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Identification
NameOlanzapine
Accession NumberDB00334  (APRD00138)
Typesmall molecule
Groupsapproved, investigational
Description

Olanzapine is an atypical antipsychotic, approved by the FDA in 1996. Olanzapine is manufactured and marketed by the pharmaceutical company Eli Lilly and Company, whose patent for olanzapine proper ends in 2011.

Structure
Thumb
Synonyms
SynonymLanguageCode
2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepineNot AvailableIUPAC
OlanzapinNot AvailablePh. Eur. 7
OlanzapineNot AvailableUSAN, BAN, Ph. Eur. 7, USP 34
OlanzapinumNot AvailablePh. Eur. 7
Salts
Name/CAS Structure Properties
Olanzapine pamoate
Thumb Not applicable DBSALT001064
Brand names
NameCompany
AedonG.L. Pharma
AmulsinSanitas
ApiscoLKM
ApsicoLKM
ArkolamylMylan
CaprilonLavipharm
CO OlanzapineCobalt
DeprexSquare
DominazolStein
DopinDaksh
EgolanzaEGIS
ElynzaElynza
FrenialBiogen
Jolyon-MDLupin
KozylexQuisisana
LanopinMolekule
LanzapinBiogened
LanzepRenata
LapenzaSmart Intermed
LapozanMedochemie
LazapixPortfarma
ZyprexaLilly
Brand mixtures
Brand NameIngredients
Depten-OZOlanzapine and Fluoxetine
SymbyaxOlanzapine and Fluoxetine
CategoriesNot Available
CAS number132539-06-1
WeightAverage: 312.432
Monoisotopic: 312.14086735
Chemical FormulaC17H20N4S
InChI KeyInChIKey=KVWDHTXUZHCGIO-UHFFFAOYSA-N
InChI
InChI=1S/C17H20N4S/c1-12-11-13-16(21-9-7-20(2)8-10-21)18-14-5-3-4-6-15(14)19-17(13)22-12/h3-6,11,19H,7-10H2,1-2H3
IUPAC Name
5-methyl-8-(4-methylpiperazin-1-yl)-4-thia-2,9-diazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),3(7),5,8,10,12-hexaene
SMILES
CN1CCN(CC1)C1=NC2=CC=CC=C2NC2=C1C=C(C)S2
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassHeterocyclic Compounds
ClassThienodiazepines
SubclassNot Available
Direct parentThienodiazepines
Alternative parents1,4-Diazepines; Piperazines; Diazinanes; Benzene and Substituted Derivatives; Thiophenes; Tertiary Amines; Carboxamidines; Polyamines; Secondary Amines
Substituentspara-diazepine; benzene; 1,4-diazinane; piperazine; thiophene; tertiary amine; secondary amine; polyamine; amidine; carboxylic acid amidine; amine; organonitrogen compound
Classification descriptionThis compound belongs to the thienodiazepines. These are heteropolycyclic containing a thiophene ring fused to a diazepine ring.
Pharmacology
IndicationFor the acute and maintenance treatment of schizophrenia and related psychotic disorders, as well as acute treatment of manic or mixed episodes of bipolar 1 disorder. Intramuscular olanzapine is indicated for the rapid control of agitated patients.
PharmacodynamicsOlanzapine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, olanzapine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors.
Mechanism of actionOlanzapine's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia.
AbsorptionWell absorbed, with approximately 40% of the dose metabolized before reaching the systemic circulation.
Volume of distribution
  • 1000 L
Protein binding93%
Metabolism

