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Terguride

Chemical compound

Chemical compound

| Drugs.com =

| elimination_half-life =

Terguride (, ), 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.

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.

As an antagonist of the 5-HT2B receptor, terguride is not associated with cardiac valvulopathy.

SiteAffinity (Ki [nM])Efficacy (Emax [%])Action
D128??
D2S0.8139Partial agonist
D2L1.10Silent antagonist
D31.036Partial agonist
D48.10Silent antagonist
D523??
5-HT1A3.571Partial agonist
5-HT1B25737Partial agonist
5-HT1D1662Partial agonist
5-HT2A4.849Partial agonist
5-HT2B7.10Silent antagonist
5-HT2C480Silent antagonist
5-HT78–42??
α1A3.50Silent antagonist
α1B35??
α1D3.9??
α2A0.300Silent antagonist
α2B0.450Silent antagonist
α2C0.760Silent antagonist
α2D1.5??
β1661??
β220??
H1339??
M110,000??
Notes: All receptors are human except α2D-adrenergic, which is rat (no human counterpart), and 5-HT7, which was guinea pig.

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.

References

References

  1. "List of 5HT3 receptor antagonists (5hydroxytryptamine receptor antagonists)".
  2. "Terguride - AdisInsight".
  3. (April 2015). "Ergotamine and nicergoline - facts and myths". Pharmacol Rep.
  4. (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes". J Pharmacol Exp Ther.
  5. (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor". J Pharmacol Exp Ther.
  6. (November 2002). "Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. III. Agonist and antagonist properties at serotonin, 5-HT(1) and 5-HT(2), receptor subtypes". J Pharmacol Exp Ther.
  7. "PDSP Database - UNC".
  8. (2015). "5-HT2B receptor antagonists inhibit fibrosis and protect from RV heart failure". BioMed Research International.
  9. [http://www.presseportal.ch/de/pm/100015139/100561578/ergonex_pharma_gmbh Presseportal (Swiss press portal, in German)]
  10. "TheDay.com 5/10/2010".
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alpha-1-blockers alpha-2-blockers d2-receptor-agonists d2-antagonists d3-receptor-agonists d4-antagonists dopamine-receptor-modulators ergolines orphan-drugs prolactin-inhibitors serotonin-receptor-antagonists serotonin-receptor-agonists ureas
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