U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C12H13N
Molecular Weight 171.2383
Optical Activity ( + )
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RASAGILINE

SMILES

C#CCN[C@@H]1CCC2=CC=CC=C12

InChI

InChIKey=RUOKEQAAGRXIBM-GFCCVEGCSA-N
InChI=1S/C12H13N/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12/h1,3-6,12-13H,7-9H2/t12-/m1/s1

HIDE SMILES / InChI
Molecular Formula C12H13N
Molecular Weight 171.2383
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Rasagiline (N-propargyl-1-(R)-aminoindan) is a selective, irreversible monoamine oxidase B (MAO B) inhibitor, which has been developed as an anti-Parkinson drug and was sold as a mesylate salt under brand name AZILECT. AZILECT is indicated for the treatment of the signs and symptoms of idiopathic Parkinson’s disease (PD) as initial monotherapy and as adjunct therapy to levodopa. The effectiveness of AZILECT was demonstrated in patients with early Parkinson’s disease who were receiving AZILECT as monotherapy and who were not receiving any concomitant dopaminergic therapy. The effectiveness of AZILECT as adjunct therapy was demonstrated in patients with Parkinson’s disease who were treated with levodopa. PD is a progressive neurodegenerative, dopamine deficiency disorder. The main therapeutic strategies for PD treatment relies on dopamine precursors (levodopa), inhibition of dopamine metabolism (monoamine oxidase [MAO] B and catechol-O-methyl transferase inhibitors), and dopamine receptor agonists. In contrast to selegiline, rasagiline is not metabolized to potentially toxic amphetamine metabolites. The precise mechanisms of action of rasagiline is unknown. One mechanism is believed to be related to its MAO-B inhibitory activity, which causes an increase in extracellular levels of dopamine in the striatum.

CNS Activity

Originator

Approval Year

2006
178
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8429
AZILECT

Approved Use

AZILECT (rasagiline tablets) is indicated for the treatment of Parkinson’s disease (PD). AZILECT, a monoamine oxidase (MAO)-B inhibitor (MAOI), is indicated for the treatment of Parkinson’s disease (1)

