in the source and is not copied here. Open the source to see it.
Research
Research
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. However, development was discontinued in 2011.[4]
Chemistry
- Formula
- C20H28N4O PC
- CAS number
- 37686-84-3 PC
- Molar mass (g/mol)
- 340.5 PC
- IUPAC name (computed by PubChem)
- 3-
[(6aR, PC9S, 10aR) - 7- methyl- 6, 6a, 8, 9, 10, 10a- hexahydro- 4H- indolo[4, 3- fg] quinolin- 9- yl] - 1, 1- diethylurea - SMILES
- CCN(CC)
C(=O) PCN[C@H] 1C[C@H] 2[C@@H] (CC3=CNC4=CC=CC2=C34) N(C1) C - InChIKey
- JOAHPSVPXZTVEP-
YXJHDRRASA- PCN - PubChem CID
- 443951
Harm reduction information
No harm reduction data is on file for this compound yet. That means no dose, timing or combination data from PsychonautWiki or TripSit. Please don't guess a dose from similar compounds. If you have taken it and feel unwell, contact emergency services or a poison control center.
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Sources
- Other List of 5HT3 receptor antagonists (5hydroxytryptamine receptor antagonists)
- Journal / agency Terguride - AdisInsight
- Journal / agency Zajdel P, Bednarski M, Sapa J, Nowak G. Ergotamine and nicergoline - facts and myths. Pharmacol Rep. April 2015. doi:10.1016/j.pharep.2014.10.010 · PMID 25712664
- Journal / agency 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. doi:10.1155/2015/438403 · PMID 25667920 · PMC4312574
- Other Presseportal (Swiss press portal, in German)
- Other TheDay.com 5/10/2010
Text and values on this page are quoted from Wikipedia (CC BY-SA 4.0), PubChem (public domain). Each value links to the exact revision it came from.