Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H26N4O.C4H4O4 |
| Molecular Weight | 454.5188 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C/C(O)=O.[H][C@@]12CC3=CNC4=C3C(=CC=C4)C1=C[C@@H](CN2C)NC(=O)N(CC)CC
InChI
InChIKey=CVQFAMQDTWVJSV-BAXNFHPCSA-N
InChI=1S/C20H26N4O.C4H4O4/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;5-3(6)1-2-4(7)8/h6-8,10-11,14,18,21H,4-5,9,12H2,1-3H3,(H,22,25);1-2H,(H,5,6)(H,7,8)/b;2-1-/t14-,18+;/m0./s1
DescriptionCurator's Comment: description was created based on several sources, including
http://www.bayerresources.com.au/resources/uploads/datasheet/file9563.pdf | https://www.ncbi.nlm.nih.gov/mesh/68008090
Curator's Comment: description was created based on several sources, including
http://www.bayerresources.com.au/resources/uploads/datasheet/file9563.pdf | https://www.ncbi.nlm.nih.gov/mesh/68008090
Lisuride (DOPERGIN®), a highly active dopaminergic ergot derivative with prolactin-lowering properties, has a pronounced affinity for dopamine receptors. It may also act as an agonist at some serotonin receptors. Lisuride (DOPERGIN®) is concentrated within the pituitary where it acts on dopamine receptors which inhibit prolactin release. It can be used in the clinical conditions where a dopaminergic or prolactin-lowering effect is needed.
CNS Activity
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2056 |
7.19 null [pKi] | ||
Target ID: CHEMBL217 |
9.47 null [pKi] | ||
Target ID: CHEMBL234 |
9.55 null [pKi] | ||
Target ID: CHEMBL219 |
8.34 null [pKi] | ||
Target ID: CHEMBL1850 |
8.45 null [pKi] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | DOPERGIN Approved UseAs a Dopamine Agonist in:
* Parkinson's disease, postencephalitic parkinsonism, parkinsonism of other origin (with the exception of the medicine-induced form)
As a Prolactin Inhibitor in:
* Prevention of the onset of lactation in the puerperium (primary ablactation) only for clearly defined medical reasons
* Galactorrhea; prolactin-induced amenorrhea; prolactin-induced infertility in women; prolactinomas
* Acromegaly |
|||
| Preventing | DOPERGIN Approved UseAs a Dopamine Agonist in:
* Parkinson's disease, postencephalitic parkinsonism, parkinsonism of other origin (with the exception of the medicine-induced form)
As a Prolactin Inhibitor in:
* Prevention of the onset of lactation in the puerperium (primary ablactation) only for clearly defined medical reasons
* Galactorrhea; prolactin-induced amenorrhea; prolactin-induced infertility in women; prolactinomas
* Acromegaly |
|||
| Primary | DOPERGIN Approved UseAs a Dopamine Agonist in:
* Parkinson's disease, postencephalitic parkinsonism, parkinsonism of other origin (with the exception of the medicine-induced form)
As a Prolactin Inhibitor in:
* Prevention of the onset of lactation in the puerperium (primary ablactation) only for clearly defined medical reasons
* Galactorrhea; prolactin-induced amenorrhea; prolactin-induced infertility in women; prolactinomas
* Acromegaly |
|||
| Primary | DOPERGIN Approved UseAs a Dopamine Agonist in:
* Parkinson's disease, postencephalitic parkinsonism, parkinsonism of other origin (with the exception of the medicine-induced form)
As a Prolactin Inhibitor in:
* Prevention of the onset of lactation in the puerperium (primary ablactation) only for clearly defined medical reasons
* Galactorrhea; prolactin-induced amenorrhea; prolactin-induced infertility in women; prolactinomas
* Acromegaly |
|||
| Primary | DOPERGIN Approved UseAs a Dopamine Agonist in:
* Parkinson's disease, postencephalitic parkinsonism, parkinsonism of other origin (with the exception of the medicine-induced form)
As a Prolactin Inhibitor in:
* Prevention of the onset of lactation in the puerperium (primary ablactation) only for clearly defined medical reasons
* Galactorrhea; prolactin-induced amenorrhea; prolactin-induced infertility in women; prolactinomas
* Acromegaly |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Levodopa-induced dyskinesias in Parkinson's disease: clinical and pharmacological classification. | 1992 |
|
| [Use of dopamine agonists in the treatment of Parkinson's disease]. | 2002 |
|
| DA agonists -- ergot derivatives: bromocriptine: management of Parkinson's disease. | 2002 |
|
| [Results of treatment for male prolactinomas]. | 2002 Dec |
|
| Sleep attacks in patients taking dopamine agonists: review. | 2002 Jun 22 |
|
| 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 Nov |
|
| 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 Nov |
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| Re-evaluation of lisuride pharmacology: 5-hydroxytryptamine1A receptor-mediated behavioral effects overlap its other properties in rats. | 2002 Oct |
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| The trigonometric responder approach: a new method for detecting responders to pharmacological or experimental challenges. | 2002 Sep |
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| Inhibition of growth hormone excess reduces insulin resistance and ovarian dysfunction in a lean case of polycystic ovary syndrome with a growth-hormone-producing pituitary adenoma. | 2003 |
|
| Effects of a partial dopamine D2-like agonist on the cocaine-induced behavioral sensitization of preweanling rats. | 2003 Aug |
|
| Cortisol as an indicator of dopaminergic effects on nicotine craving. | 2003 Aug |
|
| Prevention and treatment of motor fluctuations. | 2003 Aug |
|
| [Arrest of lactation after 2nd trimester abortion with a single dose of cabergoline in comparison with 10-day administration of teguride]. | 2003 Jan |
