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Identification
NameAsenapine
Accession NumberDB06216
TypeSmall Molecule
GroupsApproved
Description

Developed by Schering-Plough after its merger with Organon International, asenapine is a sublingually administered, atypical antipsychotic for treatment of schizophrenia and acute mania associated with bipolar disorder. Asenapine also belongs to the dibenzo-oxepino pyrrole class. It is also for severe post-traumatic stress disorder nightmares in soldiers as an off-label use. FDA approved on August 13, 2009.

Structure
Thumb
Synonyms
Saphris
External Identifiers
  • ORG-5222
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Saphristablet5 mg/1sublingualOrganon Pharmaceuticals USA2009-08-13Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Saphristablet10 mg/1sublingualSTAT Rx USA LLC2009-08-14Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Saphristablet10 mg/1sublingualForest Laboratories, Inc.2013-09-30Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Saphristablet5 mg/1sublingualForest Laboratories, Inc.2013-09-30Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Saphristablet2.5 mg/1sublingualForest Laboratories, Inc.2014-12-30Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Saphristablet10 mg/1sublingualOrganon Pharmaceuticals USA2010-06-21Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Saphristablet5 mg/1sublingualOrganon Pharmaceuticals USA2010-06-21Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Saphristablet10 mgsublingualMerck Canada Inc2011-12-19Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Saphristablet10 mg/1sublingualOrganon Pharmaceuticals USA2009-08-13Not applicableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Saphristablet5 mgsublingualMerck Canada Inc2011-12-19Not applicableCanada 5f16b84899037e23705f146ff57e3794121879cb055f0954756d94bc690476b4
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
Sycrest Lundbeck
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Asenapine Maleate
Thumb
  • InChI Key: GMDCDXMAFMEDAG-CHHFXETESA-N
  • Monoisotopic Mass: 401.103000462
  • Average Mass: 401.84
DBSALT000010
CategoriesNot Available
CAS number65576-45-6
WeightAverage: 401.84
Monoisotopic: 401.103000462
Chemical FormulaC21H20ClNO5
InChI KeyInChIKey=GMDCDXMAFMEDAG-BTJKTKAUSA-N
InChI
InChI=1S/C17H16ClNO.C4H4O4/c1-19-9-14-12-4-2-3-5-16(12)20-17-7-6-11(18)8-13(17)15(14)10-19;5-3(6)1-2-4(7)8/h2-8,14-15H,9-10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
IUPAC Name
(2Z)-but-2-enedioic acid; 17-chloro-4-methyl-13-oxa-4-azatetracyclo[12.4.0.0²,⁶.0⁷,¹²]octadeca-1(14),7,9,11,15,17-hexaene
SMILES
OC(=O)\C=C/C(O)=O.CN1CC2C(C1)C1=C(OC3=CC=CC=C23)C=CC(Cl)=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dibenzoxepines. These are compounds containing a dibenzoxepine moiety, which consists of two benzene connected by an oxazepine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzoxepines
Sub ClassDibenzoxepines
Direct ParentDibenzoxepines
Alternative Parents
Substituents
  • Dibenzoxepine
  • Diaryl ether
  • Aralkylamine
  • Chlorobenzene
  • Fatty acyl
  • Fatty acid
  • Benzenoid
  • N-alkylpyrrolidine
  • Unsaturated fatty acid
  • Dicarboxylic acid or derivatives
  • Aryl halide
  • Aryl chloride
  • Pyrrolidine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Oxacycle
  • Azacycle
  • Ether
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organochloride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
  • Aliphatic acyclic compound
Molecular FrameworkNot Available
External DescriptorsNot Available
Pharmacology
IndicationUsed for treatment in psychosis, schizophrenia and schizoaffective disorders, manic disorders, and bipolar disorders as monotherapy or in combination.
PharmacodynamicsAsenapine is a serotonin, dopamine, noradrenaline, and histamine antagonist in which asenapine possess more potent activity with serotonin receptors than dopamine. Sedation in patients is associated with asenapine's antagonist activity at histamine receptors. Its lower incidence of extrapyramidal effects are associated with the upregulation of D1 receptors. This upregulation occurs due to asenapine's dose-dependent effects on glutamate transmission in the brain. It does not have any significant activity with muscarinic, cholinergic receptors therefore symptoms associated with anticholinergic drug activity like dry mouth or constipation are not expected to be observed. Asenapine has a higher affinity for all aforementioned receptors compared to first-generation and second-generation antipsychotics except for 5-HT1A and 5-HT1B receptors.
Mechanism of actionAsenapine is an atypical antipsychotic multireceptor neuroleptic drug which shows strong 5HT2A (serotonin) and D2 (dopamine) receptor antagonism, which has been shown to enhance dopamine (DA) and acetylcholine (Ach) efflux in rat brains. Asenapine may improve cognitive function and negative symptoms in patients with schizophrenia.
AbsorptionCmax, single 5 mg dose = 4 ng/mL (within 1 hour); Bioavailability, sublingual administration = 35%; Bioavailability, oral administration (swallowed) = <2%; Time to steady state, 5 mg = 3 days; Peak plasma concentration occurs within 0.5 to 1.5 hours. Doubling dose of asenapine results in 1.7-fold increase in maximum concentration and exposure. Drinking water within 2-5 minutes post administration of asenapine results in a decrease in exposure.
Volume of distribution

20-25 L/kg

Protein binding95% protein bound
Metabolism

Asenapine is oxidized via CYP1A2 and undergoes direct glucuronidation via UGT1A4. Oxidation via CYP1A2 is asenapine's primary mode of metabolism.

Route of eliminationUrine (50%) and feces (50%)
Half life24 hours (range of 13.4 - 39.2 hours)
ClearanceNot Available
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+0.9849
Blood Brain Barrier+0.8842
Caco-2 permeable+0.5605
P-glycoprotein substrateSubstrate0.7617
P-glycoprotein inhibitor INon-inhibitor0.9375
P-glycoprotein inhibitor IINon-inhibitor0.8901
Renal organic cation transporterNon-inhibitor0.7054
CYP450 2C9 substrateNon-substrate0.7964
CYP450 2D6 substrateNon-substrate0.7864
CYP450 3A4 substrateSubstrate0.5065
CYP450 1A2 substrateNon-inhibitor0.5212
CYP450 2C9 inhibitorNon-inhibitor0.7185
CYP450 2D6 inhibitorNon-inhibitor0.6781
CYP450 2C19 inhibitorNon-inhibitor0.5762
CYP450 3A4 inhibitorNon-inhibitor0.8625
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6005
Ames testNon AMES toxic0.5417
CarcinogenicityNon-carcinogens0.8694
BiodegradationNot ready biodegradable0.9894
Rat acute toxicity2.7083 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8125
hERG inhibition (predictor II)Non-inhibitor0.6697
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tabletsublingual10 mg/1
Tabletsublingual10 mg
Tabletsublingual2.5 mg/1
Tabletsublingual5 mg/1
Tabletsublingual5 mg
PricesNot Available
Patents
CountryPatent NumberApprovedExpires (estimated)
United States57634761995-06-092015-06-09
United States77413582006-04-062026-04-06
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
logP3.72ChemAxon
pKa (Strongest Basic)7.29ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.47 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity81.65 m3·mol-1ChemAxon
Polarizability30.9 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US4145434
General References
  1. Huang M, Li Z, Dai J, Shahid M, Wong EH, Meltzer HY: Asenapine Increases Dopamine, Norepinephrine, and Acetylcholine Efflux in the Rat Medial Prefrontal Cortex and Hippocampus. Neuropsychopharmacology. 2008 Apr 16;. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologicagent with a unique human receptor signature. J Psychopharmacol. 2008 Feb 28;. Pubmed
  3. Franberg O, Wiker C, Marcus MM, Konradsson A, Jardemark K, Schilstrom B, Shahid M, Wong EH, Svensson TH: Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Psychopharmacology (Berl). 2008 Feb;196(3):417-29. Epub 2007 Oct 17. Pubmed
  4. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. Pubmed
External Links
ATC CodesN05AH05
AHFS Codes
  • 28:16.08.04
PDB EntriesNot Available
FDA labelDownload (448 KB)
MSDSDownload (91.9 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Asenapine can be increased when it is combined with Abiraterone.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Asenapine.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Asenapine.
AmisulprideThe risk or severity of adverse effects can be increased when Asenapine is combined with Amisulpride.
AmphetamineAsenapine may decrease the stimulatory activities of Amphetamine.
AzelastineAsenapine 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 Asenapine.
BortezomibThe metabolism of Asenapine can be decreased when combined with Bortezomib.
BrimonidineBrimonidine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Asenapine.
BuprenorphineAsenapine 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 Asenapine.
CarbamazepineThe metabolism of Asenapine can be increased when combined with Carbamazepine.
CathinoneAsenapine may decrease the stimulatory activities of Cathinone.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Asenapine.
CitalopramCitalopram may increase the QTc-prolonging activities of Asenapine.
Cyproterone acetateThe serum concentration of Asenapine can be decreased when it is combined with Cyproterone acetate.
DeferasiroxThe serum concentration of Asenapine can be increased when it is combined with Deferasirox.
DofetilideDofetilide may increase the QTc-prolonging activities of Asenapine.
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
DronabinolDronabinol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
EthanolAsenapine may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
FluvoxamineThe serum concentration of Asenapine can be increased when it is combined with Fluvoxamine.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Asenapine.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Asenapine.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Asenapine.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Asenapine.
GoserelinGoserelin may increase the QTc-prolonging activities of Asenapine.
HydrocodoneAsenapine may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Asenapine.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Asenapine.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Asenapine.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Asenapine.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Asenapine.
Insulin RegularThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Asenapine.
Insulin, isophaneThe therapeutic efficacy of Insulin, isophane can be decreased when used in combination with Asenapine.
IvabradineIvabradine may increase the QTc-prolonging activities of Asenapine.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Asenapine.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Asenapine.
LorazepamThe risk or severity of adverse effects can be increased when Lorazepam is combined with Asenapine.
Magnesium SulfateMagnesium Sulfate may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Asenapine.
MethotrimeprazineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
MethylphenidateThe risk or severity of adverse effects can be increased when Asenapine is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Asenapine.
MetyrosineAsenapine may increase the sedative activities of Metyrosine.
MexiletineThe metabolism of Asenapine can be decreased when combined with Mexiletine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Asenapine.
MinocyclineMinocycline may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
NabiloneNabilone may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
OctreotideOctreotide may increase the QTc-prolonging activities of Asenapine.
OrphenadrineAsenapine may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
ParaldehydeAsenapine may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
ParoxetineParoxetine may increase the QTc-prolonging activities of Asenapine.
Peginterferon alfa-2bThe serum concentration of Asenapine can be increased when it is combined with Peginterferon alfa-2b.
PerampanelPerampanel may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
PhenelzinePhenelzine may increase the orthostatic hypotensive activities of Asenapine.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Asenapine.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Asenapine.
RufinamideThe risk or severity of adverse effects can be increased when Rufinamide is combined with Asenapine.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Asenapine.
Sodium oxybateSodium oxybate may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
SulpirideThe risk or severity of adverse effects can be increased when Asenapine is combined with Sulpiride.
SuvorexantAsenapine may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
TacrineTacrine may increase the central neurotoxic activities of Asenapine.
TapentadolTapentadol may increase the central nervous system depressant (CNS depressant) activities of Asenapine.
TeriflunomideThe serum concentration of Asenapine can be decreased when it is combined with Teriflunomide.
ThalidomideAsenapine may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Asenapine.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Asenapine.
TranylcypromineTranylcypromine may increase the orthostatic hypotensive activities of Asenapine.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Asenapine.
ZolpidemAsenapine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Food Interactions
  • Avoid water and food for at least 10 minutes post administration of asenapine