Launch Date

2006
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
56.13 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/15628826
10 mg 1 times / day multiple, oral
dose: 10 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
RASAGILINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
53.53 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/15628826
10 mg 1 times / day multiple, oral
dose: 10 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
RASAGILINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.17 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/15628826
10 mg 1 times / day multiple, oral
dose: 10 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
RASAGILINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
2.5 mg single, transdermal
Dose: 2.5 mg
Route: transdermal
Route: single
Dose: 2.5 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/29159774
healthy, 22–25 years
n = 4
Health Status: healthy
Age Group: 22–25 years
Sex: M
Population Size: 4
Sources:
https://pubmed.ncbi.nlm.nih.gov/29159774
Sources:
https://pubmed.ncbi.nlm.nih.gov/29159774
2 mg single, oral
Highest studied dose
Dose: 2 mg
Route: oral
Route: single
Dose: 2 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
healthy, 33 years
n = 16
Health Status: healthy
Age Group: 33 years
Sex: M+F
Population Size: 16
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
2 mg 1 times / day steady, oral
Highest studied dose
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
healthy, 33 years
n = 16
Health Status: healthy
Age Group: 33 years
Sex: M+F
Population Size: 16
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
Other AEs: Ear discomfort, Musculoskeletal pain...
Other AEs:
Ear discomfort (1 patient)
Musculoskeletal pain (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
4 mg 1 times / day steady, oral
Highest studied dose
Dose: 4 mg, 1 times / day
Route: oral
Route: steady
Dose: 4 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/15300656
unhealthy, 62.0 years
n = 14
Health Status: unhealthy
Condition: Early Parkinson’s Disease
Age Group: 62.0 years
Sex: M+F
Population Size: 14
Sources:
https://pubmed.ncbi.nlm.nih.gov/15300656
Sources:
https://pubmed.ncbi.nlm.nih.gov/15300656
100 mg single, oral
Overdose
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
unknown, adult
n = 1
Health Status: unknown
Age Group: adult
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
Other AEs: Serotonin syndrome...
Other AEs:
Serotonin syndrome (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
3 mg 1 times / day multiple, oral
Overdose
Dose: 3 mg, 1 times / day
Route: oral
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
unknown, adult
n = 1
Health Status: unknown
Age Group: adult
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
Other AEs: Hypertension, Orthostatic hypotension...
Other AEs:
Hypertension (1 patient)
Orthostatic hypotension (1 patient)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
1 mg 1 times / day steady, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: steady
Dose: 1 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
unhealthy, adult
n = 149
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Population Size: 149
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
Disc. AE: Hallucinations...
AEs leading to
discontinuation/dose reduction:
Hallucinations
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Ear discomfort 1 patient
2 mg 1 times / day steady, oral
Highest studied dose
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
healthy, 33 years
n = 16
Health Status: healthy
Age Group: 33 years
Sex: M+F
Population Size: 16
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
Musculoskeletal pain 1 patient
2 mg 1 times / day steady, oral
Highest studied dose
Dose: 2 mg, 1 times / day
Route: oral
Route: steady
Dose: 2 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
healthy, 33 years
n = 16
Health Status: healthy
Age Group: 33 years
Sex: M+F
Population Size: 16
Sources:
https://pubmed.ncbi.nlm.nih.gov/30218626
Serotonin syndrome 1 patient
100 mg single, oral
Overdose
Dose: 100 mg
Route: oral
Route: single
Dose: 100 mg
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
unknown, adult
n = 1
Health Status: unknown
Age Group: adult
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
Hypertension 1 patient
3 mg 1 times / day multiple, oral
Overdose
Dose: 3 mg, 1 times / day
Route: oral
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
unknown, adult
n = 1
Health Status: unknown
Age Group: adult
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
Orthostatic hypotension 1 patient
3 mg 1 times / day multiple, oral
Overdose
Dose: 3 mg, 1 times / day
Route: oral
Route: multiple
Dose: 3 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
unknown, adult
n = 1
Health Status: unknown
Age Group: adult
Population Size: 1
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
Hallucinations Disc. AE
1 mg 1 times / day steady, oral
Recommended
Dose: 1 mg, 1 times / day
Route: oral
Route: steady
Dose: 1 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
unhealthy, adult
n = 149
Health Status: unhealthy
Condition: Parkinson’s disease
Age Group: adult
Population Size: 149
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/201971Orig1s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1587
inhibitor
1767
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2C19
1478

CYP2E1
882

CYP4A
19
CYP1A2
1054

P-gp
1537

CYP2A6
543
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1692
 no
CYP2A6
739
 no
CYP2C19
1553
 no
CYP2C9
1819
 no
CYP2D6
1891
 no
CYP2E1
970
 no
CYP3A4
1925
 no
CYP4A
33
 no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1054
 major
yes (co-administration study)
Comment: ciprofloxacin increased rasagiline AUC by 83%
Page: 56, 57, 69
CYP2A6
543
 no
P-gp
1537
 no
no (co-administration study)
Comment: hesperetin and narigenin enhanced the systemic exposure of rasagiline not through P-gp
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:63620
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:63620
ChemicalBook
CB2459598
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB2459598
MolPort
MolPort-003-850-132
https://www.molport.com/shop/molecule-link/MolPort-003-850-132
ZINC
ZINC000019875504
http://zinc15.docking.org/substances/ZINC000019875504
eMolecules
2727012
https://www.emolecules.com/cgi-bin/more?vid=2727012
PubMed