Hepatic

SubstrateEnzymesProduct
Olanzapine
7-hydroxyolanzapineDetails
Olanzapine
4'-N-desmethylolanzapineDetails
Olanzapine
2-hydroxymethylolanzapineDetails
Route of eliminationIt is eliminated extensively by first pass metabolism, with approximately 40% of the dose metabolized before reaching the systemic circulation. Following a single oral dose of 14C labeled olanzapine, 7% of the dose of olanzapine was recovered in the urine as unchanged drug, indicating that olanzapine is highly metabolized.
Half life21 to 54 hours
Clearance
  • 12 to 47 L/h
ToxicitySymptoms of an overdose include tachycardia, agitation, dysarthria, decreased consciousness and coma. Death has been reported after an acute overdose of 0.45g, but also survival after an acute overdose of 1500g.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated Effects
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeEffectReference(s)
5-hydroxytryptamine receptor 1A
Gene symbol: HTR1A
UniProt: P08908
rs6295 Not AvailableCC Allele (homozygous)Associated with the ability to ameliorate impaired attention in patients with schizophrenia.20533011
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.9645
Blood Brain Barrier + 0.9652
Caco-2 permeable + 0.5993
P-glycoprotein substrate Substrate 0.8524
P-glycoprotein inhibitor I Inhibitor 0.6888
P-glycoprotein inhibitor II Inhibitor 0.7204
Renal organic cation transporter Inhibitor 0.7715
CYP450 2C9 substrate Non-substrate 0.7493
CYP450 2D6 substrate Substrate 0.8918
CYP450 3A4 substrate Substrate 0.5421
CYP450 1A2 substrate Inhibitor 0.6454
CYP450 2C9 substrate Non-inhibitor 0.6914
CYP450 2D6 substrate Inhibitor 0.608
CYP450 2C19 substrate Inhibitor 0.572
CYP450 3A4 substrate Non-inhibitor 0.9526
CYP450 inhibitory promiscuity High CYP Inhibitory Promiscuity 0.707
Ames test Non AMES toxic 0.7009
Carcinogenicity Non-carcinogens 0.9369
Biodegradation Not ready biodegradable 1.0
Rat acute toxicity 2.6972 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9483
hERG inhibition (predictor II) Inhibitor 0.7569
Pharmacoeconomics
Manufacturers
  • Eli lilly and co
Packagers
Dosage forms
FormRouteStrength
Powder, for solutionIntramuscular
TabletOral
Tablet, orally disintegratingOral
Prices
Unit descriptionCostUnit
Zyprexa relprevv 405 mg vial1287.9USDvial
Zyprexa relprevv 300 mg vial954.0USDvial
Zyprexa relprevv 210 mg vial667.8USDvial
ZyPREXA Zydis 30 10 mg Dispersible Tablet Box562.35USDbox
ZyPREXA Zydis 30 5 mg Dispersible Tablet Box385.63USDbox
Zyprexa 10 mg vial35.69USDvial
Zyprexa zydis 20 mg tablet34.87USDtablet
Zyprexa 20 mg tablet34.37USDtablet
Zyprexa zydis 15 mg tablet26.45USDtablet
Zyprexa 15 mg tablet21.14USDtablet
Symbyax 12-25 mg capsule20.62USDcapsule
Symbyax 12-50 mg capsule20.62USDcapsule
Zyprexa zydis 10 mg tablet18.02USDtablet
Symbyax 6-50 mg capsule14.56USDcapsule
Zyprexa 10 mg tablet14.09USDtablet
Symbyax 6-25 mg capsule13.69USDcapsule
Zyprexa zydis 5 mg tablet12.36USDtablet
Zyprexa 7.5 mg tablet11.23USDtablet
Symbyax 3-25 mg capsule10.01USDcapsule
Zyprexa 5 mg tablet8.92USDtablet
Zyprexa Zydis 10 mg Disintegrating Tablet7.86USDtablet
Zyprexa 2.5 mg tablet7.1USDtablet
Apo-Olanzapine 15 mg Tablet6.64USDtablet
Co Olanzapine 15 mg Tablet6.64USDtablet
Novo-Olanzapine 15 mg Tablet6.64USDtablet
Pms-Olanzapine 15 mg Tablet6.64USDtablet
Apo-Olanzapine 10 mg Tablet4.43USDtablet
Co Olanzapine 10 mg Tablet4.43USDtablet
Novo-Olanzapine 10 mg Tablet4.43USDtablet
Pms-Olanzapine 10 mg Tablet4.43USDtablet
Zyprexa Zydis 5 mg Disintegrating Tablet3.93USDtablet
Co Olanzapine Odt 10 mg Disintegrating Tablet3.54USDtablet
Novo-Olanzapine Od 10 mg Disintegrating Tablet3.54USDtablet
Pms-Olanzapine Odt 10 mg Disintegrating Tablet3.54USDtablet
Sandoz Olanzapine Odt 10 mg Disintegrating Tablet3.54USDtablet
Apo-Olanzapine 7.5 mg Tablet3.32USDtablet
Co Olanzapine 7.5 mg Tablet3.32USDtablet
Novo-Olanzapine 7.5 mg Tablet3.32USDtablet
Pms-Olanzapine 7.5 mg Tablet3.32USDtablet
Apo-Olanzapine 5 mg Tablet2.21USDtablet
Co Olanzapine 5 mg Tablet2.21USDtablet
Novo-Olanzapine 5 mg Tablet2.21USDtablet
Pms-Olanzapine 5 mg Tablet2.21USDtablet
Co Olanzapine Odt 5 mg Disintegrating Tablet1.77USDtablet
Novo-Olanzapine Od 5 mg Disintegrating Tablet1.77USDtablet
Pms-Olanzapine Odt 5 mg Disintegrating Tablet1.77USDtablet
Sandoz Olanzapine Odt 5 mg Disintegrating Tablet1.77USDtablet
Apo-Olanzapine 2.5 mg Tablet1.11USDtablet
Co Olanzapine 2.5 mg Tablet1.11USDtablet
Novo-Olanzapine 2.5 mg Tablet1.11USDtablet
Pms-Olanzapine 2.5 mg Tablet1.11USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States62518951998-03-232018-03-23
United States52293821994-04-232011-04-23
Canada22163722007-11-202016-03-22
Canada20411131998-07-142011-04-24
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point195 °CNot Available
logP2Not Available
Predicted Properties
PropertyValueSource
water solubility9.42e-02 g/lALOGPS
logP3.61ALOGPS
logP3.39ChemAxon
logS-3.5ALOGPS
pKa (strongest acidic)14.17ChemAxon
pKa (strongest basic)7.24ChemAxon
physiological charge1ChemAxon
hydrogen acceptor count4ChemAxon
hydrogen donor count1ChemAxon
polar surface area30.87ChemAxon
rotatable bond count0ChemAxon
refractivity93.87ChemAxon
polarizability35.37ChemAxon
number of rings4ChemAxon
bioavailability1ChemAxon
rule of fiveYesChemAxon
Ghose filterYesChemAxon
Veber's ruleYesChemAxon
MDDR-like ruleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

