Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H15N3S |
Molecular Weight | 209.311 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=NC2=C(CCN(CC=C)CC2)S1
InChI
InChIKey=DHSSDEDRBUKTQY-UHFFFAOYSA-N
InChI=1S/C10H15N3S/c1-2-5-13-6-3-8-9(4-7-13)14-10(11)12-8/h2H,1,3-7H2,(H2,11,12)
Molecular Formula | C10H15N3S |
Molecular Weight | 209.311 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionCurator's Comment: Description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/8842679
Curator's Comment: Description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/8842679
Talipexole is a D2 receptor agonist which was marketed in June 1996 in Japan for the treatment of Parkinson's disease. Clinical trials with talipexole in patients with Parkinson's disease demonstrated statistically significant improvements from baseline for parkinsonian symptoms including akinesia, rigidity, tremor and gait disturbances.
CNS Activity
Originator
Sources: http://adisinsight.springer.com/drugs/800001261
Curator's Comment: # Boehringer Ingelheim Pharma KG
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL217 Sources: http://www.ncbi.nlm.nih.gov/pubmed/10455328 |
5.8 null [pKi] | ||
Target ID: CHEMBL234 Sources: http://www.ncbi.nlm.nih.gov/pubmed/10455328 |
7.0 null [pKi] | ||
Target ID: CHEMBL1867 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12388666 |
7.43 null [pKi] | ||
Target ID: CHEMBL1942 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12388666 |
7.09 null [pKi] | ||
Target ID: CHEMBL1916 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12388666 |
7.37 null [pKi] | ||
Target ID: CHEMBL219 Sources: http://www.ncbi.nlm.nih.gov/pubmed/12388666 |
6.48 null [pKi] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Release and aggregation of cytochrome c and alpha-synuclein are inhibited by the antiparkinsonian drugs, talipexole and pramipexole. | 2001 Apr 6 |
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Identification of the dopamine autoreceptor in the guinea-pig retina as D(2) receptor using novel subtype-selective antagonists. | 2001 Aug |
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Postjunctional alpha(2C)-adrenoceptor contractility in human saphenous vein. | 2001 Feb 16 |
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Receptor reserve analysis of the human alpha(2C)-adrenoceptor using. | 2001 Jan 12 |
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Nonlinear analysis of partial dopamine agonist effects on cAMP in C6 glioma cells. | 2001 Jan-Feb |
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[A-56-year-old woman with parkinsonism, whose mother had Parkinson's disease]. | 2001 May |
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Analysis of ligand activation of alpha 2-adrenoceptor subtypes under conditions of equal G alpha protein stoichiometry. | 2001 May |
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Modulation of ligand responses by coupling of alpha(2A)-adrenoceptors to diverse G(alpha)-proteins. | 2001 May 1 |
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Intranasal application of the alpha2-adrenoceptor agonist BHT-920 produces decongestion in the cat. | 2001 Nov-Dec |
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alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator. | 2001 Oct |
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Alpha2-adrenoceptor ligands inhibit alpha1-adrenoceptor-mediated contraction of isolated rat arteries. | 2002 Aug |
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Influence of sildenafil on central dopamine-mediated behaviour in male rats. | 2002 Feb 15 |
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Neuroleptic-like profile of the cannabinoid agonist, HU 210, on rodent behavioural models. | 2002 Jan |
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Impaired endothelial alpha-2 adrenergic receptor-mediated vascular relaxation in the fructose-fed rat. | 2002 Mar |
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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 |
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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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Inhibitory effects of D2 agonists by striatal injection on excessive release of dopamine and hyperactivity induced by Bay K 8644 in rats. | 2003 |
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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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Paraquat leads to dopaminergic neural vulnerability in organotypic midbrain culture. | 2003 Aug |
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Repeated administration of methamphetamine causes hypersensitivity of D2 receptor in rat ventral tegmental area. | 2003 Aug 21 |
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Prolonged drug-induced hypothermia in experimental stroke. | 2003 Mar-Apr |
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Effects of an alpha2-adrenoceptor agonist in nasal mucosa. | 2003 Oct |
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Blood pressure and alpha-vascular reactivity in hypertensive rats treated with amlodipine and dietary Ca. | 2004 Apr 5 |
