Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H18N4O2 |
| Molecular Weight | 298.3403 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
c1cnc(nc1)N2CCN(CC2)Cc3ccc4c(c3)OCO4
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 | 298.3403 |
| 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 |
|---|---|---|
| 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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| Pharmacological treatment for aphasia following stroke. | 2001 |
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| Antiparkinsonian agent piribedil displays antagonist properties at native, rat, and cloned, human alpha(2)-adrenoceptors: cellular and functional characterization. | 2001 Jun |
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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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| [Use of dopamine agonists in the treatment of 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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| Gateways to clinical trials. | 2002 Jul-Aug |
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| 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 Nov |
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| 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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| [Use of pronoran (piribedil) in Parkinson's disease: the results of a multicenter study]. | 2003 |
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| Quantitative determination of some pharmaceutical piperazine derivatives through complexation with iron(III) chloride. | 2003 Aug |
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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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| [Treatment of Parkinson's disease: use of piribedil]. | 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 |
|
| Acute treatment of migraine. Breaking the paradigm of monotherapy. | 2004 Jan 28 |
|
| Determination of piribedil in pharmaceutical formulations by micellar electrokinetic capillary chromatography. | 2004 May |
|
| Cognitive skill learning in healthy older adults after 2 months of double-blind treatment with piribedil. | 2004 Nov |
|
| [Modern aproaches to the treatment of early stages of Parkinson disease]. | 2005 |
|
| 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 |
|
| [The role of pronoran in the therapy of late stage of Parkinson's disease]. | 2006 |
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| Restless legs syndrome: diagnosis and review of management options. | 2006 Jun |
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| [Cognitive disturbances and dysfunction of neuromediator systems in cerebral vascular insufficiency after treatment with pronoran]. | 2007 |
|
| Identification of amino acid determinants of dopamine 2 receptor synthetic agonist function. | 2007 Apr |
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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 |
|
| [Implication of piribedil (pronoran) in the treatment of Parkinson's disease; a clinical and pharmacoeconomic analysis]. | 2008 |
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| Impact of newer pharmacological treatments on quality of life in patients with Parkinson's disease. | 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 |
|
| Ruthenium-catalyzed N-alkylation of amines and sulfonamides using borrowing hydrogen methodology. | 2009 Feb 11 |
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| Hallucinations: Etiology and clinical implications. | 2009 Jul |
|
| Orodispersible sublingual piribedil to abort OFF episodes: a single dose placebo-controlled, randomized, double-blind, cross-over study. | 2010 Feb 15 |
|
| Cognitive psychiatry in India. | 2010 Jan |
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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 |
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
Sat Jun 26 06:28:07 UTC 2021
by
admin
on
Sat Jun 26 06:28:07 UTC 2021
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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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3605-01-4
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2569
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3605-01-4
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4850
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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 |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