PubMed

TitleDatePubMed
The anti-Parkinson drug rasagiline and its cholinesterase inhibitor derivatives exert neuroprotection unrelated to MAO inhibition in cell culture and in vivo.
2001 Jun
Neuroprotective and neurotoxic effects of monoamine oxidase-B inhibitors and derived metabolites under ischemia in PC12 cells.
2002 Jan 11
Test-retest reliability of the unified Parkinson's disease rating scale in patients with early Parkinson's disease: results from a multicenter clinical trial.
2002 Jul
An anti-Parkinson's disease drug, N-propargyl-1(R)-aminoindan (rasagiline), enhances expression of anti-apoptotic bcl-2 in human dopaminergic SH-SY5Y cells.
2002 Jun 28
Mitochondria determine the survival and death in apoptosis by an endogenous neurotoxin, N-methyl(R)salsolinol, and neuroprotection by propargylamines.
2002 May
Rasagiline. Teva Pharmaceutical.
2002 May
Novel dual inhibitors of AChE and MAO derived from hydroxy aminoindan and phenethylamine as potential treatment for Alzheimer's disease.
2002 Nov 21
Involvement of MAP kinase in the regulation of amyloid precursor protein processing by novel cholinesterase inhibitors derived from rasagiline.
2002 Oct
Neuroprotection by propargylamines in Parkinson's disease: suppression of apoptosis and induction of prosurvival genes.
2002 Sep-Oct
Monoamine oxidase inhibitors l-deprenyl and clorgyline protect nonmalignant human cells from ionising radiation and chemotherapy toxicity.
2003 Nov 17
The essentiality of Bcl-2, PKC and proteasome-ubiquitin complex activations in the neuroprotective-antiapoptotic action of the anti-Parkinson drug, rasagiline.
2003 Oct 15
Recent approaches to novel anti-Alzheimer therapy.
2004
A controlled, randomized, delayed-start study of rasagiline in early Parkinson disease.
2004 Apr
Contrasting neuroprotective and neurotoxic actions of respective metabolites of anti-Parkinson drugs rasagiline and selegiline.
2004 Jan 30
Rasagiline enhances L-DOPA-induced contralateral turning in the unilateral 6-hydroxydopamine-lesioned guinea-pig.
2004 Jul
Regulation of protein kinase C by the anti-Parkinson drug, MAO-B inhibitor, rasagiline and its derivatives, in vivo.
2004 Jun
Neuroprotective effect of rasagiline in a rodent model of Parkinson's disease.
2004 Jun
Crystal structures of monoamine oxidase B in complex with four inhibitors of the N-propargylaminoindan class.
2004 Mar 25
Tolerability, safety, pharmacodynamics, and pharmacokinetics of rasagiline: a potent, selective, and irreversible monoamine oxidase type B inhibitor.
2004 Oct
[The early therapy challenge].
2005
Alternatives to levodopa in the initial treatment of early Parkinson's disease.
2005
Rasagiline.
2005
Rasagiline.
2005 Aug
Neuroprotective effect of rasagiline, a monoamine oxidase-B inhibitor, on spontaneous cell degeneration in a rat model.
2005 Aug
Binding of rasagiline-related inhibitors to human monoamine oxidases: a kinetic and crystallographic analysis.
2005 Dec 29
[Rasagiline. A new monoamine oxidase b inhibitor for Parkinson treatment].
2005 Jul
Parkinson's disease. Diagnosis and the initiation of therapy.
2005 Jun
Rasagiline for motor complications in Parkinson's disease.
2005 Mar 12-18
Evidence-based medical review update: pharmacological and surgical treatments of Parkinson's disease: 2001 to 2004.
2005 May
Recent advances in Parkinson's disease therapy: use of monoamine oxidase inhibitors.
2005 Nov
Regulation of Bcl-2 family proteins, neurotrophic factors, and APP processing in the neurorescue activity of propargylamine.
2005 Nov
Novel potential neuroprotective agents with both iron chelating and amino acid-based derivatives targeting central nervous system neurons.
2005 Nov 25
In vivo measurement of brain monoamine oxidase B occupancy by rasagiline, using (11)C-l-deprenyl and PET.
2005 Oct
Rasagiline: defining the role of a novel therapy in the treatment of Parkinson's disease.
2006 Feb
Rationale for considering that propargylamines might be neuroprotective in Parkinson's disease.
2006 May 23
Safety of rasagiline in elderly patients with Parkinson disease.
2006 May 9
Patents