Targets

1. D(2) dopamine receptor

Kind: Protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

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

References:

  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Tadori Y, Forbes RA, McQuade RD, Kikuchi T: Functional potencies of dopamine agonists and antagonists at human dopamine D(2) and D(3) receptors. Eur J Pharmacol. 2011 Jun 1. Pubmed
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

2. 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. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

3. 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. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

4. 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. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

5. 5-hydroxytryptamine receptor 2B

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 2B P41595 Details

References:

  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

6. 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. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

7. 5-hydroxytryptamine receptor 5A

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
5-hydroxytryptamine receptor 5A P47898 Details

References:

  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

8. 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. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

9. 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. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

10. 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. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

11. 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. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

12. 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. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

13. 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. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

14. 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. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

15. 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. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Tadori Y, Forbes RA, McQuade RD, Kikuchi T: Functional potencies of dopamine agonists and antagonists at human dopamine D(2) and D(3) receptors. Eur J Pharmacol. 2011 Jun 1. Pubmed
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

16. 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. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. Pubmed
  2. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  3. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

17. Histamine H1 receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Histamine H1 receptor P35367 Details

References:

  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

18. Histamine H2 receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Histamine H2 receptor P25021 Details

References:

  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. Epub 2008 Feb 28. Pubmed

19. Beta-1 adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Beta-1 adrenergic receptor P08588 Details

References:

  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. Pubmed

20. Beta-2 adrenergic receptor

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: antagonist

Components

Name UniProt ID Details
Beta-2 adrenergic receptor P07550 Details

References:

  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. Pubmed
  2. Shahid M, Walker GB, Zorn SH, Wong EH: Asenapine: a novel psychopharmacologic agent with a unique human receptor signature. J Psychopharmacol. 2009 Jan;23(1):65-73. doi: 10.1177/0269881107082944. Epub 2008 Feb 28. Pubmed

Enzymes

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. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed

2. Cytochrome P450 2D6

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. Citrome L: Role of sublingual asenapine in treatment of schizophrenia. Neuropsychiatr Dis Treat. 2011;7:325-39. Epub 2011 May 26. Pubmed

3. UDP-glucuronosyltransferase 1-4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-4 P22310 Details

References:

  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. Pubmed

4. Cytochrome P450 3A4

Kind: Protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Fagiolini A, Forgione RN, Morana B, Maccari M, Goracci A, Bossini L, Pellegrini F, Cuomo A, Casamassima F: Asenapine for the treatment of manic and mixed episodes associated with bipolar I disorder: from clinical research to clinical practice. Expert Opin Pharmacother. 2013 Mar;14(4):489-504. doi: 10.1517/14656566.2013.765859. Epub 2013 Jan 29. Pubmed

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Drug created on March 19, 2008 10:17 / Updated on October 08, 2013 14:22