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Identification
NameRasagiline
Accession NumberDB01367  (EXPT02758)
TypeSmall Molecule
GroupsApproved
Description

Rasagiline is an irreversible inhibitor of monoamine oxidase and is used as a monotherapy in early Parkinson’s disease or as an adjunct therapy in more advanced cases.

Structure
Thumb
Synonyms
(1R)-N-Propargylindan-1-amine
(R)-Indan-1-yl-prop-2-ynyl-amine
(R)-N-2-Propynyl-1-indanamine
RAS
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Azilecttablet1 mg/1oralPhysicians Total Care, Inc.2010-12-03Not applicableUs
Azilecttablet1.0 mgoralTeva Pharmaceutical Industries Ltd2006-09-14Not applicableCanada
Azilecttablet0.5 mgoralTeva Pharmaceutical Industries Ltd2006-09-14Not applicableCanada
Azilecttablet1 mg/1oralTeva Neuroscience, Inc.2006-07-10Not applicableUs
Azilecttablet.5 mg/1oralTeva Neuroscience, Inc.2006-07-10Not applicableUs
Teva-rasagilinetablet1.0 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Teva-rasagilinetablet0.5 mgoralTeva Canada LimitedNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-rasagilinetablet0.5 mgoralApotex Inc2016-01-12Not applicableCanada
Apo-rasagilinetablet1 mgoralApotex Inc2016-01-12Not applicableCanada
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Rasagiline mesylate
ThumbNot applicableDBSALT001384
Categories
UNII003N66TS6T
CAS number136236-51-6
WeightAverage: 171.2383
Monoisotopic: 171.104799421
Chemical FormulaC12H13N
InChI KeyInChIKey=RUOKEQAAGRXIBM-GFCCVEGCSA-N
InChI
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
IUPAC Name
(1R)-N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine
SMILES
C#CCN[C@@H]1CCC2=CC=CC=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as indanes. These are compounds containing an indane moiety, which consists of a cyclopentane fused to a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassIndanes
Sub ClassNot Available
Direct ParentIndanes
Alternative Parents
Substituents
  • Indane
  • Aralkylamine
  • Secondary amine
  • Secondary aliphatic amine
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic homopolycyclic compound
Molecular FrameworkAromatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of the signs and symptoms of idiopathic Parkinsons disease as initial monotherapy and as adjunct therapy to levodopa.
PharmacodynamicsRasagiline is a propargylamine and an irreversible inhibitor of monoamine oxidase (MAO). MAO, a flavin-containing enzyme, regulates the metabolic degradation of catecholamines and serotonin in the CNS and peripheral tissues. It is classified into two major molecular species, A and B, and is localized in mitochondrial membranes throughout the body in nerve terminals, brain, liver and intestinal mucosa. MAO-A is found predominantly in the GI tract and liver, and regulates the metabolic degradation of circulating catecholamines and dietary amines. MAO-B is the major form in the human brain and is responsible for the regulation of the metabolic degradation of dopamine and phenylethylamine. In ex vivo animal studies in brain, liver and intestinal tissues rasagiline was shown to be a potent,selective, and irreversible monoamine oxidase type B (MAO-B) inhibitor. At the recommended therapeutic doses, Rasagiline was also shown to be a potent and irreversible inhibitor of MAO-B in platelets. The selectivity of rasagiline for inhibiting only MAO-B (and not MAO-A) in humans and the sensitivity to tyramine during rasagiline treatment at any dose has not been sufficiently characterized to avoid restriction of dietary tyramine and amines contained in medications.
Mechanism of actionThe 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. The elevated dopamine level and subsequent increased dopaminergic activity are likely to mediate rasagiline's beneficial effects seen in models of dopaminergic motor dysfunction.
Related Articles
AbsorptionRasagiline is rapidly absorbed following oral administration. The absolute bioavailability of rasagiline is about 36%.
Volume of distribution
  • 87 L
Protein bindingPlasma protein binding ranges from 88-94% with mean extent of binding of 61-63% to human albumin over the concentration range of 1-100 ng/ml.
Metabolism

Rasagiline undergoes almost complete biotransformation in the liver prior to excretion. In vitro experiments indicate that both routes of rasagiline metabolism are dependent on the cytochrome P450 (CYP) system, with CYP 1A2 being the major isoenzyme involved in rasagiline metabolism.

