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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| Age-related mild cognitive deficit: a ready-to-use concept? | 2003 Mar |
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| [Pronoran in the treatment of mental organic syndrome in the elderly]. | 2004 |
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| Efficacy and safety of piribedil in early combination with L-dopa in the treatment of Parkinson's disease: a 6-month open study. | 2004 Nov |
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| Drug treatment of Parkinson's disease. | 2004 Sep |
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| [Modern aproaches to the treatment of early stages of Parkinson disease]. | 2005 |
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| [Efficacy of pronoran in age-related memory impairment]. | 2005 |
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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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| End-of-dose akinesia after a single intravenous infusion of the dopaminergic agonist piribedil in Parkinson's disease patients: a pharmacokinetic/pharmacodynamic, randomized, double-blind study. | 2005 Jul |
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| Chemically modified carbon paste electrode for the potentiometric flow injection analysis of piribedil in pharmaceutical preparation and urine. | 2005 Jul 15 |
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| [Dopaminergic and noradrenergic therapy of cognitive impairment]. | 2006 |
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| [The role of pronoran in the therapy of late stage of Parkinson's disease]. | 2006 |
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| Pharmacokinetic optimisation in the treatment of Parkinson's disease : an update. | 2006 |
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| Pathophysiology and management of syncope in Kearns-Sayre syndrome. | 2006 Fall |
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| Proposed dose equivalence for rapid switch between dopamine receptor agonists in Parkinson's disease: a review of the literature. | 2006 Jan |
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| Restless legs syndrome: diagnosis and review of management options. | 2006 Jun |
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| Activation of D2-like receptors induces sympathetic climactic-like responses in male and female anaesthetised rats. | 2006 Jun |
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| Enhancement in dissolution pattern of piribedil by molecular encapsulation with beta-cyclodextrin. | 2006 Mar |
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| Prevalence and costs of parkinsonian syndromes associated with orthostatic hypotension. | 2006 Mar-Apr |
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| Switching from levodopa to the long-acting dopamine D2/D3 agonist piribedil reduces the expression of dyskinesia while maintaining effective motor activity in MPTP-treated primates. | 2006 May-Jun |
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| Antidepressant-like properties of the anti-Parkinson agent, piribedil, in rodents: mediation by dopamine D2 receptors. | 2006 Nov |
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| A reversed-phase high-performance liquid chromatographic method for the determination of zafirlukast in pharmaceutical formulations and human plasma. | 2006 Nov-Dec |
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| [Effect of dopamine deficiency on the preparation of visually guided saccadic eye movements]. | 2006 Sep-Oct |
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| [Cognitive disturbances and dysfunction of neuromediator systems in cerebral vascular insufficiency after treatment with pronoran]. | 2007 |
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| Importance of solid lipid nanoparticles (SLN) in various administration routes and future perspectives. | 2007 |
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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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| 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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| [Implication of piribedil (pronoran) in the treatment of Parkinson's disease; a clinical and pharmacoeconomic analysis]. | 2008 |
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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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| Functional neuroanatomy of the noradrenergic locus coeruleus: its roles in the regulation of arousal and autonomic function part II: physiological and pharmacological manipulations and pathological alterations of locus coeruleus activity in humans. | 2008 Sep |
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| Tinnitus treatment with piribedil guided by electrocochleography and acoustic otoemissions. | 2009 Aug |
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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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| Hallucinations: Etiology and clinical implications. | 2009 Jul |
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| Dopamine Agonists and their risk to induce psychotic episodes in Parkinson's disease: a case-control study. | 2009 Jun 10 |
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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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| Delusional infestation induced by piribedil add-on in Parkinson's disease. | 2010 Aug |
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| Plasma neuropeptide Y: a biomarker for symptom severity in chronic fatigue syndrome. | 2010 Dec 29 |
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| Orodispersible sublingual piribedil to abort OFF episodes: a single dose placebo-controlled, randomized, double-blind, cross-over study. | 2010 Feb 15 |
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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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| Impulse control disorder and piribedil: report of 5 cases. | 2010 Jan-Feb |
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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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WHO-VATC |
QN04BC08
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NCI_THESAURUS |
C66884
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DB12478
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D010891
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8353
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DO22K1PRDJ
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C81082
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M8877
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222-764-6
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PIRIBEDIL
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CHEMBL1371770
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3605-01-4
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2569
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DTXSID9045188
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4850
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2202
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SUB09908MIG
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)