Patents

07375249
5
07476757
5
07491847
5
07547806
5
07750051
5
07855233
5
07968749
5
08143315
5
08163960
5
08334409
5
08614252
5
08691872
5
08741962
5
JP2000508292A
5
JP2003160481A
5
JP2009527574A
5
JP2010018626A
5
JP2011051986A
5
JP2011524353A
5
JP2011524907A
5
JP2011529480A
5
JP3341898B2
5
JP4108750B2
5
JP5356248B2
5
JPH03294248A
5

Sample Use Guides

In Vivo Use Guide
Monotherapy: the recommended AZILECT (RASAGILINE MESYLATE) dose for the treatment of Parkinson’s disease patients is 1 mg administered once daily. Adjunctive Therapy: the recommended initial dose is 0.5 mg administered once daily. If a sufficient clinical response is not achieved, the dose may be increased to 1 mg administered once daily. Change of levodopa dose in adjunct therapy: When AZILECT is used in combination with levodopa, a reduction of the levodopa dosage may be considered based upon individual response. During the controlled trials of AZILECT as adjunct therapy to levodopa, levodopa dosage was reduced in some patients. In clinical studies, dosage reduction of levodopa was allowed within the first 6 weeks if dopaminergic side effects, including dyskinesia and hallucinations, emerged.
Route of Administration: Oral
In Vitro Use Guide
The present series of in vitro experiments using the rat hippocampal slice preparation deals with effects of rasagiline and its metabolite R-(-)-aminoindan on the pyramidal cell response after electric stimulation of the Schaffer Collaterals in comparison to selegiline, another MAO B inhibitor. During the first series, this response was attenuated in the presence of rasagiline and aminoindan-to a lesser degree of selegiline-in a concentration dependent manner (5-50 μM) after single stimuli as well as under theta burst stimulation (TBS). The presence of rasagiline and aminoindan, but rarely the presence of selegiline, prevented this break down. Following glutamate receptor mediated enhancements of neuronal transmission in a second series of experiments very clear differences could be observed in comparison to the action of selegiline: NMDA receptor, AMPA receptor as well as metabotropic glutamate receptor mediated increases of transmission were concentration dependently (0,3 - 2 μM) antagonized by rasagiline and aminoindan, but not by selegiline. On the opposite, only selegiline attenuated kainate receptor mediated increases of excitability. Thus, both monoamino oxidase (MAO) B inhibitors show attenuation of glutamatergic transmission in the hippocampus but interfere with different receptor mediated excitatory modulations at low concentrations.
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:28:14 GMT 2023
Edited
by admin
on Fri Dec 15 16:28:14 GMT 2023
Record UNII
003N66TS6T
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
RASAGILINE
EMA EPAR   HSDB   INN   MI   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
1H-INDEN-1-AMINE, 2,3-DIHYDRO-N-2-PROPYN-1-YL-, (1R)-
Systematic Name English
AGN-1135
Code English
NSC-759639
Code English
rasagiline [INN]
Common Name English
RASAGILINE [HSDB]
Common Name English
RASAGILINE [ORANGE BOOK]
Common Name English
(R)-(+)-RASAGILINE
Common Name English
RASAGILINE [VANDF]
Common Name English
TV-1030
Code English
(1R)-2,3-DIHYDRO-N-2-PROPYN-1-YL-1H-INDEN-1-AMINE
Systematic Name English
1H-INDEN-1-AMINE, 2,3-DIHYDRO-N-2-PROPYNYL-, (R)-
Systematic Name English
RASAGILINE [MI]
Common Name English
RASAGILINE [EMA EPAR]
Common Name English
1H-INDEN-1-AMINE, 2,3-DIHYDRO-N-2-PROPYNYL-, (1R)-
Systematic Name English
Rasagiline [WHO-DD]
Common Name English
RASAGILINE [USAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C38149
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
WHO-ATC N04BD02