Charles Arthur Bunnell, Samuel Dean Larsen, John Richard Nichols, Susan Marie Reutzel, Gregory Alan Stephenson, “Intermediates and process for preparing olanzapine.” U.S. Patent US6020487, issued September, 1996.

US6020487
General Reference
  1. de Haan L, van Amelsvoort T, Rosien K, Linszen D: Weight loss after switching from conventional olanzapine tablets to orally disintegrating olanzapine tablets. Psychopharmacology (Berl). 2004 Sep;175(3):389-90. Pubmed
  2. Pollack MH, Simon NM, Zalta AK, Worthington JJ, Hoge EA, Mick E, Kinrys G, Oppenheimer J: Olanzapine augmentation of fluoxetine for refractory generalized anxiety disorder: a placebo controlled study. Biol Psychiatry. 2006 Feb 1;59(3):211-5. Epub 2005 Sep 1. Pubmed
  3. Sepede G, De Berardis D, Gambi F, Campanella D, La Rovere R, D’Amico M, Cicconetti A, Penna L, Peca S, Carano A, Mancini E, Salerno RM, Ferro FM: Olanzapine augmentation in treatment-resistant panic disorder: a 12-week, fixed-dose, open-label trial. J Clin Psychopharmacol. 2006 Feb;26(1):45-9. Pubmed
  4. Jakovljevic M, Sagud M, Mihaljevic-Peles A: Olanzapine in the treatment-resistant, combat-related PTSD—a series of case reports. Acta Psychiatr Scand. 2003 May;107(5):394-6; discussion 396. Pubmed
  5. McGlashan TH, Zipursky RB, Perkins D, Addington J, Miller TJ, Woods SW, Hawkins KA, Hoffman R, Lindborg S, Tohen M, Breier A: The PRIME North America randomized double-blind clinical trial of olanzapine versus placebo in patients at risk of being prodromally symptomatic for psychosis. I. Study rationale and design. Schizophr Res. 2003 May 1;61(1):7-18. Pubmed
External Links
ResourceLink
KEGG DrugD00454
KEGG CompoundC07322
BindingDB35254
ChEBI7735
ChEMBLCHEMBL715
Therapeutic Targets DatabaseDAP000022
PharmGKBPA450688
IUPHAR47
Guide to Pharmacology47
Drug Product Database2247099
RxListhttp://www.rxlist.com/cgi/generic3/symbyax.htm
Drugs.comhttp://www.drugs.com/cdi/olanzapine.html
WikipediaOlanzapine
ATC CodesN05AH03
AHFS Codes
  • 28:16.08.04
PDB EntriesNot Available
FDA labelshow(251 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
DonepezilPossible antagonism of action
FluvoxamineFluvoxamine increases the effect and toxicity of olanzapine
GalantaminePossible antagonism of action
RitonavirRitonavir decreases the effect of olanzapine
RivastigminePossible antagonism of action
TacrineThe therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Olanzapine, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
TetrabenazineMay cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
TrimethobenzamideTrimethobenzamide and Olanzapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
TriprolidineTriprolidine and Olanzapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
TrospiumTrospium and Olanzapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Food Interactions
  • Avoid alcohol.
  • Take without regard to meals.

