Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H27N |
Molecular Weight | 293.4458 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)N1CCC(CC1)(C2=CC=CC=C2)C3=CC=CC=C3
InChI
InChIKey=QIHLUZAFSSMXHQ-UHFFFAOYSA-N
InChI=1S/C21H27N/c1-20(2,3)22-16-14-21(15-17-22,18-10-6-4-7-11-18)19-12-8-5-9-13-19/h4-13H,14-17H2,1-3H3
Budipine is an antiparkinsonian drug, which was developed by Byk Gulden (now Takeda) for the treatment of Parkinson's disease. The drug has multiple mechanisms of action: it was found to interfere with dopamine biosynthesis, mainly by inhibiting MAO-B enzyme and stimulating aromatic L-amino acid decarboxylase. Also the drug inhibits the dopamine re-uptake and has weak affinity to NMDA and muscarinic receptors. Budipine passes the blood-brain barrier, is metabolized by hydroxylation, and is excreted by both in urine and feces within 24 h.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P27338 Gene ID: 4129.0 Gene Symbol: MAOB Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/10370904 |
5.0 µM [IC50] | ||
Target ID: Q01959 Gene ID: 6531.0 Gene Symbol: SLC6A3 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/10370904 |
11.0 µM [IC50] | ||
Target ID: P20711 Gene ID: 1644.0 Gene Symbol: DDC Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/10370904 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | PARKINSAN Approved UseFor combination therapy of Parkinson's disease. Launch Date1996 |
PubMed
Title | Date | PubMed |
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Non-dopaminergic drug treatment of Parkinson's disease. | 2001 Apr |
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Budipine provides additional benefit in patients with Parkinson disease receiving a stable optimum dopaminergic drug regimen. | 2002 May |
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Evaluation of possible pro- or antioxidative properties and of the interaction capacity with the microsomal cytochrome P450 system of different NMDA-receptor ligands and of taurine in vitro. | 2003 Jun |
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[Diagnosis and treatment of Parkinson's syndrome. What is important for the general practitioner?]. | 2003 May 26 |
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Drug binding to aromatic residues in the HERG channel pore cavity as possible explanation for acquired Long QT syndrome by antiparkinsonian drug budipine. | 2003 Nov |
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Synergism between topiramate and budipine in refractory status epilepticus in the rat. | 2004 Nov |
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Effects of amantadine and budipine on antidepressant drug-evoked changes in extracellular 5-HT in the frontal cortex of freely moving rats. | 2005 Jul |
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The anti-Parkinson drug budipine is exported actively out of the brain by P-glycoprotein in mice. | 2005 Jul 22-29 |
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Effects of amantadine and budipine on antidepressant drug-evoked changes in extracellular dopamine in the frontal cortex of freely moving rats. | 2006 Oct 30 |
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Paradoxical aspects of parkinsonian tremor. | 2008 Jan 30 |
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A new strategy for antidepressant prescription. | 2010 |
Patents
Sample Use Guides
The dosage is determined individually. The treatment should start with 3 times daily 10 mg budipine hydrochloride. If necessary, the daily dose should be increased at the earliest after 1 week to 3 x 20 mg budipine hydrochloride or 2 x 30 mg budipine hydrochloride.
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://orbilu.uni.lu/handle/10993/17136
10(-7), 10(-8), 10(-9) mol/l of budipine significantly reduced release of TNF-alpha and Il-6 in PBMC and decreased apoptotic cell death after 50 hours and 74 hours in the SH-SY 5Y cells.
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C38149
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)