Route of eliminationRasagiline undergoes almost complete biotransformation in the liver prior to excretion. Glucuronide conjugation of rasagiline and its metabolites, with subsequent urinary excretion, is the major elimination pathway. After oral administration of 14C-labeled rasagiline, elimination occurred primarily via urine and secondarily via feces (62% of total dose in urine and 7% of total dose in feces over 7 days), with a total calculated recovery of 84% of the dose over a period of 38 days. Less than 1% of rasagiline was excreted as unchanged drug in urine.
Half lifeRasagiline has a mean steady-state half life of 3 hours but there is no correlation of pharmacokinetics with its pharmacological effect because of its irreversible inhibition of MAO-B.
ClearanceNot Available
ToxicitySigns and symptoms of overdosage may include, alone or in combination, any of the following: drowsiness, dizziness, faintness, irritability, hyperactivity, agitation, severe headache, hallucinations, trismus, opisthotonos, convulsions, and coma; rapid and irregular pulse, hypertension, hypotension and vascular collapse; precordial pain, respiratory depression and failure, hyperpyrexia, diaphoresis, and cool, clammy skin.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9901
Blood Brain Barrier+0.9782
Caco-2 permeable+0.5585
P-glycoprotein substrateNon-substrate0.661
P-glycoprotein inhibitor INon-inhibitor0.7409
P-glycoprotein inhibitor IINon-inhibitor0.7116
Renal organic cation transporterNon-inhibitor0.5584
CYP450 2C9 substrateNon-substrate0.8037
CYP450 2D6 substrateSubstrate0.5724
CYP450 3A4 substrateNon-substrate0.6928
CYP450 1A2 substrateInhibitor0.9037
CYP450 2C9 inhibitorNon-inhibitor0.8259
CYP450 2D6 inhibitorInhibitor0.6769
CYP450 2C19 inhibitorInhibitor0.5689
CYP450 3A4 inhibitorNon-inhibitor0.8542
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.534
Ames testNon AMES toxic0.6468
CarcinogenicityNon-carcinogens0.8959
BiodegradationNot ready biodegradable0.6073
Rat acute toxicity2.8164 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7804
hERG inhibition (predictor II)Non-inhibitor0.7137
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Tabletoral1 mg
Tabletoral.5 mg/1
Tabletoral0.5 mg
Tabletoral1 mg/1
Tabletoral1.0 mg
Prices
Unit descriptionCostUnit
Azilect 0.5 mg tablet12.11USD tablet
Azilect 1 mg tablet12.11USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2031714 No1998-08-252010-12-06Canada
CA2232310 No2008-01-082016-09-18Canada
US5387612 No1995-02-072012-02-07Us
US5453446 No1997-02-072017-02-07Us
US6126968 No1996-09-182016-09-18Us
US7572834 No2006-12-052026-12-05Us
US7815942 No2007-08-272027-08-27Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.0249 mg/mLALOGPS
logP2.26ALOGPS
logP2.3ChemAxon
logS-3.8ALOGPS
pKa (Strongest Basic)8.69ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area12.03 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity54.47 m3·mol-1ChemAxon
Polarizability20.25 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Jeffrey Sterling, David Lerner, Harel Rosen, Leonid Bronov, Dalia Medini-Green, Berta Iosefzon, Tirtsah Berger-Peskin, Ramy Lidor-Hadas, Eliezer Bahar, “Rasagiline formulations and processes for their preparation.” U.S. Patent US07598420, issued October 06, 2009.

US07598420
General References
  1. Weinreb O, Amit T, Bar-Am O, Youdim MB: Rasagiline: a novel anti-Parkinsonian monoamine oxidase-B inhibitor with neuroprotective activity. Prog Neurobiol. 2010 Nov;92(3):330-44. doi: 10.1016/j.pneurobio.2010.06.008. Epub 2010 Jun 19. [PubMed:20600573 ]
  2. Leegwater-Kim J, Bortan E: The role of rasagiline in the treatment of Parkinson's disease. Clin Interv Aging. 2010 May 25;5:149-56. [PubMed:20517484 ]
  3. Chen JJ, Swope DM, Dashtipour K: Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease. Clin Ther. 2007 Sep;29(9):1825-49. [PubMed:18035186 ]
External Links
ATC CodesN04BD02
AHFS Codes
  • 28:92.00
PDB Entries
FDA labelDownload (200 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Rasagiline can be increased when it is combined with Abiraterone.
AcepromazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Acetophenazine.
