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
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
|||
Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
---|---|---|
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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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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Antagonistic activity of ascorbic acid (vitamin C) on dopaminergic modulation: apomorphine-induced stereotypic behavior in mice. | 2006 |
|
Effect of bromocriptine on the severity of ovarian hyperstimulation syndrome and outcome in high responders undergoing assisted reproduction. | 2010 May |
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
Edited
Fri Dec 15 15:28:52 GMT 2023
by
admin
on
Fri Dec 15 15:28:52 GMT 2023
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Record UNII |
9R6E1D8H1O
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Record Status |
Validated (UNII)
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Record Version |
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PRIMARY | Merck Index |
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |