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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyProtriptyline
Identification
- Name
- Protriptyline
- Accession Number
- DB00344 (APRD00441)
- Type
- Small Molecule
- Groups
- Approved
- Description
Protriptyline hydrochloride is a dibenzocycloheptene-derivative tricyclic antidepressant (TCA). TCAs are structurally similar to phenothiazines. They contain a tricyclic ring system with an alkyl amine substituent on the central ring. In non-depressed individuals, protriptyline does not affect mood or arousal, but may cause sedation. In depressed individuals, protriptyline exerts a positive effect on mood. TCAs are potent inhibitors of serotonin and norepinephrine reuptake. In addition, TCAs down-regulate cerebral cortical β-adrenergic receptors and sensitize post-synaptic serotonergic receptors with chronic use. The antidepressant effects of TCAs are thought to be due to an overall increase in serotonergic neurotransmission. TCAs also block histamine H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e.g. blurred vision, dry mouth, constipation, urinary retention), respectively. See toxicity section below for a complete listing of side effects. Protriptyline may be used for the treatment of depression.
- Structure
Structure for Protriptyline (DB00344)
- Synonyms
- 3-(5H-dibenzo[a,d][7]annulen-5-yl)-N-methylpropan-1-amine
- 3-(5H-dibenzo[a,d]cyclohepten-5-yl)-N-methyl-1-propanamine
- 5-(3-methylaminopropyl)-5H-dibenzo[a,d]cycloheptene
- 7-(3-methylaminopropyl)-1,2:5,6-dibenzocycloheptatriene
- Amimetilina
- N-methyl-5H-dibenzo[a,d]cycloheptene-5-propanamine
- N-methyl-5H-dibenzo[a,d]cycloheptene-5-propylamine
- Protriptilina
- Protriptylin
- Protriptyline
- Protriptylinum
- External IDs
- MK 240 / MK-240
- Product Ingredients
Ingredient UNII CAS InChI Key Protriptyline hydrochloride 44665V00O8 1225-55-4 OGQDIIKRQRZXJH-UHFFFAOYSA-N - Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Unlock Additional DataTriptil Tab 10mg Tablet Oral Merck Frosst Canada & Cie, Merck Frosst Canada & Co. 1966-12-31 2001-01-25 Canada 
Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Unlock Additional DataProtriptyline Hydrochloride Tablet, film coated 10 mg/1 Oral Barr Laboratories 2008-12-23 2013-06-30 US 
Protriptyline Hydrochloride Tablet, film coated 5 mg/1 Oral Rising Pharmaceuticals 2010-06-11 Not applicable US Protriptyline Hydrochloride Tablet, film coated 10 mg/1 Oral Epic Pharma, LLC 2013-01-09 Not applicable US Protriptyline Hydrochloride Tablet, film coated 5 mg/1 Oral Barr Laboratories 2008-12-23 2013-06-30 US Protriptyline Hydrochloride Tablet, film coated 5 mg/1 Oral Epic Pharma, LLC 2013-01-09 Not applicable US Protriptyline Hydrochloride Tablet 10 mg/1 Oral West-Ward Pharmaceuticals Corp. 2008-09-16 Not applicable US Protriptyline hydrochloride Tablet, film coated 10 mg/1 Oral Hi-Tech Pharmacal Co., Inc. 2013-10-28 Not applicable US Protriptyline Hydrochloride Tablet 5 mg/1 Oral West-Ward Pharmaceuticals Corp. 2008-09-16 Not applicable US Protriptyline Hydrochloride Tablet, film coated 10 mg/1 Oral Rising Pharmaceuticals 2010-06-11 Not applicable US Protriptyline hydrochloride Tablet, film coated 5 mg/1 Oral Hi-Tech Pharmacal Co., Inc. 2013-10-28 Not applicable US Additional Data Available- Application NumberApplication Number
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct Code
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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- International/Other Brands
- Triptil
- Categories
- Adrenergic Agents
- Adrenergic Uptake Inhibitors
- Agents that produce hypertension
- Agents that reduce seizure threshold
- Antidepressive Agents
- Antidepressive Agents, Tricyclic
- Benzocycloheptenes
- Central Nervous System Agents
- Central Nervous System Depressants
- Combined Inhibitors of Serotonin/Norepinephrine Reuptake
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 CYP2D6 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Substrates
- Dibenzocycloheptenes
- Membrane Transport Modulators
- Narrow Therapeutic Index Drugs
- Nervous System
- Neurotoxic agents
- Neurotransmitter Agents
- Neurotransmitter Uptake Inhibitors
- Non-Selective Monoamine Reuptake Inhibitors
- P-glycoprotein inhibitors
- Potential QTc-Prolonging Agents
- Psychoanaleptics
- Psychotropic Drugs
- QTc Prolonging Agents
- Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
- Serotonin Agents
- Serotonin Modulators
- UNII
- 4NDU154T12
- CAS number
- 438-60-8
- Weight
- Average: 263.3767
Monoisotopic: 263.167399677 - Chemical Formula
- C19H21N
- InChI Key
- BWPIARFWQZKAIA-UHFFFAOYSA-N
- InChI
- InChI=1S/C19H21N/c1-20-14-6-11-19-17-9-4-2-7-15(17)12-13-16-8-3-5-10-18(16)19/h2-5,7-10,12-13,19-20H,6,11,14H2,1H3
- IUPAC Name
- methyl(3-{tricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,9,11,13-heptaen-2-yl}propyl)amine
- SMILES
- CNCCCC1C2=CC=CC=C2C=CC2=CC=CC=C12
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Pharmacology
- Indication
For the treatment of depression.