AltretamineAltretamine may increase the orthostatic hypotensive activities of Rasagiline.
AmisulprideThe risk or severity of adverse effects can be increased when Rasagiline is combined with Amisulpride.
AmitriptylineRasagiline may increase the serotonergic activities of Amitriptyline.
AmphetamineRasagiline may increase the hypertensive activities of Amphetamine.
ApraclonidineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Apraclonidine.
AripiprazoleThe risk or severity of adverse effects can be increased when Rasagiline is combined with Aripiprazole.
AtomoxetineRasagiline may increase the central neurotoxic activities of Atomoxetine.
AtropineRasagiline may increase the hypertensive activities of Atropine.
BenzquinamideThe risk or severity of adverse effects can be increased when Rasagiline is combined with Benzquinamide.
BetahistineThe serum concentration of Betahistine can be increased when it is combined with Rasagiline.
BezafibrateThe risk or severity of adverse effects can be increased when Rasagiline is combined with Bezafibrate.
BortezomibThe metabolism of Rasagiline can be decreased when combined with Bortezomib.
BrimonidineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Brimonidine.
BuprenorphineThe risk or severity of adverse effects can be increased when Buprenorphine is combined with Rasagiline.
BupropionRasagiline may increase the hypertensive activities of Bupropion.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Rasagiline.
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Rasagiline.
CarphenazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Carphenazine.
CathinoneRasagiline may increase the hypertensive activities of Cathinone.
ChlormezanoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Chlorprothixene.
CiprofloxacinThe serum concentration of Rasagiline can be increased when it is combined with Ciprofloxacin.
ClozapineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Clozapine.
CyclobenzaprineCyclobenzaprine may increase the serotonergic activities of Rasagiline.
CyproheptadineRasagiline may increase the anticholinergic activities of Cyproheptadine.
Cyproterone acetateThe serum concentration of Rasagiline can be decreased when it is combined with Cyproterone acetate.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Rasagiline.
DeferasiroxThe serum concentration of Rasagiline can be increased when it is combined with Deferasirox.
DexmethylphenidateRasagiline may increase the hypertensive activities of Dexmethylphenidate.
DextromethorphanRasagiline may increase the serotonergic activities of Dextromethorphan.
DiethylpropionRasagiline may increase the hypertensive activities of Diethylpropion.
DomperidoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Domperidone.
DoxapramRasagiline may increase the hypertensive activities of Doxapram.
DroperidolThe risk or severity of adverse effects can be increased when Rasagiline is combined with Droperidol.
EpinephrineRasagiline may increase the hypertensive activities of Epinephrine.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Rasagiline.
FencamfamineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Fencamfamine.
FlupentixolThe risk or severity of adverse effects can be increased when Rasagiline is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Fluspirilene.
FluvoxamineThe serum concentration of Rasagiline can be increased when it is combined with Fluvoxamine.
GranisetronGranisetron may increase the serotonergic activities of Rasagiline.
HaloperidolThe risk or severity of adverse effects can be increased when Rasagiline is combined with Haloperidol.
HydrocodoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Hydrocodone.
HydromorphoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Hydromorphone.
Insulin HumanRasagiline may increase the hypoglycemic activities of Insulin Regular.
IsomethepteneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Isometheptene.
L-TryptophanThe risk or severity of adverse effects can be increased when L-Tryptophan is combined with Rasagiline.
LevodopaThe risk or severity of adverse effects can be increased when Levodopa is combined with Rasagiline.
LevonordefrinRasagiline may increase the hypertensive activities of Levonordefrin.
LinezolidThe risk or severity of adverse effects can be increased when Rasagiline is combined with Linezolid.
LithiumThe risk or severity of adverse effects can be increased when Rasagiline is combined with Lithium.
LoxapineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Loxapine.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Rasagiline.
MequitazineRasagiline may increase the anticholinergic activities of Mequitazine.
MesoridazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Mesoridazine.
MethadoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Methadone.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Methotrimeprazine.
MethoxsalenThe serum concentration of Rasagiline can be increased when it is combined with Methoxsalen.
MethyldopaThe risk or severity of adverse effects can be increased when Rasagiline is combined with Methyldopa.
Methylene blueRasagiline may increase the serotonergic activities of Methylene blue.
MethylphenidateRasagiline may increase the hypertensive activities of Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Rasagiline is combined with Metoclopramide.
MexiletineThe serum concentration of Rasagiline can be increased when it is combined with Mexiletine.
MianserinRasagiline may increase the neurotoxic activities of Mianserin.
MidodrineRasagiline may increase the hypertensive activities of Midodrine.
MirtazapineRasagiline may increase the central neurotoxic activities of Mirtazapine.
MoclobemideThe risk or severity of adverse effects can be increased when Rasagiline is combined with Moclobemide.
MolindoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Molindone.
MorphineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Morphine.
MoxonidineRasagiline may increase the hypotensive activities of Moxonidine.
NorepinephrineRasagiline may increase the hypertensive activities of Norepinephrine.
OfloxacinThe serum concentration of Rasagiline can be increased when it is combined with Ofloxacin.
OlanzapineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Olanzapine.
OndansetronThe risk or severity of adverse effects can be increased when Rasagiline is combined with Ondansetron.
OrciprenalineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Orciprenaline.
OxycodoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Oxycodone.
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Rasagiline.
PaliperidoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Paliperidone.
ParoxetineRasagiline may increase the serotonergic activities of Paroxetine.
Peginterferon alfa-2bThe serum concentration of Rasagiline can be increased when it is combined with Peginterferon alfa-2b.
PerphenazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Perphenazine.
PethidineRasagiline may increase the serotonergic activities of Pethidine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Rasagiline.
PholcodinePholcodine may increase the serotonergic activities of Rasagiline.
PimozideThe risk or severity of adverse effects can be increased when Rasagiline is combined with Pimozide.
PipamperoneThe therapeutic efficacy of Pipamperone can be decreased when used in combination with Rasagiline.
PiperacetazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Piperacetazine.
PizotifenRasagiline may increase the anticholinergic activities of Pizotifen.
PrimaquineThe serum concentration of Rasagiline can be increased when it is combined with Primaquine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Quetiapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Rasagiline is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Reserpine.
RisperidoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Risperidone.
SertindoleThe risk or severity of adverse effects can be increased when Rasagiline is combined with Sertindole.
StiripentolThe serum concentration of Rasagiline can be increased when it is combined with Stiripentol.
SufentanilSufentanil may increase the serotonergic activities of Rasagiline.
SulpirideThe risk or severity of adverse effects can be increased when Rasagiline is combined with Sulpiride.
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Rasagiline.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Rasagiline.
TeriflunomideThe serum concentration of Rasagiline can be decreased when it is combined with Teriflunomide.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Rasagiline.
TetryzolineRasagiline may increase the hypertensive activities of Tetryzoline.
ThioridazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Thiothixene.
TolcaponeThe risk or severity of adverse effects can be increased when Tolcapone is combined with Rasagiline.
TramadolTramadol may increase the neuroexcitatory activities of Rasagiline.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Rasagiline.
TrazodoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Trazodone.
TrifluoperazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Triflupromazine.
VemurafenibThe serum concentration of Rasagiline can be increased when it is combined with Vemurafenib.
VenlafaxineRasagiline may increase the serotonergic activities of Venlafaxine.
ZiprasidoneThe risk or severity of adverse effects can be increased when Rasagiline is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Rasagiline is combined with Zuclopenthixol.
Food Interactions
  • Avoid alcohol and caffeine.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Primary amine oxidase activity
Specific Function:
Catalyzes the oxidative deamination of biogenic and xenobiotic amines and has important functions in the metabolism of neuroactive and vasoactive amines in the central nervous system and peripheral tissues. MAOB preferentially degrades benzylamine and phenylethylamine.
