Terguride

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title: "Terguride" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["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"] description: "Chemical compound" topic_path: "general/alpha-1-blockers" source: "https://en.wikipedia.org/wiki/Terguride" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0

::summary Chemical compound ::

| verifiedrevid = 437134889 | IUPAC_name = 3-[(6aR,9S,10aR)-7-methyl-6,6a,8,9,10,10a-hexahydro-4H-indolo[4,3-fg]quinolin-9-yl]-1,1-diethylurea | image = Terguride.png | image_class = skin-invert-image | width = 200px | image2 = Terguride 3D.png | image_class2 = bg-transparent | width2 = 200px

| tradename = Teluron | Drugs.com = | pregnancy_category = | legal_status = Rx-only | routes_of_administration = Oral

| bioavailability = | metabolism = | elimination_half-life = | excretion =

| CAS_number = 37686-84-3 | ATC_prefix = G02 | ATC_suffix = CB06 | PubChem = 443951 | ChemSpiderID = 392004 | IUPHAR_ligand = 56 | DrugBank_Ref = | DrugBank = DB13399 | UNII_Ref = | UNII = 21OJT43Q88 | KEGG_Ref = | KEGG = D01348 | synonyms = Dironyl; Mysalfon; trans-Dihydrolisuride; Transdihydrolisuride; TDHL; SH-406; VUFB-6638; ZK-31224; N,N-Diethyl-N'-[(8α)-6-methylergolin-8-yl]urea

| C=20 | H=28 | N=4 | O=1 | StdInChI = 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 | StdInChIKey = JOAHPSVPXZTVEP-YXJHDRRASA-N | SMILES = CCN(CC)C(=O)N[C@H]1C[C@H]2C@@HN(C1)C

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.

::data[format=table title="{{Nowrap|Activities of terguride at various sites{{cite journal | vauthors = Millan MJ, Maiofiss L, Cussac D, Audinot V, Boutin JA, Newman-Tancredi A | title = 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 | journal = J Pharmacol Exp Ther | volume = 303 | issue = 2 | pages = 791–804 | date = November 2002 | pmid = 12388666 | doi = 10.1124/jpet.102.039867 | s2cid = 6200455 | url = }}{{cite journal | vauthors = Newman-Tancredi A, Cussac D, Audinot V, Nicolas JP, De Ceuninck F, Boutin JA, Millan MJ | title = 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 | journal = J Pharmacol Exp Ther | volume = 303 | issue = 2 | pages = 805–14 | date = November 2002 | pmid = 12388667 | doi = 10.1124/jpet.102.039875 | s2cid = 35238120 | url = }}{{cite journal | vauthors = Newman-Tancredi A, Cussac D, Quentric Y, Touzard M, Verrièle L, Carpentier N, Millan MJ | title = 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 | journal = J Pharmacol Exp Ther | volume = 303 | issue = 2 | pages = 815–22 | date = November 2002 | pmid = 12388668 | doi = 10.1124/jpet.102.039883 | s2cid = 19260572 | url = }}{{cite web |url=https://pdsp.unc.edu/databases/pdsp.php?testFreeRadio=testFreeRadio&testLigand=Terguride&doQuery=Submit+Query |title=PDSP Database - UNC |website=pdsp.unc.edu |access-date=15 January 2022 |archive-url=https://web.archive.org/web/20210413033753/https://pdsp.unc.edu/databases/pdsp.php?testFreeRadio=testFreeRadio&testLigand=Terguride&doQuery=Submit+Query |archive-date=13 April 2021 }}}}"]

Site	Affinity (Ki [nM])	Efficacy (Emax [%])	Action
D1	28	?	?
D2S	0.81	39	Partial agonist
D2L	1.1	0	Silent antagonist
D3	1.0	36	Partial agonist
D4	8.1	0	Silent antagonist
D5	23	?	?
5-HT1A	3.5	71	Partial agonist
5-HT1B	257	37	Partial agonist
5-HT1D	16	62	Partial agonist
5-HT2A	4.8	49	Partial agonist
5-HT2B	7.1	0	Silent antagonist
5-HT2C	48	0	Silent antagonist
5-HT7	8–42	?	?
α1A	3.5	0	Silent antagonist
α1B	35	?	?
α1D	3.9	?	?
α2A	0.30	0	Silent antagonist
α2B	0.45	0	Silent antagonist
α2C	0.76	0	Silent antagonist
α2D	1.5	?	?
β1	661	?	?
β2	20	?	?
H1	339	?	?
M1	10,000	?	?
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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