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
NDF-RT N0000175744
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
LIVERTOX NBK547919
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
NDF-RT N0000000184
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
NCI_THESAURUS C667
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
WHO-VATC QN04BD02
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
Code System Code Type Description
MERCK INDEX
m9504
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY Merck Index
EVMPD
SUB10261MIG
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
RXCUI
134748
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY RxNorm
CAS
136236-51-6
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
FDA UNII
003N66TS6T
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
EPA CompTox
DTXSID3041112
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
INN
7151
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
CHEBI
63620
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
WIKIPEDIA
RASAGILINE
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
MESH
C031967
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
PUBCHEM
3052776
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
DRUG BANK
DB01367
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
DAILYMED
003N66TS6T
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
IUPHAR
6641
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
HSDB
7699
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
LACTMED
Rasagiline
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
ChEMBL
CHEMBL887
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
NCI_THESAURUS
C66510
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
DRUG CENTRAL
3521
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
USAN
YY-124
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
NSC
759639
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
SMS_ID
100000089182
Created by admin on Fri Dec 15 16:28:14 GMT 2023 , Edited by admin on Fri Dec 15 16:28:14 GMT 2023
PRIMARY
Related Record Type Details
Structure of RASAGILINE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
Structure of RASAGILINE BESYLATE
SALT/SOLVATE -> PARENT
CYTOCHROME P450 1A2
METABOLIC ENZYME -> SUBSTRATE
Structure of RASAGILINE TARTRATE
SALT/SOLVATE -> PARENT
Structure of RASAGILINE MESYLATE
SALT/SOLVATE -> PARENT
AMINE OXIDASE (FLAVIN-CONTAINING) B
TARGET -> INHIBITOR
Structure of Rasagiline, (±)-
RACEMATE -> ENANTIOMER
Related Record Type Details
Structure of 1-INDANOL
METABOLITE -> PARENT
Structure of 1H-INDEN-1-ONE, 3-AMINO-2,3-DIHYDRO-, (3R)-
METABOLITE -> PARENT
Structure of 2,3-Dihydro-3-(2-propyn-1-ylamino)-1H-inden-1-one, (3R)-
METABOLITE -> PARENT
Structure of 3-KETO-AAI
METABOLITE -> PARENT
Structure of 2,3-DIHYDRO-3-(2-PROPYN-1-YLAMINO)-1H-INDEN-1-OL, (3R)-
METABOLITE -> PARENT
Structure of (3R)-3-AMINO-2,3-DIHYDRO-1H-INDEN-1-OL
METABOLITE -> PARENT
Structure of 1-AMINOINDANE, (R)-
METABOLITE -> PARENT
major metabolite, 1(R)-aminoindan, which is not an MAO inhibitor, has been therapeutically active in animal models relevant to Parkinson?s disease
MAJOR
PLASMA
Structure of 1-INDANONE
METABOLITE -> PARENT
Structure of ((3R)-3-(PROP-2-YNYLAMINO)INDAN-1-YL) DIHYDROGEN PHOSPHATE
METABOLITE -> PARENT
Structure of 3-OH-AAI
METABOLITE -> PARENT
Structure of 1-AMINOINDANE, (R)-
METABOLITE -> PARENT
In vitro experiments indicate that both routes of rasagiline metabolism are dependent on the cytochrome P450 (CYP) system, with CYP1A2 being the major isoenzyme involved in rasagiline metabolism
Related Record Type Details
Structure of RASAGILINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC
NIH
NCATS
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