Gene Name:
MAOB
Uniprot ID:
P27338
Molecular Weight:
58762.475 Da
References
  1. Naoi M, Maruyama W: Functional mechanism of neuroprotection by inhibitors of type B monoamine oxidase in Parkinson's disease. Expert Rev Neurother. 2009 Aug;9(8):1233-50. doi: 10.1586/ern.09.68. [PubMed:19673610 ]
  2. Uzun M, Alp R, Uzlu E, Alp S, Citil M, Topcu B, Erdogan HM: Investigation of oral selegiline and rasagiline administration on QT interval in conscious rabbits. Eur Rev Med Pharmacol Sci. 2009 Mar-Apr;13(2):95-8. [PubMed:19499843 ]
  3. Youdim MB, Weinstock M: Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R)aminoindan-5-YL)-ethyl methyl carbamate]. Cell Mol Neurobiol. 2001 Dec;21(6):555-73. [PubMed:12043833 ]
  4. Chau KY, Cooper JM, Schapira AH: Rasagiline protects against alpha-synuclein induced sensitivity to oxidative stress in dopaminergic cells. Neurochem Int. 2010 Nov;57(5):525-9. doi: 10.1016/j.neuint.2010.06.017. Epub 2010 Jul 17. [PubMed:20624440 ]
  5. Weinreb O, Amit T, Bar-Am O, Youdim MB: Rasagiline: a novel anti-Parkinsonian monoamine oxidase-B inhibitor with neuroprotective activity. Prog Neurobiol. 2010 Nov;92(3):330-44. doi: 10.1016/j.pneurobio.2010.06.008. Epub 2010 Jun 19. [PubMed:20600573 ]
  6. Youdim MB, Bar Am O, Yogev-Falach M, Weinreb O, Maruyama W, Naoi M, Amit T: Rasagiline: neurodegeneration, neuroprotection, and mitochondrial permeability transition. J Neurosci Res. 2005 Jan 1-15;79(1-2):172-9. [PubMed:15573406 ]
  7. Leegwater-Kim J, Bortan E: The role of rasagiline in the treatment of Parkinson's disease. Clin Interv Aging. 2010 May 25;5:149-56. [PubMed:20517484 ]
  8. Chen JJ, Swope DM, Dashtipour K: Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease. Clin Ther. 2007 Sep;29(9):1825-49. [PubMed:18035186 ]
  9. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
activator
General Function:
Ubiquitin protein ligase binding
Specific Function:
Suppresses apoptosis in a variety of cell systems including factor-dependent lymphohematopoietic and neural cells. Regulates cell death by controlling the mitochondrial membrane permeability. Appears to function in a feedback loop system with caspases. Inhibits caspase activity either by preventing the release of cytochrome c from the mitochondria and/or by binding to the apoptosis-activating f...
Gene Name:
BCL2
Uniprot ID:
P10415
Molecular Weight:
26265.66 Da
References
  1. Youdim MB, Weinstock M: Molecular basis of neuroprotective activities of rasagiline and the anti-Alzheimer drug TV3326 [(N-propargyl-(3R)aminoindan-5-YL)-ethyl methyl carbamate]. Cell Mol Neurobiol. 2001 Dec;21(6):555-73. [PubMed:12043833 ]
  2. Akao Y, Maruyama W, Yi H, Shamoto-Nagai M, Youdim MB, Naoi M: 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. Neurosci Lett. 2002 Jun 28;326(2):105-8. [PubMed:12057839 ]
  3. Maruyama W, Akao Y, Carrillo MC, Kitani K, Youdium MB, Naoi M: Neuroprotection by propargylamines in Parkinson's disease: suppression of apoptosis and induction of prosurvival genes. Neurotoxicol Teratol. 2002 Sep-Oct;24(5):675-82. [PubMed:12200198 ]
  4. Youdim MB, Amit T, Falach-Yogev M, Bar Am O, Maruyama W, Naoi M: The essentiality of Bcl-2, PKC and proteasome-ubiquitin complex activations in the neuroprotective-antiapoptotic action of the anti-Parkinson drug, rasagiline. Biochem Pharmacol. 2003 Oct 15;66(8):1635-41. [PubMed:14555244 ]
  5. Bar-Am O, Weinreb O, Amit T, Youdim MB: Regulation of Bcl-2 family proteins, neurotrophic factors, and APP processing in the neurorescue activity of propargylamine. FASEB J. 2005 Nov;19(13):1899-901. Epub 2005 Sep 7. [PubMed:16148027 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Lecht S, Haroutiunian S, Hoffman A, Lazarovici P: Rasagiline - a novel MAO B inhibitor in Parkinson's disease therapy. Ther Clin Risk Manag. 2007 Jun;3(3):467-74. [PubMed:18488080 ]
  2. Leegwater-Kim J, Bortan E: The role of rasagiline in the treatment of Parkinson's disease. Clin Interv Aging. 2010 May 25;5:149-56. [PubMed:20517484 ]
  3. Chen JJ, Swope DM, Dashtipour K: Comprehensive review of rasagiline, a second-generation monoamine oxidase inhibitor, for the treatment of Parkinson's disease. Clin Ther. 2007 Sep;29(9):1825-49. [PubMed:18035186 ]
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Drug created on June 13, 2005 07:24 / Updated on May 29, 2016 02:11