TERGURIDE

Possibly Marketed Outside US

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C20H28N4O
Molecular Weight	340.4625
Optical Activity	UNSPECIFIED
Defined Stereocenters	3 / 3
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCN(CC)C(=O)N[C@H]1C[C@H]2[C@@H](CC3=CNC4=C3C2=CC=C4)N(C)C1

InChI

InChIKey=JOAHPSVPXZTVEP-YXJHDRRASA-N

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

HIDE SMILES / InChI

Molecular Formula	C20H28N4O
Molecular Weight	340.4625
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	3 / 3
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22049464
Curator's Comment: description was created based on several sources, including https://www.drugs.com/international/terguride.html | https://www.ncbi.nlm.nih.gov/pubmed/2571729 | https://www.ncbi.nlm.nih.gov/pubmed/11520375 | https://www.ncbi.nlm.nih.gov/pubmed/3127243

Terguride (INN), also known as trans-dihydrolisuride, is a serotonin receptor antagonist and dopamine receptor agonist of the ergoline family. Terguride 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.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Serotonin 1a (5-HT1a) receptor 177 Target ID: CHEMBL273 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2571729	Antagonist 2849	25.0 nM [IC50]
Dopamine D2 receptor 311 Target ID: CHEMBL339 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2571729	Antagonist 2849	4.0 nM [IC50]
Dopamine D1 receptor 106 Target ID: CHEMBL265 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2571729	Antagonist 2849	69.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hyperprolactinemia 4 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11520375	Primary		Approved 8583	Teluron Approved Use Unknown

C_max

Value	Dose	Analyte	Population
1.53 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	50 μg single, intravenous dose: 50 μg route of administration: Intravenous experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.38 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.4 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.42 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.64 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.31 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.95 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.82 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.51 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.64 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.93 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.03 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
2.28 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732377/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.28 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732377/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
1.12 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	50 μg single, intravenous dose: 50 μg route of administration: Intravenous experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
0.77 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.55 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.37 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.85 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.64 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.09 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.49 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.11 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
5.56 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.87 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.81 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
9.49 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732377/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9.49 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732377/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.78 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12704865/	1 mg 1 times / day unknown, oral dose: 1 mg route of administration: Oral experiment type: UNKNOWN co-administered:	TERGURIDE unknown	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
1.55 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	50 μg single, intravenous dose: 50 μg route of administration: Intravenous experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.06 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.78 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
2.07 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.27 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	250 μg 2 times / day multiple, oral dose: 250 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
0.74 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.62 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.34 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.05 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	500 μg 2 times / day multiple, oral dose: 500 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.73 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.61 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
1.32 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.49 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2373136/	750 μg 2 times / day multiple, oral dose: 750 μg route of administration: Oral experiment type: MULTIPLE co-administered:	TERGURIDE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: UNKNOWN
2.47 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732377/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.47 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/3732377/	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	TERGURIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
32% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/12704865/	1 mg 1 times / day unknown, oral dose: 1 mg route of administration: Oral experiment type: UNKNOWN co-administered:		TERGURIDE unknown	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
1.5 mg 2 times / day multiple, oral Highest studied dose Dose: 1.5 mg, 2 times / day Route: oral Route: multiple Dose: 1.5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/	Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (12.3%) Vomiting (6.2%) Dizziness (4.6%) Constipation (3.1%) Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/
1 mg single, oral Studied dose Dose: 1 mg Route: oral Route: single Dose: 1 mg Sources: https://pubmed.ncbi.nlm.nih.gov/3127243/	healthy Health Status: healthy Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/3127243/	Sources: https://pubmed.ncbi.nlm.nih.gov/3127243/

AEs

AE	Significance	Dose	Population
Nausea	12.3% Disc. AE	1.5 mg 2 times / day multiple, oral Highest studied dose Dose: 1.5 mg, 2 times / day Route: oral Route: multiple Dose: 1.5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/
Constipation	3.1% Disc. AE	1.5 mg 2 times / day multiple, oral Highest studied dose Dose: 1.5 mg, 2 times / day Route: oral Route: multiple Dose: 1.5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/
Dizziness	4.6% Disc. AE	1.5 mg 2 times / day multiple, oral Highest studied dose Dose: 1.5 mg, 2 times / day Route: oral Route: multiple Dose: 1.5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/
Vomiting	6.2% Disc. AE	1.5 mg 2 times / day multiple, oral Highest studied dose Dose: 1.5 mg, 2 times / day Route: oral Route: multiple Dose: 1.5 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/20039417/

PubMed

Title	Date	PubMed
The dopamine D(2) partial agonist and antagonist terguride decreases heroin self-administration on fixed- and progressive-ratio schedules.	2010-12	20705086
Increased expression of 5-hydroxytryptamine2A/B receptors in idiopathic pulmonary fibrosis: a rationale for therapeutic intervention.	2010-11	20671305
Development and application of an LC-MS/MS method for measuring the effect of (partial) agonists on cAMP accumulation in vitro.	2010-04-30	20122962
LSD but not lisuride disrupts prepulse inhibition in rats by activating the 5-HT(2A) receptor.	2010-02	19937319
Evaluation of the efficacy and safety of terguride in patients with fibromyalgia syndrome: results of a twelve-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study.	2010-01	20039417
Co-administration of the partial dopamine D2 agonist terguride with L-dopa attenuates L-dopa-induced locomotor sensitization in hemiparkinsonian mice.	2009-09-14	19463706
Dopamine receptor subtypes contribution to Homer1a induction: insights into antipsychotic molecular action.	2009-08-01	19243698
Recognition properties and competitive assays of a dual dopamine/serotonin selective molecularly imprinted polymer.	2008-12	19330079
Characterization of aripiprazole partial agonist activity at human dopamine D3 receptors.	2008-11-12	18831971
The effect of terguride in carbon tetrachloride-induced liver fibrosis in rat.	2008-11	18703754
Recruitment of beta-arrestin2 to the dopamine D2 receptor: insights into anti-psychotic and anti-parkinsonian drug receptor signaling.	2008-06	18455202
Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes.	2008-01	18066532
Effects of aripiprazole and terguride on dopamine synthesis in the dorsal striatum and medial prefrontal cortex of preweanling rats.	2008	17994191
[A case of ruptured internal carotid artery aneurysm mimicking pituitary apoplexy].	2007-12	18080517
Long-term serotonin effects in the rat are prevented by terguride.	2007-10-04	17391782
In vitro characterization of SLV308 (7-[4-methyl-1-piperazinyl]-2(3H)-benzoxazolone, monohydrochloride): a novel partial dopamine D2 and D3 receptor agonist and serotonin 5-HT1A receptor agonist.	2006-12-15	17001660
Pre- and postsynaptic actions of a partial D2 receptor agonist in reserpinized young rats: longevity of agonistic effects.	2006-12-08	17070785
Effects of terguride, ropinirole, and acetyl-L-carnitine on methamphetamine withdrawal in the rat.	2006-03	16647107
The partial dopamine D2-like receptor agonist terguride functions as an agonist in preweanling rats after a 5-day reserpine regimen.	2006-03	16447063
Effects of a partial D2-like receptor agonist on striatal dopamine autoreceptor functioning in preweanling rats.	2006-02-16	16427034
Aripiprazole's low intrinsic activities at human dopamine D2L and D2S receptors render it a unique antipsychotic.	2005-05-16	15894311
Influence of steric hindrance on enantioseparation of Dns-amino acids and pesticides on terguride based chiral selectors in capillary electrophoresis.	2005-05	15912739
Agonism at 5-HT2B receptors is not a class effect of the ergolines.	2005-04-25	15862804
The partial D2-like dopamine receptor agonist terguride acts as a functional antagonist in states of high and low dopaminergic tone: evidence from preweanling rats.	2005-04	15765258
Buprenorphine and a CRF1 antagonist block the acquisition of opiate withdrawal-induced conditioned place aversion in rats.	2005-01	15138444
In vitro antiplasmodial activities of semisynthetic N,N'-spacer-linked oligomeric ergolines.	2004-02-15	14759742
Effects of terguride treatment on glucose abnormalities induced by ischemic brain damage in SHR/N-cp lean Koletsky strain and in rats of Wistar strain.	2004	15658573
Pergolide, terguride and N,N'-spacer-linked oligomers of both interact with 5-HT2A receptors of rat tail artery.	2004	14984312
Management of restless legs syndrome by the partial D2-agonist terguride.	2003-09	14592288
Effects of a partial dopamine D2-like agonist on the cocaine-induced behavioral sensitization of preweanling rats.	2003-08	13679214
[Pharmacokinetic/pharmacodynamic analysis of anti-hyperprolactinemic effect of terguride based on dopamine D2 receptor occupancy].	2003-04	12704865
Suppression of cocaine- and food-maintained behavior by the D2-like receptor partial agonist terguride in squirrel monkeys.	2003-03	12589523
[Arrest of lactation after 2nd trimester abortion with a single dose of cabergoline in comparison with 10-day administration of teguride].	2003-01	12708116
[Results of treatment for male prolactinomas].	2002-12	12491580
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.	2002-11	12388668
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.	2002-11	12388667
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.	2002-11	12388666
Terguride treatment attenuated prolactin release and enhanced insulin receptor affinity and GLUT 4 content in obese spontaneously hypertensive female, but not male rats.	2002-06	12079879
Clustered ergot alkaloids modulate cell-mediated cytotoxicity.	2002-02	11741789
Atypical kinetics for a series of putative dopamine antagonists to reverse the low-magnitude Ca2+ phase in the dopamine-bound D2short receptor state.	2002-01	11862337
Dopamine partial agonist reverses amphetamine withdrawal in rats.	2001-11	11682262
Reinforcing effects of D2 dopamine receptor agonists and partial agonists in rhesus monkeys.	2001-10-01	11543991
Effects of terguride on anterior pituitary function in parkinsonian patients treated with L-dopa: a double-blind study versus placebo.	1996-02	8867520
Effects of several partial dopamine D2 receptor agonists in Cebus apella monkeys previously treated with haloperidol.	1993-06-24	8103465
Effects of terguride, a partial D2 agonist, on MPTP-lesioned parkinsonian cynomolgus monkeys.	1993-05	8098931
Partial dopamine agonist therapy of levodopa-induced dyskinesias.	1992-06	1351273
Antagonist effect of terguride in Parkinson's disease.	1991-10	1683813
Effect of D1 and D2 agonists and antagonists on dyskinesia produced by L-dopa in 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine-treated monkeys.	1991-10	1681090
Behavioural profile of partial D2 dopamine receptor agonists. 1. Atypical inhibition of d-amphetamine-induced locomotor hyperactivity and stereotypy.	1991	1686815
Transdihydrolisuride in parkinsonism.	1987	3815388