|
| Suppression of cocaine- and food-maintained behavior by the D2-like receptor partial agonist terguride in squirrel monkeys. | 2003 Mar |
|
| The dopamine receptor agonist lisuride attenuates iron-mediated dopaminergic neurodegeneration. | 2003 Nov |
|
| Dopamine receptor agonists in current clinical use: comparative dopamine receptor binding profiles defined in the human striatum. | 2003 Oct |
|
| Management of restless legs syndrome by the partial D2-agonist terguride. | 2003 Sep |
|
| Transdermal lisuride delivery in the treatment of Parkinson's disease. | 2004 |
|
| LSD, 5-HT (serotonin), and the evolution of a behavioral assay. | 2004 Jan |
|
| No evidence of the usefulness of eye blinking as a marker for central dopaminergic activity. | 2004 Mar |
|
| 8R-lisuride is a potent stereospecific histamine H1-receptor partial agonist. | 2004 Mar |
|
| Familial acromegaly: a familial report and review of the literature. | 2004 May |
|
| Evidence for the management of mastalgia. | 2004 May |
|
| 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 Apr |
|
| Mastalgia: a review of management. | 2005 Dec |
|
| Capillary zone electrophoresis separation of enantiomers of lisuride. | 2005 Feb 25 |
|
| Buprenorphine and a CRF1 antagonist block the acquisition of opiate withdrawal-induced conditioned place aversion in rats. | 2005 Jan |
|
| Dopamine and serotonin modulate the onset of metamorphosis in the ascidian Phallusia mammillata. | 2005 Jun 1 |
|
| Evidence-based medical review update: pharmacological and surgical treatments of Parkinson's disease: 2001 to 2004. | 2005 May |
|
| Aripiprazole's low intrinsic activities at human dopamine D2L and D2S receptors render it a unique antipsychotic. | 2005 May 16 |
|
| Advances in the delivery of treatments for Parkinson's disease. | 2005 Nov |
|
| Treatment of pituitary tumors: dopamine agonists. | 2005 Oct |
|
| Transdermal treatment options for neurological disorders: impact on the elderly. | 2006 |
|
| Pharmacokinetic optimisation in the treatment of Parkinson's disease : an update. | 2006 |
|
| Dopamine stimulation via infusion in the lateral ventricle. | 2006 Aug |
|
| Ergoline and non-ergoline derivatives in the treatment of Parkinson's disease. | 2006 Aug |
|
| Striking differences of action of lisuride stereoisomers at histamine H1 receptors. | 2006 Dec |
|
| 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 Dec 15 |
|
| Effects of a partial D2-like receptor agonist on striatal dopamine autoreceptor functioning in preweanling rats. | 2006 Feb 16 |
|
| Lisuride treatment of restless legs syndrome: first studies with monotherapy in de novo patients and in combination with levodopa in advanced disease. | 2006 Jan |
|
| Transdermal lisuride: short-term efficacy and tolerability study in patients with severe restless legs syndrome. | 2006 Jan |
|
| Homology modelling of the serotoninergic 5-HT2c receptor. | 2006 Jun |
|
| Effects of terguride, ropinirole, and acetyl-L-carnitine on methamphetamine withdrawal in the rat. | 2006 Mar |
|
| The partial dopamine D2-like receptor agonist terguride functions as an agonist in preweanling rats after a 5-day reserpine regimen. | 2006 Mar |
|
| Potential vascular alpha1-adrenoceptor blocking properties of an array of 5-HT receptor ligands in the rat. | 2006 Mar 27 |
|
| Lisuride, a dopamine receptor agonist with 5-HT2B receptor antagonist properties: absence of cardiac valvulopathy adverse drug reaction reports supports the concept of a crucial role for 5-HT2B receptor agonism in cardiac valvular fibrosis. | 2006 Mar-Apr |
|
| Observed smoking in cars: a method and differences by socioeconomic area. | 2006 Oct |
|
| Glutamate-induced cell death and formation of radicals can be reduced by lisuride in mesencephalic primary cell culture. | 2006 Sep |
|
| In vitro functional characteristics of dopamine D2 receptor partial agonists in second and third messenger-based assays of cloned human dopamine D2Long receptor signalling. | 2007 Aug |
Sample Use Guides
Parkinsonism:
The treatment begins with half of a 0.2 mg DOPERGIN® tablet (0.1 mg) in the evening and should be increased by 0.1 mg weekly until a clinical effect becomes apparent.
Endocrine Indications:
One DOPERGIN® 0.2 mg tablet should be taken 2 to 3 times daily for 14 days.
Route of Administration:
Oral
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FDA ORPHAN DRUG |
906822
Created by
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EU-Orphan Drug |
EU/3/11/869
Created by
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| Code System | Code | Type | Description | ||
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SUB02940MIG
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100000086150
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31776
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6553
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DBSALT001034
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DTXSID501017378
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m6844
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5282421
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243-387-3
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19875-60-6
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UV1635N8XW
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CHEMBL157138
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ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
