Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H18N4O2.CH4O3S |
| Molecular Weight | 394.445 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CS(O)(=O)=O.C(N1CCN(CC1)C2=NC=CC=N2)C3=CC=C4OCOC4=C3
InChI
InChIKey=DEZKFCIOSKCCHK-UHFFFAOYSA-N
InChI=1S/C16H18N4O2.CH4O3S/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;1-5(2,3)4/h1-5,10H,6-9,11-12H2;1H3,(H,2,3,4)
| Molecular Formula | CH4O3S |
| Molecular Weight | 96.106 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| 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) |
|||
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). |
|||
| Palliative | TRIVASTAL Approved UseAdjunctive symptomatic treatment of chronic pathological cognitive and neurosensorial deficit in elderly subjects (excluding Alzheimer's disease and other dementia). |
|||
| 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 |
|
| A comparison of piribedil, procyclidine and placebo in the control of phenothiazine-induced parkinsonism. | 1977 Jun |
|
| Dopamine receptor stimulation in the treatment of depression: piribedil (ET-495). | 1978 |
|
| [Pronoran in the treatment of mental organic syndrome in the elderly]. | 2004 |
|
| Drugs in development for Parkinson's disease. | 2004 Jul |
|
| 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 |
|
| [Modern aproaches to the treatment of early stages of Parkinson disease]. | 2005 |
|
| [An impact of pronoran on cognitive and affective disorders in Parkinson's disease]. | 2005 |
|
| The effects of dopaminergic agonists on genital reflexes in paradoxical sleep-deprived male rats. | 2005 Feb 15 |
|
| Evidence-based medical review update: pharmacological and surgical treatments of Parkinson's disease: 2001 to 2004. | 2005 May |
|
| [Dopaminergic and noradrenergic therapy of cognitive impairment]. | 2006 |
|
| [The role of pronoran in the therapy of late stage of Parkinson's disease]. | 2006 |
|
| Pharmacokinetic optimisation in the treatment of Parkinson's disease : an update. | 2006 |
|
| Early piribedil monotherapy of Parkinson's disease: A planned seven-month report of the REGAIN study. | 2006 Dec |
|
| Pathophysiology and management of syncope in Kearns-Sayre syndrome. | 2006 Fall |
|
| Proposed dose equivalence for rapid switch between dopamine receptor agonists in Parkinson's disease: a review of the literature. | 2006 Jan |
|
| Restless legs syndrome: diagnosis and review of management options. | 2006 Jun |
|
| Activation of D2-like receptors induces sympathetic climactic-like responses in male and female anaesthetised rats. | 2006 Jun |
|
| Enhancement in dissolution pattern of piribedil by molecular encapsulation with beta-cyclodextrin. | 2006 Mar |
|
| Prevalence and costs of parkinsonian syndromes associated with orthostatic hypotension. | 2006 Mar-Apr |
|
| 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 |
|
| Antidepressant-like properties of the anti-Parkinson agent, piribedil, in rodents: mediation by dopamine D2 receptors. | 2006 Nov |
|
| The dopamine agonist piribedil with L-DOPA improves attentional dysfunction: relevance for Parkinson's disease. | 2006 Nov |
|
| [Effect of dopamine deficiency on the preparation of visually guided saccadic eye movements]. | 2006 Sep-Oct |
|
| [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 |
|
| Impaired cognition and attention in adults: pharmacological management strategies. | 2007 Feb |
|
| Effects of the dopamine agonist piribedil on prefrontal temporal cortical network function in normal aging as assessed by verbal fluency. | 2007 Jan 30 |
|
| About the anti-Parkinson equivalency of levodopa and dopamine agonists. | 2007 Jan-Feb |
|
| Genetic Contribution of Catechol-O-methyltransferase Polymorphism in Patients with Migraine without Aura. | 2007 Mar |
|
| Peripheral edema and dopamine agonists in Parkinson disease. | 2007 Oct |
|
| [Implication of piribedil (pronoran) in the treatment of Parkinson's disease; a clinical and pharmacoeconomic analysis]. | 2008 |
|
| Impact of newer pharmacological treatments on quality of life in patients with Parkinson's disease. | 2008 |
|
| Current management of the cognitive dysfunction in Parkinson's disease: how far have we come? | 2008 Aug |
|
| Comparative effects of the dopaminergic agonists piribedil and bromocriptine in three different memory paradigms in rodents. | 2008 Jul |
|
| 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 |
|
| Tinnitus treatment with piribedil guided by electrocochleography and acoustic otoemissions. | 2009 Aug |
|
| Ruthenium-catalyzed N-alkylation of amines and sulfonamides using borrowing hydrogen methodology. | 2009 Feb 11 |
|
| Hallucinations: Etiology and clinical implications. | 2009 Jul |
|
| Dopamine Agonists and their risk to induce psychotic episodes in Parkinson's disease: a case-control study. | 2009 Jun 10 |
|
| Parkinson's disease sleep scale, sleep logs, and actigraphy in the evaluation of sleep in parkinsonian patients. | 2009 Sep |
|
| Delusional infestation induced by piribedil add-on in Parkinson's disease. | 2010 Aug |
|
| Plasma neuropeptide Y: a biomarker for symptom severity in chronic fatigue syndrome. | 2010 Dec 29 |
|
| 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 |
|
| Is there an inhibitory-response-control system in the rat? Evidence from anatomical and pharmacological studies of behavioral inhibition. | 2010 Jan |
|
| 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
Fri Dec 15 15:47:17 GMT 2023
by
admin
on
Fri Dec 15 15:47:17 GMT 2023
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| Record UNII |
1U37NGM6KK
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| Record Status |
Validated (UNII)
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| Record Version |
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