- Associated Conditions
- Pharmacodynamics
Protriptyline is a tricyclic antidepressant. It was thought that tricyclic antidepressants work by inhibiting the reuptake of the neurotransmitters norepinephrine and serotonin by nerve cells. The effectiveness of antidepressants appear after approximately two weeks following recommended adminsitration schedule. Gradual changes are thought to occur in the cerebral cortex and hippocampus, involved in emotion regulation as part of the limbic system, as receptor sensitivity is enhanced. While α1 and β1 receptors are sensitized, α2 receptors are desensitized (leading to increased noradrenaline production). Tricyclics are also reported to alter the perceptions of pain, including neuropathic or neuralgic pain, so they may exhibit analgesic properties. The mechanism of action behind this analgesic property is not fully understood; however, it is thought to involve modulation of endogenous opioid systems in the CNS via an indirect serotonergic route. Tricyclic antidepressants are also effective in relieving migraine prophylaxis, but not in abortion of acute migraine attack, potentially via their serotonergic effects.
- Mechanism of action
Protriptyline acts by decreasing the reuptake of norepinephrine and serotonin (5-HT).
Target Actions Organism ASodium-dependent noradrenaline transporter inhibitorHumans ASodium-dependent serotonin transporter inhibitorHumans - Absorption
- Not Available
- Volume of distribution
- Not Available
- Protein binding
- Not Available
- Metabolism
- Not Available
- Route of elimination
Protriptyline is reported to undergo cumulative urinary excretion during 16 days, which accounts for approximately 50% of the total drug administered. The fecal excretion pathway seems to play a minimal role in drug elimination.
- Half life
- Not Available
- Clearance
- Not Available
- Toxicity
Side effects include anxiety, blood disorders, confusion, decreased libido, dizziness, flushing, headache, impotence, insomnia, low blood pressure, nightmares, rapid or irregular heartbeat, rash, seizures, sensitivity to sunlight, stomach and intestinal discomfort, sedation, hypotension, blurred vision, dry mouth, constipation, urinary retention, postural hypotension, tachycardia, hypertension, ECG changes, heart failure, impaired memory and delirium, and precipitation of hypomanic or manic episodes in bipolar depression. Withdrawal symptoms include gastrointestinal disturbances, anxiety, and insomnia.
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details Cytochrome P450 2D6 CYP2D6*3 Not Available C allele Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*4 Not Available C allele Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*5 Not Available Whole-gene deletion Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*6 Not Available 1707delT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*7 Not Available 2935A>C Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*8 Not Available 1758G>T Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*11 Not Available 883G>C Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*12 Not Available 124G>A Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*13 Not Available CYP2D7/2D6 hybrid gene structure Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*14A Not Available 1758G>A Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*15 Not Available 137insT, 137_138insT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*19 Not Available 2539_2542delAACT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*20 Not Available 1973_1974insG Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*21 Not Available 2573insC Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*31 Not Available -1770G>A / -1584C>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*36 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*38 Not Available 2587_2590delGACT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*40 Not Available 1863_1864ins(TTT CGC CCC)2 Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*42 Not Available 3259_3260insGT Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*44 Not Available 2950G>C Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*47 Not Available 100C>T / -1426C>T … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*51 Not Available -1584C>G / -1235A>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*56 Not Available 3201C>T Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*57 Not Available 100C>T / 310G>T … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*62 Not Available 4044C>T Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*68A Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*68B Not Available Similar but not identical switch region compared to CYP2D6*68A. Found in tandem arrangement with CYP2D6*4. Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*69 Not Available 2988G>A / -1426C>T … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*92 Not Available 1995delC Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*100 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer. Details Cytochrome P450 2D6 CYP2D6*101 Not Available -1426C>T / -1235A>G … show all Effect Inferred Poor drug metabolizer. Details
