Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H15N3S.2ClH |
Molecular Weight | 282.233 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.NC1=NC2=C(CCN(CC=C)CC2)S1
InChI
InChIKey=DPQAXNSOFFYKDS-UHFFFAOYSA-N
InChI=1S/C10H15N3S.2ClH/c1-2-5-13-6-3-8-9(4-7-13)14-10(11)12-8;;/h2H,1,3-7H2,(H2,11,12);2*1H
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 |
---|---|---|
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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[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 |
|
Intranasal application of the alpha2-adrenoceptor agonist BHT-920 produces decongestion in the cat. | 2001 Nov-Dec |
|
alpha(2)-adrenoceptor antagonist properties of OPC-28326, a novel selective peripheral vasodilator. | 2001 Oct |
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Influence of sildenafil on central dopamine-mediated behaviour in male rats. | 2002 Feb 15 |
|
Neuroleptic-like profile of the cannabinoid agonist, HU 210, on rodent behavioural models. | 2002 Jan |
|
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. 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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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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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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MPP(+)-induced cytotoxicity in neuroblastoma cells: Antagonism and reversal by guanosine. | 2007 Sep |
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Genetic findings in Parkinson's disease and translation into treatment: a leading role for mitochondria? | 2008 Mar |
|
Effective control of catatonia in Parkinson's disease by electroconvulsive therapy: a case report. | 2009 Feb |
|
Oxidative stress induction of DJ-1 protein in reactive astrocytes scavenges free radicals and reduces cell injury. | 2009 Jan-Mar |
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
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36085-73-1
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104870
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100000090502
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DTXSID20189669
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SUB04670MIG
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m10441
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PRIMARY | Merck Index |
ACTIVE MOIETY
SUBSTANCE RECORD