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
| Molecular Formula | C16H18N4O2 |
| Molecular Weight | 298.3397 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
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 |
|---|---|---|
| Clinical and pharmacological evaluation of the effects of piribedil in patients with parkinsonism. | 1975 Jan |
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| Piribedil: its synergistic effect in multidrug regimens for parkinsonism. | 1976 May |
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| Parkinsonism by haloperidol and piribedil. | 1978 Oct 31 |
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| Sleep attacks and Parkinson's disease treatment. | 2000 Apr 15 |
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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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| Randomized study of the dopamine receptor agonist piribedil in the treatment of mild cognitive impairment. | 2001 Sep |
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| DA agonists -- non-ergot derivatives: piribedil: management of Parkinson's disease. | 2002 |
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| Gateways to clinical trials. | 2002 Jul-Aug |
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| 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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| [The use of pronoran (piribedil) in Parkinson's disease]. | 2003 |
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| Efficacy of piribedil as early combination to levodopa in patients with stable Parkinson's disease: a 6-month, randomized, placebo-controlled study. | 2003 Apr |
|
| Piribedil enhances frontocortical and hippocampal release of acetylcholine in freely moving rats by blockade of alpha 2A-adrenoceptors: a dialysis comparison to talipexole and quinelorane in the absence of acetylcholinesterase inhibitors. | 2003 Apr |
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| Quantitative determination of some pharmaceutical piperazine derivatives through complexation with iron(III) chloride. | 2003 Aug |
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| Piribedil as an adjunct to levodopa in advanced Parkinson's disease: the Asian experience. | 2003 Dec |
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| Electroanalytical characteristics of piribedil and its differential pulse and square wave voltammetric determination in pharmaceuticals and human serum. | 2003 Mar 10 |
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| [Clinical and stabilometric analysis of postural instability in Parkinson's disease]. | 2004 |
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| Adsorptive stripping voltammetric behaviour of azomethine group in pyrimidine-containing drugs. | 2004 Feb 18 |
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| Drugs in development for Parkinson's disease. | 2004 Jul |
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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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| Evidence-based medical review update: pharmacological and surgical treatments of Parkinson's disease: 2001 to 2004. | 2005 May |
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| [The role of pronoran in the therapy of late stage of Parkinson's disease]. | 2006 |
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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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| 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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| Prevalence and costs of parkinsonian syndromes associated with orthostatic hypotension. | 2006 Mar-Apr |
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| The dopamine agonist piribedil with L-DOPA improves attentional dysfunction: relevance for Parkinson's disease. | 2006 Nov |
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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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| 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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| Parkinson's disease sleep scale, sleep logs, and actigraphy in the evaluation of sleep in parkinsonian patients. | 2009 Sep |
|
| Plasma neuropeptide Y: a biomarker for symptom severity in chronic fatigue syndrome. | 2010 Dec 29 |
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| Impulse control disorder and piribedil: report of 5 cases. | 2010 Jan-Feb |
|
| 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 |
|
| 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.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 22:35:53 UTC 2023
by
admin
on
Wed Jul 05 22:35:53 UTC 2023
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| Record UNII |
DO22K1PRDJ
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| Record Status |
Validated (UNII)
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| Record Version |
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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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100000081665
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2202
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SUB09908MIG
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| Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT | |||
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TARGET -> AGONIST |
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ACTIVE MOIETY |
