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Details

Stereochemistry ACHIRAL
Molecular Formula C21H27N.ClH
Molecular Weight 329.907
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BUDIPINE HYDROCHLORIDE

SMILES

Cl.CC(C)(C)N1CCC(CC1)(C2=CC=CC=C2)C3=CC=CC=C3

InChI

InChIKey=USUUKNCFNKZGEY-UHFFFAOYSA-N
InChI=1S/C21H27N.ClH/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;1H

HIDE SMILES / InChI

Description

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.

CNS Activity

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
5.0 µM [IC50]
11.0 µM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
PARKINSAN

Funbound

ValueDoseCo-administeredAnalytePopulation
4%
BUDIPINE plasma
Homo sapiens

Doses

AEs

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
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
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.