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Identification
NameLurasidone
Accession NumberDB08815
TypeSmall Molecule
GroupsApproved
Description

Lurasidone is an atypical antipsychotic developed by Dainippon Sumitomo Pharma. It was approved by the U.S. Food and Drug Administration (FDA) for treatment of schizophrenia on October 29, 2010 and is currently pending approval for the treatment of bipolar disorder in the United States. (Wikipedia)

Structure
Thumb
Synonyms
Lurasidona
Lurasidonum
External Identifiers
  • SM-13496
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Latudatablet120 mgoralSunovion Pharmaceuticals Canada Inc2012-09-06Not applicableCanada
Latudatablet, film coated20 mg/1oralSunovion Pharmaceuticals Inc.2011-12-07Not applicableUs
Latudatablet80 mgoralSunovion Pharmaceuticals Canada Inc2012-09-05Not applicableCanada
Latudatablet40 mgoralSunovion Pharmaceuticals Canada Inc2012-09-06Not applicableCanada
Latudatablet, film coated40 mg/1oralAvera Mc Kennan Hospital2015-03-02Not applicableUs
Latudatablet, film coated120 mg/1oralSunovion Pharmaceuticals Inc.2012-04-26Not applicableUs
Latudatablet, film coated80 mg/1oralSunovion Pharmaceuticals Inc.2010-10-28Not applicableUs
Latudatablet20 mgoralSunovion Pharmaceuticals Canada Inc2014-04-09Not applicableCanada
Latudatablet, film coated60 mg/1oralSunovion Pharmaceuticals Inc.2013-07-12Not applicableUs
Latudatablet60 mgoralSunovion Pharmaceuticals Canada Inc2014-03-14Not applicableCanada
Latudatablet, film coated40 mg/1oralSunovion Pharmaceuticals Inc.2010-10-28Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Lurasidone Hydrochloride
Thumb
  • InChI Key: NEKCRUIRPWNMLK-SCIYSFAVSA-N
  • Monoisotopic Mass: 528.232574845
  • Average Mass: 529.137
DBSALT000113
Categories
UNII22IC88528T
CAS number367514-87-2
WeightAverage: 492.676
Monoisotopic: 492.255897106
Chemical FormulaC28H36N4O2S
InChI KeyInChIKey=PQXKDMSYBGKCJA-CVTJIBDQSA-N
InChI
InChI=1S/C28H36N4O2S/c33-27-24-18-9-10-19(15-18)25(24)28(34)32(27)17-21-6-2-1-5-20(21)16-30-11-13-31(14-12-30)26-22-7-3-4-8-23(22)35-29-26/h3-4,7-8,18-21,24-25H,1-2,5-6,9-17H2/t18-,19+,20-,21-,24+,25-/m0/s1
IUPAC Name
(1R,2S,6R,7S)-4-{[(1R,2R)-2-{[4-(1,2-benzothiazol-3-yl)piperazin-1-yl]methyl}cyclohexyl]methyl}-4-azatricyclo[5.2.1.0²,⁶]decane-3,5-dione
SMILES
O=C1[[email protected]]2[C@@H]3CC[C@@H](C3)[[email protected]]2C(=O)N1C[C@@H]1CCCC[[email protected]]1CN1CCN(CC1)C1=NSC2=CC=CC=C12
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-arylpiperazines. These are organic compounds containing a piperazine ring where the nitrogen ring atom carries an aryl group.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassDiazinanes
Sub ClassPiperazines
Direct ParentN-arylpiperazines
Alternative Parents
Substituents
  • N-arylpiperazine
  • Norbornane monoterpenoid
  • Monoterpenoid
  • Isoindolone
  • Aromatic monoterpenoid
  • Isoindole or derivatives
  • Isoindoline
  • 1,2-benzothiazole
  • Dialkylarylamine
  • N-alkylpiperazine
  • Dicarboximide
  • Imidolactam
  • Benzenoid
  • N-alkylpyrrolidine
  • 2-pyrrolidone
  • Pyrrolidone
  • Carboxylic acid imide, n-substituted
  • Heteroaromatic compound
  • Thiazole
  • Pyrrolidine
  • Carboxylic acid imide
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Lactam
  • Carboxamide group
  • Azacycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationTreatment of schizophrenia.
PharmacodynamicsLurasidone is a benzothiazol derivative that is an antagonist and binds with high affinity to Dopamine-2 (D2) (Ki = 0.994 nM), 5-HT2A (Ki = 0.47 nM) receptors, and 5-HT7 receptors (Ki = 0.495 nM). It also binds with moderate affinity to alpha-2C adrenergic receptors (Ki = 10.8 nM) and is a partial agonist at 5-HT1A receptors (Ki = 6.38 nM). Its actions on histaminergic and muscarinic receptors are negligible.
Mechanism of actionLurasidone is an atypical antipsychotic that is a D2 and 5-HT2A (mixed serotonin and dopamine activity) to improve cognition. It is thought that antagonism of serotonin receptors can improve negative symptoms of psychoses and reduce the extrapyramidal side effects that are often associated with typical antipsychotics.
Related Articles
AbsorptionLurasidone is readily absorbed and quickly reaches maximal concentrations (Cmax) within 1-4 hours. When taken with food, there is a two-fold increase in exposure and time to maximal concentration is increased by 0.5-1.5 hours. This occurs regardless of fat or caloric content. Bioavailability = 9-19%.
Volume of distribution

6173 L

Protein binding~99% bound to serum proteins.
Metabolism

Lurasidone is metabolized by CYP3A4 in which its major active metabolite is referred to as ID-14283 (25% of parent exposure). Its two minor metabolites are referred to as ID14326 and ID11614 which make up 3% and 1% of parent exposure respectively. Its two non-active metabolites are referred to as ID-20219 and ID-20220.

SubstrateEnzymesProduct
Lurasidone
Not Available
ID11614Details
Lurasidone
Not Available
ID14326Details
Route of eliminationUrine (~9%) and feces (~80%)
Half life40 mg dose= 18 hours 120 mg - 160 mg dose = 29-37 hours
Clearance

3902 mL/min

ToxicityNot Available
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+1.0
Blood Brain Barrier+0.9907
Caco-2 permeable+0.5257
P-glycoprotein substrateSubstrate0.6029
P-glycoprotein inhibitor IInhibitor0.6713
P-glycoprotein inhibitor IIInhibitor0.73
Renal organic cation transporterInhibitor0.5487
CYP450 2C9 substrateNon-substrate0.7897
CYP450 2D6 substrateSubstrate0.8918
CYP450 3A4 substrateSubstrate0.5922
CYP450 1A2 substrateNon-inhibitor0.677
CYP450 2C9 inhibitorInhibitor0.6714
CYP450 2D6 inhibitorNon-inhibitor0.8292
CYP450 2C19 inhibitorInhibitor0.7439
CYP450 3A4 inhibitorNon-inhibitor0.7835
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.8126
Ames testNon AMES toxic0.6477
CarcinogenicityNon-carcinogens0.8986
BiodegradationNot ready biodegradable0.9959
Rat acute toxicity2.4051 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.6636
hERG inhibition (predictor II)Inhibitor0.5858
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletoral120 mg
Tabletoral20 mg
Tabletoral40 mg
Tabletoral60 mg
Tabletoral80 mg
Tablet, film coatedoral120 mg/1
Tablet, film coatedoral20 mg/1
Tablet, film coatedoral40 mg/1
Tablet, film coatedoral60 mg/1
Tablet, film coatedoral80 mg/1
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5532372 No1998-07-022018-07-02Us
US8729085 No2006-05-262026-05-26Us
US8883794 No2006-05-262026-05-26Us
US9174975 No2006-06-252026-06-25Us
US9259423 No2011-05-232031-05-23Us
USRE45573 No2005-06-232025-06-23Us
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
Water Solubility0.00789 mg/mLALOGPS
logP5.25ALOGPS
logP4.56ChemAxon
logS-4.8ALOGPS
pKa (Strongest Basic)8.5ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area56.75 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity139.33 m3·mol-1ChemAxon
Polarizability56.2 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
  2. Tarazi FI, Stahl SM: Iloperidone, asenapine and lurasidone: a primer on their current status. Expert Opin Pharmacother. 2012 Sep;13(13):1911-22. doi: 10.1517/14656566.2012.712114. Epub 2012 Jul 31. [PubMed:22849428 ]
External Links
ATC CodesN05AE05
AHFS Codes
  • 28:16.08.04
PDB EntriesNot Available
FDA labelDownload (452 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Lurasidone.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Lurasidone.
AmisulprideThe risk or severity of adverse effects can be increased when Lurasidone is combined with Amisulpride.
AmphetamineLurasidone may decrease the stimulatory activities of Amphetamine.
AprepitantThe serum concentration of Lurasidone can be increased when it is combined with Aprepitant.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Lurasidone.
AtazanavirThe serum concentration of Lurasidone can be increased when it is combined with Atazanavir.
AzelastineLurasidone may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
BaclofenThe risk or severity of adverse effects can be increased when Baclofen is combined with Lurasidone.
BexaroteneThe serum concentration of Lurasidone can be decreased when it is combined with Bexarotene.
BoceprevirThe serum concentration of Lurasidone can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Lurasidone can be decreased when it is combined with Bosentan.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Lurasidone.
BuprenorphineLurasidone may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Lurasidone.
CarbamazepineThe serum concentration of Lurasidone can be decreased when it is combined with Carbamazepine.
CathinoneLurasidone may decrease the stimulatory activities of Cathinone.
CeritinibThe serum concentration of Lurasidone can be increased when it is combined with Ceritinib.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Lurasidone.
ClarithromycinThe serum concentration of Lurasidone can be increased when it is combined with Clarithromycin.
CobicistatThe serum concentration of Lurasidone can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Lurasidone can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Lurasidone can be increased when it is combined with Crizotinib.
DabrafenibThe serum concentration of Lurasidone can be decreased when it is combined with Dabrafenib.
DarunavirThe serum concentration of Lurasidone can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Lurasidone can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Lurasidone can be decreased when it is combined with Deferasirox.
DelavirdineThe serum concentration of Lurasidone can be increased when it is combined with Delavirdine.
DiltiazemThe serum concentration of Lurasidone can be increased when it is combined with Diltiazem.
DisopyramideLurasidone may increase the QTc-prolonging activities of Disopyramide.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Lurasidone.
DopamineDopamine may increase the hypotensive activities of Lurasidone.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
DronedaroneThe serum concentration of Lurasidone can be increased when it is combined with Dronedarone.
DroperidolDroperidol may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
EnzalutamideThe serum concentration of Lurasidone can be decreased when it is combined with Enzalutamide.
EpinephrineEpinephrine may increase the hypotensive activities of Lurasidone.
ErythromycinThe serum concentration of Lurasidone can be increased when it is combined with Erythromycin.
EthanolLurasidone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Lurasidone.
FluconazoleThe serum concentration of Lurasidone can be increased when it is combined with Fluconazole.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Lurasidone.
FosamprenavirThe serum concentration of Lurasidone can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Lurasidone can be increased when it is combined with Fosaprepitant.
FosphenytoinThe serum concentration of Lurasidone can be decreased when it is combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Lurasidone can be increased when it is combined with Fusidic Acid.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Lurasidone.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Lurasidone.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Lurasidone.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Lurasidone.
HydrocodoneLurasidone may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
IdelalisibThe serum concentration of Lurasidone can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Lurasidone can be increased when it is combined with Imatinib.
IndinavirThe serum concentration of Lurasidone can be increased when it is combined with Indinavir.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Lurasidone.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Lurasidone.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Lurasidone.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Lurasidone.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Lurasidone.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Lurasidone.
IsavuconazoniumThe serum concentration of Lurasidone can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Lurasidone can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Lurasidone can be increased when it is combined with Ivacaftor.
KetoconazoleThe serum concentration of Lurasidone can be increased when it is combined with Ketoconazole.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Lurasidone.
LithiumLithium may increase the neurotoxic activities of Lurasidone.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Lurasidone.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Lurasidone.
LuliconazoleThe serum concentration of Lurasidone can be increased when it is combined with Luliconazole.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
MequitazineLurasidone may increase the arrhythmogenic activities of Mequitazine.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Lurasidone.
MethotrimeprazineLurasidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Lurasidone is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Lurasidone.
MetyrosineLurasidone may increase the sedative activities of Metyrosine.
MifepristoneThe serum concentration of Lurasidone can be increased when it is combined with Mifepristone.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
MirtazapineLurasidone may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
MitotaneThe serum concentration of Lurasidone can be decreased when it is combined with Mitotane.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
NefazodoneThe serum concentration of Lurasidone can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Lurasidone can be increased when it is combined with Nelfinavir.
NilotinibThe serum concentration of Lurasidone can be increased when it is combined with Nilotinib.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Lurasidone.
OrphenadrineLurasidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
PalbociclibThe serum concentration of Lurasidone can be increased when it is combined with Palbociclib.
ParaldehydeLurasidone may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineThe risk or severity of adverse effects can be increased when Lurasidone is combined with Paroxetine.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Lurasidone.
PhenobarbitalThe serum concentration of Lurasidone can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Lurasidone can be decreased when it is combined with Phenytoin.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Lurasidone.
PosaconazoleThe serum concentration of Lurasidone can be increased when it is combined with Posaconazole.
PrimidoneThe serum concentration of Lurasidone can be decreased when it is combined with Primidone.
ProcainamideLurasidone may increase the QTc-prolonging activities of Procainamide.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Lurasidone.
QuinidineLurasidone may increase the QTc-prolonging activities of Quinidine.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Lurasidone.
RifabutinThe serum concentration of Lurasidone can be decreased when it is combined with Rifabutin.
RifampicinThe serum concentration of Lurasidone can be decreased when it is combined with Rifampicin.
RifapentineThe serum concentration of Lurasidone can be decreased when it is combined with Rifapentine.
RitonavirThe serum concentration of Lurasidone can be increased when it is combined with Ritonavir.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Lurasidone.
SaquinavirThe serum concentration of Lurasidone can be increased when it is combined with Saquinavir.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Lurasidone.
SiltuximabThe serum concentration of Lurasidone can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Lurasidone can be increased when it is combined with Simeprevir.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
St. John's WortThe serum concentration of Lurasidone can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Lurasidone can be increased when it is combined with Stiripentol.
SulpirideThe risk or severity of adverse effects can be increased when Lurasidone is combined with Sulpiride.
SuvorexantLurasidone may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineTacrine may increase the central neurotoxic activities of Lurasidone.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Lurasidone.
TelaprevirThe serum concentration of Lurasidone can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Lurasidone can be increased when it is combined with Telithromycin.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Lurasidone.
ThalidomideLurasidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TocilizumabThe serum concentration of Lurasidone can be decreased when it is combined with Tocilizumab.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Lurasidone.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Lurasidone.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Lurasidone.
VerapamilThe serum concentration of Lurasidone can be increased when it is combined with Verapamil.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Lurasidone.
VoriconazoleThe serum concentration of Lurasidone can be increased when it is combined with Voriconazole.
ZolpidemLurasidone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • When taken with food, there is a two-fold increase in exposure and time to maximal concentration is increased by 0.5-1.5 hours.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Potassium channel regulator activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name:
DRD2
Uniprot ID:
P14416
Molecular Weight:
50618.91 Da
References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Virus receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
Molecular Weight:
52602.58 Da
References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
Molecular Weight:
53554.43 Da
References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Serotonin receptor activity
Specific Function:
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
Molecular Weight:
46106.335 Da
References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
Protein homodimerization activity
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name:
ADRA2C
Uniprot ID:
P18825
Molecular Weight:
49521.585 Da
References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Thioesterase binding
Specific Function:
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
Molecular Weight:
48956.275 Da
References
  1. Tarazi FI, Stahl SM: Iloperidone, asenapine and lurasidone: a primer on their current status. Expert Opin Pharmacother. 2012 Sep;13(13):1911-22. doi: 10.1517/14656566.2012.712114. Epub 2012 Jul 31. [PubMed:22849428 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
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 performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. George M, Amrutheshwar R, Rajkumar RP, Kattimani S, Dkhar SA: Newer antipsychotics and upcoming molecules for schizophrenia. Eur J Clin Pharmacol. 2013 Aug;69(8):1497-509. doi: 10.1007/s00228-013-1498-4. Epub 2013 Apr 2. [PubMed:23545936 ]
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Drug created on July 24, 2011 11:04 / Updated on June 29, 2016 02:25