Patents

Sample Use Guides

In Vivo Use Guide

Terguride was given orally in doses of 0.25 mg, 0.5 mg, and 1 mg.

Route of Administration: Oral

In Vitro Use Guide

Collagen synthesis activity was assessed by measuring the incorporation of [3H]proline as follows: 3 x 104 cells were seeded in 24-well plates and grown overnight in DMEM/F12 medium supplemented with 10% dialyzed fetal calf serum and penicillin/streptomycin. The medium was replaced with a low serum concentration of 0.5%. After 48 h the cells were incubated in DMEM/F12 supplemented with 10 mkM phenelzine (a nonselective monoamine oxidase inhibitor) and 0.6 mM ascorbic acid. 5-HT (in the absence and presence of terguride) and terguride alone were added. Terguride was added 30 min before 5-HT. Cells were then incubated for 48 h in the presence of 1 mkCi/ml [3H]proline. Cells were washed twice with ice-cold PBS before precipitation with ice-cold 10% trichloroacetic acid for 1 h at 4°C. The precipitates were solubilized in 0.3 N NaOH/0.1% SDS solution at 37°C under gentle agitation, mixed with scintillation cocktail, and measured in a beta-scintillation counter. Experiments were performed in triplicate or quadruplicate. Results are presented as fold-changes compared with untreated control cells.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:15:11 GMT 2025` Edited by `admin` on `Mon Mar 31 18:15:11 GMT 2025`
Record UNII	21OJT43Q88
Record Status	`Validated (UNII)`
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Name

Type

Language

TERGURIDE

Official Name

English

TELURON

Preferred Name

English

Terguride [WHO-DD]

Common Name

English

terguride [INN]

Common Name

English

1,1-DIETHYL-3-(6-METHYLERGOLIN-8.ALPHA.-YL)UREA

Systematic Name

English

TERGURIDE [MART.]

Common Name

English

TERGURIDE [MI]

Common Name

English

TERGURIDE [JAN]

Common Name

English

Classification Tree Code System Code

WHO-ATC

G02CB06