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Immunohistochemical and functional evidence for a noradrenergic regulation in the horse penile deep dorsal vein. | 2004 Dec |
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An update on the dopaminergic treatment of restless legs syndrome and periodic limb movement disorder. | 2004 May 1 |
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Practice parameters for the dopaminergic treatment of restless legs syndrome and periodic limb movement disorder. | 2004 May 1 |
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Low dose pramipexole is neuroprotective in the MPTP mouse model of Parkinson's disease, and downregulates the dopamine transporter via the D3 receptor. | 2004 Oct 11 |
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Drug treatment of Parkinson's disease. | 2004 Sep |
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Antagonistic activity of ascorbic acid (vitamin C) on dopaminergic modulation: apomorphine-induced stereotypic behavior in mice. | 2006 |
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Pre-junctional alpha2-adrenoceptors modulation of the nitrergic transmission in the pig urinary bladder neck. | 2007 |
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alpha2-adrenoceptor agonists as nasal decongestants. | 2007 |
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MPP(+)-induced cytotoxicity in neuroblastoma cells: Antagonism and reversal by guanosine. | 2007 Sep |
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Pharmacological modulation of dopaminergic brain activity and its reflection in spectral frequencies of the rat electropharmacogram. | 2008 |
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Mechanism of decongestant activity of alpha 2-adrenoceptor agonists. | 2008 |
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Clinical characteristics of restless legs syndrome in end-stage renal failure and idiopathic RLS patients. | 2008 Apr 30 |
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Dopamine receptor agonists reverse behavioral abnormalities of alpha-synuclein transgenic mouse, a new model of Parkinson's disease. | 2008 Feb 15 |
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Genetic findings in Parkinson's disease and translation into treatment: a leading role for mitochondria? | 2008 Mar |
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The frequency of cardiac valvular regurgitation in Parkinson's disease. | 2008 May 15 |
|
Bromocriptine, a dopamine D(2) receptor agonist with the structure of the amino acid ergot alkaloids, induces neurite outgrowth in PC12 cells. | 2008 Nov 19 |
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Effective control of catatonia in Parkinson's disease by electroconvulsive therapy: a case report. | 2009 Feb |
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Oxidative stress induction of DJ-1 protein in reactive astrocytes scavenges free radicals and reduces cell injury. | 2009 Jan-Mar |
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Pharmacokinetic profile of talipexole in healthy volunteers is not altered when it is co-administered with Madopar (co-beneldopa). | 2009 Jun |
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Oxidative neurodegeneration is prevented by UCP0045037, an allosteric modulator for the reduced form of DJ-1, a wild-type of familial Parkinson's disease-linked PARK7. | 2009 Nov 5 |
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The neuroprotective effect of talipexole from paraquat-induced cell death in dopaminergic neuronal cells. | 2010 Dec |
|
Effect of bromocriptine on the severity of ovarian hyperstimulation syndrome and outcome in high responders undergoing assisted reproduction. | 2010 May |
|
[Dopaminergic neuroprotection and reconstruction of neural network tiara]. | 2010 Oct |
Patents
Sample Use Guides
Initially 0.2 or 0-4 mg/day, increased by 0.4 mg every week (usual maintenance dosage 1.2 to 3.6 mg/day)
Below 0.8 mg/day, once a day; 0.8 to 1.2 mg/day, twice a day; over 1.2 mg/day, 3 times a day
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/11301060
Talipexole at low concentration (0.1-1 mM) significantly inhibited the accumulation of cytochrome c in the cytosolic fraction of human neuroblastoma SH-SY5Y cells
Substance Class |
Chemical
Created
by
admin
on
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Fri Dec 15 17:37:10 GMT 2023
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Record UNII |
7AM2J46Z1Y
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Record Status |
Validated (UNII)
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Record Version |
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C66884
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m10441
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TALIPEXOLE
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Related Record | Type | Details | ||
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TARGET -> AGONIST | |||
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TRANSPORTER -> INHIBITOR | |||
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SALT/SOLVATE -> PARENT | |||
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TRANSPORTER -> INHIBITOR | |||
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TARGET -> AGONIST |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |