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QuickView for olanzapine (compound)
PubChem
| Name: | olanzapine |
|---|---|
| PubChem Compound ID: | 4585 |
| Molecular formula: | C17H20N4S |
| Molecular weight: | 312.434 g/mol |
| Synonyms: |
Olanzapine (JAN/USAN); Olanzapine; 10H-thieno[2,3-b][1,5]benzodiazepine, 2-methyl-4-(4-methyl-1-piperazinyl)-; Zyprexa; Zyprexa Zydis; LS-152313; Zyprexa Velotab; LY-170053; D00454; LY 170053.
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Olanzapine (JAN/USAN); Olanzapine; 10H-thieno[2,3-b][1,5]benzodiazepine, 2-methyl-4-(4-methyl-1-piperazinyl)-; Zyprexa; Zyprexa Zydis; LS-152313; Zyprexa Velotab; LY-170053; D00454; LY 170053; 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno(2,3-b)(1,5)benzodiazepine; Olansek; 2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine; Midax; 10H-Thieno(2,3-b)(1,5)benzodiazepine, 2-methyl-4-(4-methyl-1-piperazinyl)-; 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine; Lanzac; Symbyax; 132539-06-1; C07322; Zyprexa (TN); InChI=1/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,7-10H2,1-2H; Olanzapine [USAN:INN]
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DrugBank
Identification
| Name: | olanzapine |
|---|---|
| Name (isomeric): | DB00334 |
| Drug Type: | small molecule |
| Brand: | Zydis, Zyprexa Intramuscular, Symbyax, Olansek, Zyprexa Zydis, Zyprexa |
| Category: | Antiemetics, Antipsychotic Agents, Antipsychotics, Serotonin Uptake Inhibitors |
| CAS number: | 132539-06-1 |
Pharmacology
| Indication: | For 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. |
|---|---|
| Pharmacology: |
Olanzapine, 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 sim...
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Olanzapine, 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.
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| Mechanism of Action: | Olanzapine'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. |
| Absorption: | Well absorbed, with approximately 40% of the dose metabolized before reaching the systemic circulation. |
| Protein binding: | 93% |
| Biotransformation: | Hepatic |
| Route of elimination: | It 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 Life: | 21 to 54 hours |
| Clearance: | 12 to 47 L/h |
| Toxicity: | Symptoms 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 |
Interactions
| Food interaction: |
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| Drug interaction: |
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Targets
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. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. This receptor is involved in tracheal smooth muscle contraction, bronchoconstriction, and control of aldosterone production
| UniProt ID: | P28223 | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Gene: | HTR2A | |||||||||
| Actions: | antagonist | |||||||||
| References: |
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This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
| UniProt ID: | P14416 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| Gene: | DRD2 | ||||||||
| Actions: | antagonist, agonist | ||||||||
| References: |
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This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
| UniProt ID: | P21728 | |||
|---|---|---|---|---|
| Gene: | DRD1 | |||
| Actions: | antagonist | |||
| References: |
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This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase
| UniProt ID: | P21918 | ||
|---|---|---|---|
| Gene: | DRD5 | ||
| Actions: | antagonist | ||
| References: |
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This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
| UniProt ID: | P35462 | ||
|---|---|---|---|
| Gene: | DRD3 | ||
| Actions: | antagonist | ||
| References: |
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This is one of the five types (D1 to D5) of receptors for dopamine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase
| UniProt ID: | P21917 | ||
|---|---|---|---|
| Gene: | DRD4 | ||
| Actions: | antagonist | ||
| References: |
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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 inhibit adenylate cyclase activity
| UniProt ID: | P08908 | |
|---|---|---|
| Gene: | HTR1A | |
| Actions: | antagonist | |
| References: |
|
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 inhibit adenylate cyclase activity
| UniProt ID: | P28222 | |
|---|---|---|
| Gene: | HTR1B | |
| Actions: | antagonist | |
| References: |
|
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 inhibit adenylate cyclase activity
| UniProt ID: | P28221 | |
|---|---|---|
| Gene: | HTR1D | |
| Actions: | antagonist | |
| References: |
|
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 inhibit adenylate cyclase activity
| UniProt ID: | P28566 | |
|---|---|---|
| Gene: | HTR1E | |
| Actions: | antagonist | |
| References: |
|
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. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system
| UniProt ID: | P28335 | |||||||
|---|---|---|---|---|---|---|---|---|
| Gene: | HTR2C | |||||||
| Actions: | antagonist | |||||||
| References: |
|
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. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel
| UniProt ID: | P46098 | |
|---|---|---|
| Gene: | HTR3A | |
| Actions: | antagonist | |
| References: |
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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. It has a high affinity for tricyclic psychotropic drugs
| UniProt ID: | P50406 | |
|---|---|---|
| Gene: | HTR6 | |
| Actions: | antagonist | |
| References: |
|
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
| UniProt ID: | P34969 | |
|---|---|---|
| Gene: | HTR7 | |
| Actions: | antagonist | |
| References: |
|
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system
| UniProt ID: | P35367 | ||||||
|---|---|---|---|---|---|---|---|
| Gene: | HRH1 | ||||||
| Actions: | antagonist | ||||||
| References: |
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This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins
| UniProt ID: | P35348 | ||
|---|---|---|---|
| Gene: | ADRA1A | ||
| Actions: | antagonist | ||
| References: |
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This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system
| UniProt ID: | P35368 | ||||
|---|---|---|---|---|---|
| Gene: | ADRA1B | ||||
| Actions: | antagonist | ||||
| References: |
|
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 = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol
| UniProt ID: | P08913 | |
|---|---|---|
| Gene: | ADRA2A | |
| Actions: | antagonist | |
| References: |
|
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 clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol
| UniProt ID: | P18089 | |
|---|---|---|
| Gene: | ADRA2B | |
| Actions: | antagonist | |
| References: |
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Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins
| UniProt ID: | P18825 | |
|---|---|---|
| Gene: | ADRA2C | |
| Actions: | antagonist | |
| References: |
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The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
| UniProt ID: | P11229 | |||
|---|---|---|---|---|
| Gene: | CHRM1 | |||
| Actions: | antagonist | |||
| References: |
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The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition
| UniProt ID: | P08172 | ||
|---|---|---|---|
| Gene: | CHRM2 | ||
| Actions: | antagonist | ||
| References: |
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The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
| UniProt ID: | P20309 | ||
|---|---|---|---|
| Gene: | CHRM3 | ||
| Actions: | antagonist | ||
| References: |
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The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is inhibition of adenylate cyclase
| UniProt ID: | P08173 | ||
|---|---|---|---|
| Gene: | CHRM4 | ||
| Actions: | antagonist | ||
| References: |
|
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover
| UniProt ID: | P08912 | ||
|---|---|---|---|
| Gene: | CHRM5 | ||
| Actions: | antagonist | ||
| References: |
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Enzymes
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen
| UniProt ID: | P05177 | |||||
|---|---|---|---|---|---|---|
| Gene: | CYP1A2 | |||||
| Actions: | substrate | |||||
| References: |
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Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants
| UniProt ID: | P10635 | ||
|---|---|---|---|
| Gene: | CYP2D6 | ||
| Actions: | substrate, inhibitor | ||
| References: |
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Involved in the oxidative metabolism of a variety of xenobiotics such as drugs and pesticides. It N-oxygenates primary aliphatic alkylamines as well as secondary and tertiary amines. Plays an important role in the metabolism of trimethylamine (TMA), via the production of TMA N-oxide (TMAO). Is also able to perform S-oxidation when acting on sulfide compounds
| UniProt ID: | P31513 | |
|---|---|---|
| Gene: | FMO3 | |
| Actions: | substrate | |
| References: |
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Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine
| UniProt ID: | P33261 | |
|---|---|---|
| Gene: | CYP2C19 | |
| Actions: | inhibitor | |
| References: |
|
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan
| UniProt ID: | P11712 | |
|---|---|---|
| Gene: | CYP2C9 | |
| Actions: | inhibitor | |
| References: |
|
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 xenobiotics. The enzyme also hydroxylates etoposide
| UniProt ID: | P08684 | |
|---|---|---|
| Gene: | CYP3A4 | |
| Actions: | inhibitor | |
| References: |
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Transporters
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells
| UniProt ID: | P08183 | |
|---|---|---|
| Gene: | ABCB1 | |
| Actions: | substrate | |
| References: |
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Carriers
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood
| UniProt ID: | P02768 | |
|---|---|---|
| Gene: | ALB | |
| References: |
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Appears to function in modulating the activity of the immune system during the acute-phase reaction
| UniProt ID: | P02763 | |
|---|---|---|
| Gene: | ORM1 | |
| References: |
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