1. 5-hydroxytryptamine receptor 2A

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2A P28223 Details

References:

  1. McDonald LM, Moran PM, Vythelingum GN, Joseph MH, Stephenson JD, Gray JA: Enhancement of latent inhibition by two 5-HT2A receptor antagonists only when given at both pre-exposure and conditioning. Psychopharmacology (Berl). 2003 Sep;169(3-4):321-31. Epub 2002 Aug 9. Pubmed
  2. Moresco RM, Cavallaro R, Messa C, Bravi D, Gobbo C, Galli L, Lucignani G, Colombo C, Rizzo G, Velona I, Smeraldi E, Fazio F: Cerebral D2 and 5-HT2 receptor occupancy in Schizophrenic patients treated with olanzapine or clozapine. J Psychopharmacol. 2004 Sep;18(3):355-65. Pubmed
  3. Sharpley AL, Attenburrow ME, Hafizi S, Cowen PJ: Olanzapine increases slow wave sleep and sleep continuity in SSRI-resistant depressed patients. J Clin Psychiatry. 2005 Apr;66(4):450-4. Pubmed
  4. Yatham LN, Goldstein JM, Vieta E, Bowden CL, Grunze H, Post RM, Suppes T, Calabrese JR: Atypical antipsychotics in bipolar depression: potential mechanisms of action. J Clin Psychiatry. 2005;66 Suppl 5:40-8. Pubmed
  5. Padin JF, Rodriguez MA, Dominguez E, Dopeso-Reyes IG, Buceta M, Cano E, Sotelo E, Brea J, Caruncho HJ, Isabel Cadavid M, Castro M, Isabel Loza M: Parallel regulation by olanzapine of the patterns of expression of 5-HT2A and D3 receptors in rat central nervous system and blood cells. Neuropharmacology. 2006 Sep;51(4):923-32. Epub 2006 Aug 14. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  7. Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. Pubmed
  8. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  9. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

2. D(2) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist agonist

Components

Name UniProt ID Details
D(2) dopamine receptor P14416 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Naiker DV, Catts SV, Catts VS, Bedi KS, Bryan-Lluka LJ: Dose determination of haloperidol, risperidone and olanzapine using an in vivo dopamine D2-receptor occupancy method in the rat. Eur J Pharmacol. 2006 Jul 1;540(1-3):87-90. Epub 2006 May 11. Pubmed
  3. Weizman T, Pick CG, Backer MM, Rigai T, Bloch M, Schreiber S: The antinociceptive effect of amisulpride in mice is mediated through opioid mechanisms. Eur J Pharmacol. 2003 Oct 8;478(2-3):155-9. Pubmed
  4. Jordan S, Regardie K, Johnson JL, Chen R, Kambayashi J, McQuade R, Kitagawa H, Tadori Y, Kikuchi T: In vitro functional characteristics of dopamine D2 receptor partial agonists in second and third messenger-based assays of cloned human dopamine D2Long receptor signalling. J Psychopharmacol. 2007 Aug;21(6):620-7. Epub 2006 Nov 8. Pubmed
  5. Thacker SK, Perna MK, Ward JJ, Schaefer TL, Williams MT, Kostrzewa RM, Brown RW: The effects of adulthood olanzapine treatment on cognitive performance and neurotrophic factor content in male and female rats neonatally treated with quinpirole. Eur J Neurosci. 2006 Oct;24(7):2075-83. Pubmed
  6. Lencz T, Robinson DG, Xu K, Ekholm J, Sevy S, Gunduz-Bruce H, Woerner MG, Kane JM, Goldman D, Malhotra AK: DRD2 promoter region variation as a predictor of sustained response to antipsychotic medication in first-episode schizophrenia patients. Am J Psychiatry. 2006 Mar;163(3):529-31. Pubmed
  7. Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. Pubmed
  8. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