Unlock Additional Data
Additional Data Available
Adverse Effects
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Learn more Additional Data Available
Contraindications
Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Learn more Additional Data Available
Blackbox Warnings
Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
Learn moreInteractions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Unlock Additional Data(R)-warfarin The risk or severity of adverse effects can be increased when Protriptyline is combined with (R)-warfarin. (S)-Warfarin The risk or severity of adverse effects can be increased when Protriptyline is combined with (S)-Warfarin. 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine The metabolism of Protriptyline can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine. 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid The risk or severity of hypertension can be increased when Protriptyline is combined with 1-(3-Mercapto-2-Methyl-Propionyl)-Pyrrolidine-2-Carboxylic Acid. 1-benzylimidazole The risk or severity of hypertension can be increased when Protriptyline is combined with 1-benzylimidazole. 2,4-thiazolidinedione Protriptyline may decrease the hypoglycemic activities of 2,4-thiazolidinedione. 2,5-Dimethoxy-4-ethylamphetamine The therapeutic efficacy of Protriptyline can be increased when used in combination with 2,5-Dimethoxy-4-ethylamphetamine. 2,5-Dimethoxy-4-ethylthioamphetamine The therapeutic efficacy of Protriptyline can be increased when used in combination with 2,5-Dimethoxy-4-ethylthioamphetamine. 4-Bromo-2,5-dimethoxyamphetamine The therapeutic efficacy of Protriptyline can be increased when used in combination with 4-Bromo-2,5-dimethoxyamphetamine. 4-Bromo-2,5-dimethoxyphenethylamine The risk or severity of hypertension can be increased when Protriptyline is combined with 4-Bromo-2,5-dimethoxyphenethylamine. Additional Data Available- Extended DescriptionExtended Description
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - Severity
- Evidence Level
- ActionAction
An effect category for each drug interaction. Know how this interaction affects the subject drug.
Learn more
- Food Interactions
- Not Available
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0014488
- KEGG Drug
- D08447
- KEGG Compound
- C07408
- PubChem Compound
- 4976
- PubChem Substance
- 46505128
- ChemSpider
- 4805
- BindingDB
- 50176062
- ChEBI
- 8597
- ChEMBL
- CHEMBL668
- Therapeutic Targets Database
- DAP000863
- PharmGKB
- PA451168
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Protriptyline
- ATC Codes
- N06AA11 — Protriptyline
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count Not Available Completed Treatment Depression 1
Pharmacoeconomics
- Manufacturers
- Sanofi aventis us llc
- Pfizer laboratories div pfizer inc
- Roxane laboratories inc
- Sigmapharm laboratories llc
- Odyssey pharmaceuticals inc
- Packagers
- Barr Pharmaceuticals
- Duramed
- Mallinckrodt Inc.
- Pliva Inc.
- Qualitest
- Rising Pharmaceuticals
- Roxane Labs
- Sanofi-Aventis Inc.
- Dosage forms
Form Route Strength Tablet Oral 10 mg/1 Tablet Oral 5 mg/1 Tablet, film coated Oral 10 mg/1 Tablet, film coated Oral 5 mg/1 Tablet Oral - Prices
Unit description Cost Unit Tofranil-PM 30 125 mg capsule Bottle 588.33USD bottle Tofranil-PM 30 150 mg capsule Bottle 588.33USD bottle Tofranil-PM 30 75 mg capsule Bottle 588.33USD bottle Tofranil 30 50 mg tablet Bottle 185.09USD bottle Tofranil-pm 100 mg capsule 19.23USD capsule Tofranil-pm 150 mg capsule 18.86USD capsule Tofranil-pm 75 mg capsule 18.86USD capsule Tofranil-pm 125 mg capsule 18.68USD capsule Anafranil 25 mg capsule 13.51USD capsule Anafranil 50 mg capsule 13.51USD capsule Anafranil 75 mg capsule 13.24USD capsule Tofranil 50 mg tablet 6.64USD tablet Norpramin 150 mg tablet 6.23USD tablet Surmontil 100 mg capsule 5.92USD capsule Tofranil 25 mg tablet 4.97USD tablet Tofranil 10 mg tablet 4.73USD tablet Norpramin 100 mg tablet 4.27USD tablet Surmontil 50 mg capsule 4.15USD capsule Vivactil 10 mg tablet 4.05USD tablet Norpramin 75 mg tablet 3.27USD tablet Protriptyline hcl 10 mg tablet 3.07USD tablet Vivactil 5 mg tablet 2.86USD tablet Norpramin 50 mg tablet 2.59USD tablet Surmontil 25 mg capsule 2.49USD capsule Protriptyline hcl 5 mg tablet 2.12USD tablet Norpramin 25 mg tablet 1.4USD tablet Norpramin 10 mg tablet 1.16USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 169-171 °C (Protriptyline HCl) Not Available water solubility 1.04 mg/L Not Available logP 4.7 Not Available - Predicted Properties
