Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H18N4O2 |
| Molecular Weight | 298.3397 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C(N1CCN(CC1)C2=NC=CC=N2)C3=CC=C4OCOC4=C3
InChI
InChIKey=OQDPVLVUJFGPGQ-UHFFFAOYSA-N
InChI=1S/C16H18N4O2/c1-4-17-16(18-5-1)20-8-6-19(7-9-20)11-13-2-3-14-15(10-13)22-12-21-14/h1-5,10H,6-9,11-12H2
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: P35462 Gene ID: 1814.0 Gene Symbol: DRD3 Target Organism: Homo sapiens (Human) |
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Target ID: P14416 Gene ID: 1813.0 Gene Symbol: DRD2 Target Organism: Homo sapiens (Human) |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | TRIVASTAL Approved UseAdjunctive treatment of intermittent claudication in chronic obliterating arteriopathies of the lower limbs (in stage 2). |
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| Palliative | TRIVASTAL Approved UseAdjunctive symptomatic treatment of chronic pathological cognitive and neurosensorial deficit in elderly subjects (excluding Alzheimer's disease and other dementia). |
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| Primary | TRIVASTAL Approved UseTreatment of Parkinson's disease: either as monotherapy (treatment of forms with predominant tremor), or in association with dopatherapy from the outset, or secondarily, particularly in forms with tremor. |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Piribedil: its synergistic effect in multidrug regimens for parkinsonism. | 1976 May |
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| A comparison of piribedil, procyclidine and placebo in the control of phenothiazine-induced parkinsonism. | 1977 Jun |
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| Dopamine receptor stimulation in the treatment of depression: piribedil (ET-495). | 1978 |
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| Parkinsonism by haloperidol and piribedil. | 1978 Oct 31 |
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| Discriminative stimulus properties of the dopamine D3 receptor agonists, PD128,907 and 7-OH-DPAT: a comparative characterization with novel ligands at D3 versus D2 receptors. | 2000 Feb 14 |
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| Pharmacological treatment for aphasia following stroke. | 2001 |
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| Dopamine agonist-induced dyskinesias are correlated to both firing pattern and frequency alterations of pallidal neurones in the MPTP-treated monkey. | 2001 Mar |
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| Piribedil for restless legs syndrome: a pilot study. | 2001 May |
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| [Use of dopamine analogs in Parkinson's disease treatment]. | 2002 |
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| DA agonists -- non-ergot derivatives: piribedil: management of Parkinson's disease. | 2002 |
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| Choosing the right dopamine agonist for patients with Parkinson's disease. | 2002 |
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| Clinical pharmacokinetic and pharmacodynamic properties of drugs used in the treatment of Parkinson's disease. | 2002 |
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| Psychomotor and cognitive effects of piribedil, a dopamine agonist, in young healthy volunteers. | 2002 Feb |
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| Sleep attacks in patients taking dopamine agonists: review. | 2002 Jun 22 |
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| Repeated administration of piribedil induces less dyskinesia than L-dopa in MPTP-treated common marmosets: a behavioural and biochemical investigation. | 2002 Sep |
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| [Use of pronoran (piribedil) in Parkinson's disease: the results of a multicenter study]. | 2003 |
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| Piribedil-induced sleep attacks in Parkinson's disease. | 2003 Feb |
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| Age-related mild cognitive deficit: a ready-to-use concept? | 2003 Mar |
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| [Clinical and stabilometric analysis of postural instability in Parkinson's disease]. | 2004 |
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| [The effectiveness and tolerance of piribedil as adjunct therapy to levodopa in patients with Parkinson's disease: a nine month follow up]. | 2004 Apr 16-30 |
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| Acute treatment of migraine. Breaking the paradigm of monotherapy. | 2004 Jan 28 |
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| Drug treatment of Parkinson's disease. | 2004 Sep |
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| The effects of dopaminergic agonists on genital reflexes in paradoxical sleep-deprived male rats. | 2005 Feb 15 |
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| Evidence-based medical review update: pharmacological and surgical treatments of Parkinson's disease: 2001 to 2004. | 2005 May |
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| The Parkinson-Control study: a 1-year randomized, double-blind trial comparing piribedil (150 mg/day) with bromocriptine (25 mg/day) in early combination with levodopa in Parkinson's disease. | 2006 Apr |
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| Early piribedil monotherapy of Parkinson's disease: A planned seven-month report of the REGAIN study. | 2006 Dec |
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| Impaired cognition and attention in adults: pharmacological management strategies. | 2007 Feb |
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| Effects of the dopamine agonist piribedil on prefrontal temporal cortical network function in normal aging as assessed by verbal fluency. | 2007 Jan 30 |
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| About the anti-Parkinson equivalency of levodopa and dopamine agonists. | 2007 Jan-Feb |
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| Genetic Contribution of Catechol-O-methyltransferase Polymorphism in Patients with Migraine without Aura. | 2007 Mar |
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| Peripheral edema and dopamine agonists in Parkinson disease. | 2007 Oct |
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| Current management of the cognitive dysfunction in Parkinson's disease: how far have we come? | 2008 Aug |
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| Comparative effects of the dopaminergic agonists piribedil and bromocriptine in three different memory paradigms in rodents. | 2008 Jul |
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| Ruthenium-catalyzed N-alkylation of amines and sulfonamides using borrowing hydrogen methodology. | 2009 Feb 11 |
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| Mild cognitive impairment: The dilemma. | 2009 Jan |
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| Parkinson's disease sleep scale, sleep logs, and actigraphy in the evaluation of sleep in parkinsonian patients. | 2009 Sep |
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| Plasma neuropeptide Y: a biomarker for symptom severity in chronic fatigue syndrome. | 2010 Dec 29 |
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| Cognitive psychiatry in India. | 2010 Jan |
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| Is there an inhibitory-response-control system in the rat? Evidence from anatomical and pharmacological studies of behavioral inhibition. | 2010 Jan |
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| From the cell to the clinic: a comparative review of the partial D₂/D₃receptor agonist and α2-adrenoceptor antagonist, piribedil, in the treatment of Parkinson's disease. | 2010 Nov |
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| Pre-treatment with dopamine agonists influence L-dopa mediated rotations without affecting abnormal involuntary movements in the 6-OHDA lesioned rat. | 2010 Nov 12 |
Patents
Sample Use Guides
For the treatment of Parkinson's disease as a monotherapy, piribedil should be administered orally at 150 to 250 mg.
Route of Administration:
Oral
Binding of piribedil to D2, D3 and D4 receptors was measured using [3H]spiperone as a radiolabel. Coronal sections from rat brains were cut at the level of the anterior caudate-putame. The sections were thaw-mounted on gelatin-coated glass slides. Sections were incubated for 5 min in a 50mM Tris-HCl buffer, then were incubated for 30 min at room temperature in the incubation buffer. Piribedil was tested in vitro at 5 different concentrations, from 10 uM to 1 nM.
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WHO-ATC |
N04BC08
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QN04BC08
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NCI_THESAURUS |
C66884
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PIRIBEDIL
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SUB09908MIG
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