3. D(1A) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(1A) dopamine receptor P21728 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  3. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

4. D(1B) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(1B) dopamine receptor P21918 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  2. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

5. D(3) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(3) dopamine receptor P35462 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

6. D(4) dopamine receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
D(4) dopamine receptor P21917 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Hutchison KE, Ray L, Sandman E, Rutter MC, Peters A, Davidson D, Swift R: The effect of olanzapine on craving and alcohol consumption. Neuropsychopharmacology. 2006 Jun;31(6):1310-7. Pubmed

7. 5-hydroxytryptamine receptor 1A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1A P08908 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

8. 5-hydroxytryptamine receptor 1B

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1B P28222 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

9. 5-hydroxytryptamine receptor 1D

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1D P28221 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

10. 5-hydroxytryptamine receptor 1E

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 1E P28566 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

11. 5-hydroxytryptamine receptor 2C

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2C P28335 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Zhang JY, Kowal DM, Nawoschik SP, Lou Z, Dunlop J: Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms. Biochem Pharmacol. 2006 Feb 14;71(4):521-9. Epub 2005 Dec 5. Pubmed
  3. Overstreet DH, Knapp DJ, Breese GR: Drug challenges reveal differences in mediation of stress facilitation of voluntary alcohol drinking and withdrawal-induced anxiety in alcohol-preferring P rats. Alcohol Clin Exp Res. 2007 Sep;31(9):1473-81. Epub 2007 Jul 11. Pubmed
  4. Theisen FM, Haberhausen M, Firnges MA, Gregory P, Reinders JH, Remschmidt H, Hebebrand J, Antel J: No evidence for binding of clozapine, olanzapine and/or haloperidol to selected receptors involved in body weight regulation. Pharmacogenomics J. 2007 Aug;7(4):275-81. Epub 2006 Sep 19. Pubmed
  5. Wood MD, Scott C, Clarke K, Cato KJ, Patel N, Heath J, Worby A, Gordon L, Campbell L, Riley G, Davies CH, Gribble A, Jones DN: Pharmacological profile of antipsychotics at monoamine receptors: atypicality beyond 5-HT2A receptor blockade. CNS Neurol Disord Drug Targets. 2006 Aug;5(4):445-52. Pubmed
  6. Hertel P: Comparing sertindole to other new generation antipsychotics on preferential dopamine output in limbic versus striatal projection regions: mechanism of action. Synapse. 2006 Dec 1;60(7):543-52. Pubmed
  7. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

12. 5-hydroxytryptamine receptor 3A

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 3A P46098 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

13. 5-hydroxytryptamine receptor 6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 6 P50406 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

14. 5-hydroxytryptamine receptor 7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 7 P34969 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

15. Histamine H1 receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Histamine H1 receptor P35367 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Poyurovsky M, Pashinian A, Levi A, Weizman R, Weizman A: The effect of betahistine, a histamine H1 receptor agonist/H3 antagonist, on olanzapine-induced weight gain in first-episode schizophrenia patients. Int Clin Psychopharmacol. 2005 Mar;20(2):101-3. Pubmed
  3. Rasmussen K, Benvenga MJ, Bymaster FP, Calligaro DO, Cohen IR, Falcone JF, Hemrick-Luecke SK, Martin FM, Moore NA, Nisenbaum LK, Schaus JM, Sundquist SJ, Tupper DE, Wiernicki TR, Nelson DL: Preclinical pharmacology of FMPD [6-fluoro-10-[3-(2-methoxyethyl)-4-methyl-piperazin-1-yl]-2-methyl-4H-3-th ia-4,9-diaza-benzo[f]azulene]: a potential novel antipsychotic with lower histamine H1 receptor affinity than olanzapine. J Pharmacol Exp Ther. 2005 Dec;315(3):1265-77. Epub 2005 Sep 1. Pubmed
  4. Altschuler EL, Kast RE: Using histamine (H1) antagonists, in particular atypical antipsychotics, to treat anemia of chronic disease via interleukin-6 suppression. Med Hypotheses. 2005;65(1):65-7. Pubmed
  5. Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. Pubmed
  6. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