Property Value Source Water Solubility 0.000231 mg/mL ALOGPS logP 4.65 ALOGPS logP 4.5 ChemAxon logS -6.1 ALOGPS pKa (Strongest Basic) 10.54 ChemAxon Physiological Charge 1 ChemAxon Hydrogen Acceptor Count 1 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 12.03 Å2 ChemAxon Rotatable Bond Count 4 ChemAxon Refractivity 87.3 m3·mol-1 ChemAxon Polarizability 31.6 Å3 ChemAxon Number of Rings 3 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule Yes ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9862 Caco-2 permeable + 0.7821 P-glycoprotein substrate Substrate 0.7406 P-glycoprotein inhibitor I Inhibitor 0.8563 P-glycoprotein inhibitor II Inhibitor 0.5597 Renal organic cation transporter Inhibitor 0.6622 CYP450 2C9 substrate Non-substrate 0.7206 CYP450 2D6 substrate Substrate 0.9034 CYP450 3A4 substrate Substrate 0.5285 CYP450 1A2 substrate Non-inhibitor 0.7595 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Inhibitor 0.8933 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Inhibitor 0.641 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7512 Ames test Non AMES toxic 0.6 Carcinogenicity Non-carcinogens 0.9322 Biodegradation Not ready biodegradable 0.7732 Rat acute toxicity 3.0087 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.736 hERG inhibition (predictor II) Inhibitor 0.8132
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Mass Spectrum (Electron Ionization) MS splash10-006x-8910000000-ec599ee02d998905757e Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as dibenzocycloheptenes. These are compounds containing a dibenzocycloheptene moiety, which consists of two benzene rings connected by a cycloheptene ring.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Dibenzocycloheptenes
- Sub Class
- Not Available
- Direct Parent
- Dibenzocycloheptenes
- Alternative Parents
- Aralkylamines / Dialkylamines / Organopnictogen compounds / Hydrocarbon derivatives
- Substituents
- Dibenzocycloheptene / Aralkylamine / Secondary amine / Secondary aliphatic amine / Organic nitrogen compound / Organopnictogen compound / Hydrocarbon derivative / Organonitrogen compound / Amine / Aromatic homopolycyclic compound
- Molecular Framework
- Aromatic homopolycyclic compounds
- External Descriptors
- organic tricyclic compound (CHEBI:8597)
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Norepinephrine:sodium symporter activity
- Specific Function
- Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
- Gene Name
- SLC6A2
- Uniprot ID
- P23975
- Uniprot Name
- Sodium-dependent noradrenaline transporter
- Molecular Weight
- 69331.42 Da
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
- Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
- Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
- Cheetham SC, Viggers JA, Butler SA, Prow MR, Heal DJ: [3H]nisoxetine--a radioligand for noradrenaline reuptake sites: correlation with inhibition of [3H]noradrenaline uptake and effect of DSP-4 lesioning and antidepressant treatments. Neuropharmacology. 1996 Jan;35(1):63-70. [PubMed:8684598]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Serotonin:sodium symporter activity
- Specific Function
- Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
- Gene Name
- SLC6A4
- Uniprot ID
- P31645
- Uniprot Name
- Sodium-dependent serotonin transporter
- Molecular Weight
- 70324.165 Da
References
- McDougle CJ, Epperson CN, Price LH, Gelernter J: Evidence for linkage disequilibrium between serotonin transporter protein gene (SLC6A4) and obsessive compulsive disorder. Mol Psychiatry. 1998 May;3(3):270-3. [PubMed:9672904]
- Rouillon F, Blachier C, Dreyfus JP, Bouhassira M, Allicar MP: [Pharmaco-epidemiologic study of the use of antidepressant drugs in the general population]. Encephale. 1996 May;22 Spec No 1:39-48. [PubMed:8767026]
- Frazer A, Daws LC: Serotonin transporter function in vivo: assessment by chronoamperometry. Ann N Y Acad Sci. 1998 Dec 15;861:217-29. [PubMed:9928259]
- Daws LC, Toney GM, Gerhardt GA, Frazer A: In vivo chronoamperometric measures of extracellular serotonin clearance in rat dorsal hippocampus: contribution of serotonin and norepinephrine transporters. J Pharmacol Exp Ther. 1998 Aug;286(2):967-76. [PubMed:9694957]
- Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
- Kovachich GB, Aronson CE, Brunswick DJ: Effect of repeated administration of antidepressants on serotonin uptake sites in limbic and neocortical structures of rat brain determined by quantitative autoradiography. Neuropsychopharmacology. 1992 Dec;7(4):317-24. [PubMed:1476595]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Ibrahim S, Peggins J, Knapton A, Licht T, Aszalos A: Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation. J Pharmacol Exp Ther. 2000 Dec;295(3):1276-83. [PubMed:11082465]
Drug created on June 13, 2005 07:24 / Updated on November 02, 2019 04:23