16. Alpha-1A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1A adrenergic receptor P35348 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  2. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

17. Alpha-1B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-1B adrenergic receptor P35368 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. Pubmed
  3. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  4. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

18. Alpha-2A adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2A adrenergic receptor P08913 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

19. Alpha-2B adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2B adrenergic receptor P18089 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

20. Alpha-2C adrenergic receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Alpha-2C adrenergic receptor P18825 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed

21. Muscarinic acetylcholine receptor M1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M1 P11229 Details

References:

  1. Uchida S, Kato Y, Hirano K, Kagawa Y, Yamada S: Brain neurotransmitter receptor-binding characteristics in rats after oral administration of haloperidol, risperidone and olanzapine. Life Sci. 2007 Apr 3;80(17):1635-40. Epub 2007 Jan 27. Pubmed
  2. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  3. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

22. Muscarinic acetylcholine receptor M2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M2 P08172 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  2. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

23. Muscarinic acetylcholine receptor M3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M3 P20309 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  2. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

24. Muscarinic acetylcholine receptor M4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M4 P08173 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  2. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

25. Muscarinic acetylcholine receptor M5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Muscarinic acetylcholine receptor M5 P08912 Details

References:

  1. Nasrallah HA: Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles. Mol Psychiatry. 2008 Jan;13(1):27-35. Epub 2007 Sep 11. Pubmed
  2. Bymaster FP, Nelson DL, DeLapp NW, Falcone JF, Eckols K, Truex LL, Foreman MM, Lucaites VL, Calligaro DO: Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro. Schizophr Res. 1999 May 4;37(1):107-22. Pubmed

1. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM: Olanzapine. Pharmacokinetic and pharmacodynamic profile. Clin Pharmacokinet. 1999 Sep;37(3):177-93. Pubmed
  2. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  3. Pelkonen O, Maenpaa J, Taavitsainen P, Rautio A, Raunio H: Inhibition and induction of human cytochrome P450 (CYP) enzymes. Xenobiotica. 1998 Dec;28(12):1203-53. Pubmed
  4. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  5. Carrillo JA, Benitez J: Clinically significant pharmacokinetic interactions between dietary caffeine and medications. Clin Pharmacokinet. 2000 Aug;39(2):127-53. Pubmed

2. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM: Olanzapine. Pharmacokinetic and pharmacodynamic profile. Clin Pharmacokinet. 1999 Sep;37(3):177-93. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

3. Dimethylaniline monooxygenase [N-oxide-forming] 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Dimethylaniline monooxygenase [N-oxide-forming] 3 P31513 Details

References:

  1. Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM: Olanzapine. Pharmacokinetic and pharmacodynamic profile. Clin Pharmacokinet. 1999 Sep;37(3):177-93. Pubmed

4. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

5. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

6. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

1. Serum albumin

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Serum albumin P02768 Details

References:

  1. Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM: Olanzapine. Pharmacokinetic and pharmacodynamic profile. Clin Pharmacokinet. 1999 Sep;37(3):177-93. Pubmed

2. Alpha-1-acid glycoprotein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Alpha-1-acid glycoprotein 1 P02763 Details

References:

  1. Callaghan JT, Bergstrom RF, Ptak LR, Beasley CM: Olanzapine. Pharmacokinetic and pharmacodynamic profile. Clin Pharmacokinet. 1999 Sep;37(3):177-93. Pubmed

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Boulton DW, DeVane CL, Liston HL, Markowitz JS: In vitro P-glycoprotein affinity for atypical and conventional antipsychotics. Life Sci. 2002 May 31;71(2):163-9. Pubmed

Comments
Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:09