DGIdb - AMITRIPTYLINE Drug Record

AMITRIPTYLINE chembl:CHEMBL629 Approved

Alternate Names:

AMITRIL
ELAVIL
AMITRIPTYLINE
ENDEP
AMITID
ETRAFON-FORTE
LIMBITROL
ETRAFON-A
10,11-DIHYDRO-N,N-DIMETHYL-5H-DIBENZO(A,D)HEPTALENE-DELTA(5),GAMMA-PROPYLAMINE
AMITRYPTILINE
5-(3-DIMETHYLAMINOPROPYLIDENE)-10,11-DIHYDRO-5H-DIBENZO(A,D)CYCLOHEPTATRIENE
ELAVIL®
10,11-DIHYDRO-5-(GAMMA-DIMETHYLAMINOPROPYLIDENE)-5H-DIBENZO(A,D)CYCLOHEPTENE
5-(3-DIMETHYLAMINOPROPYLIDENE)-10,11-DIHYDRO-5H-DIBENZO(A,D)CYCLOHEPTENE
5-(GAMMA-DIMETHYLAMINOPROPYLIDENE)-5H-DIBENZO[A,D][1,4]CYCLOHEPTADIENE
AMITRIPTILINA
3-(10,11-DIHYDRO-5H-DIBENZO[A,D]CYCLOHEPTEN-5-YLIDENE)-N,N-DIMETHYLPROPAN-1-AMINE
AMITRIPTYLINUM
AMITRIPTYLIN
ENDEP®
3-(10,11-DIHYDRO-5H-DIBENZO(A,D)CYCLOHEPTEN-5-YLIDENE)-N,N-DIMETHYL-1-PROPANAMINE
pubchem.compound:2160
chembl:CHEMBL629
chemidplus:50-48-6
drugbank:00321
rxcui:704

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	analgesic
Drug Categories	dibenzocycloheptenes
Drug Categories	analgesics, non-narcotic
Year of Approval	1961
Drug Class	antidepressive agents, tricyclic
Drug Categories	adrenergic alpha-1 receptor antagonists
Drug Categories	adrenergic alpha-antagonists
Drug Categories	adrenergic antagonists
Drug Categories	agents producing tachycardia
Drug Categories	agents that produce hypertension
Drug Categories	agents that reduce seizure threshold
Drug Categories	anticholinergic agents
Drug Categories	combined inhibitors of serotonin/norepinephrine reuptake
Drug Categories	cytochrome p-450 cyp2c19 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2c8 inhibitors (moderate)
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs that are mainly renally excreted
Drug Categories	histamine antagonists
Drug Categories	histamine h1 antagonists
Drug Categories	moderate risk qtc-prolonging agents
Drug Categories	muscarinic antagonists
Drug Categories	neurotoxic agents
Drug Categories	p-glycoprotein substrates
Drug Categories	qtc prolonging agents
Drug Categories	serotonergic drugs shown to increase risk of serotonin syndrome
Drug Categories	serotonin 5-ht2 receptor antagonists
Drug Categories	serotonin agents
Drug Categories	serotonin receptor antagonists
Drug Categories	tertiary amine tricyclic antidepressants
Drug Categories	tricyclics and other norepinephrine-reuptake inhibitors
Drug Categories	ugt1a1 inhibitors
Drug Categories	ugt1a1 substrates
Drug Categories	ugt1a4 substrates

(6 More Sources)

Publications:

Werling et al., 2007, A comparison of the binding profiles of dextromethorphan, memantine, fluoxetine and amitriptyline: treatment of involuntary emotional expression disorder., Exp. Neurol.
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Sebben et al., 1994, 5-HT6 receptors positively coupled to adenylyl cyclase in striatal neurones in culture., Neuroreport
Kohen et al., 1996, Cloning, characterization, and chromosomal localization of a human 5-HT6 serotonin receptor., J. Neurochem.
Lucchelli et al., 2000, The interaction of antidepressant drugs with enteric 5-HT7 receptors., Naunyn Schmiedebergs Arch. Pharmacol.
Liu J et al., 2013, Spinal serotonin 5-HT7 and adenosine A1 receptors, as well as peripheral adenosine A1 receptors, are involved in antinociception by systemically administered amitriptyline., Eur J Pharmacol
Angus et al., 1980, Pharmacological assay of cardiac H2-receptor blockade by amitriptyline and lysergic acid diethylamide., Circ. Res.
Traiffort E et al., 1992, Pharmacological characterization and autoradiographic localization of histamine H2 receptors in human brain identified with [125I]iodoaminopotentidine., J Neurochem
Ushijima et al., 2005, Chronopharmacological study of antidepressants in forced swimming test of mice., J. Pharmacol. Exp. Ther.
Vaishnavi et al., 2004, Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity., Biol. Psychiatry
Kalia, 2005, Neurobiological basis of depression: an update., Metab. Clin. Exp.
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Troelsen et al., 2005, Chronic treatment with duloxetine is necessary for an anxiolytic-like response in the mouse zero maze: the role of the serotonin transporter., Psychopharmacology (Berl.)
Gould et al., 2006, A comparison of the chronic treatment effects of venlafaxine and other antidepressants on serotonin and norepinephrine transporters., Biol. Psychiatry
Bryson HM et al., 1996, Amitriptyline. A review of its pharmacological properties and therapeutic use in chronic pain states., Drugs Aging
Dilsaver SC et al., 1987, Amitriptyline supersensitizes a central cholinergic mechanism., Biol Psychiatry
Snyder SH et al., 1977, Antidepressants and the muscarinic acetylcholine receptor., Arch Gen Psychiatry
Goldman P et al., 1989, Interaction of amitriptyline with muscarinic receptor subtypes in the rat brain., Neurochem Int
Onali et al., 2010, Direct agonist activity of tricyclic antidepressants at distinct opioid receptor subtypes., J. Pharmacol. Exp. Ther.
Benbouzid M et al., 2008, Delta-opioid receptors are critical for tricyclic antidepressant treatment of neuropathic allodynia., Biol Psychiatry
Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
Nojimoto et al., The tricyclic antidepressants amitriptyline, nortriptyline and imipramine are weak antagonists of human and rat alpha1B-adrenoceptors., Neuropharmacology
Villard et al., 2011, Pharmacological interaction with the sigma1 (σ1)-receptor in the acute behavioral effects of antidepressants., J. Pharmacol. Sci.
Breitenstein B et al., 2016, Association of ABCB1 gene variants, plasma antidepressant concentration, and treatment response: Results from a randomized clinical study., J Psychiatr Res
Huang X et al., 2013, ABCB6, ABCB1 and ABCG1 genetic polymorphisms and antidepressant response of SSRIs in Chinese depressive patients., Pharmacogenomics
de Klerk OL et al., 2013, ABCB1 gene variants influence tolerance to selective serotonin reuptake inhibitors in a large sample of Dutch cases with major depressive disorder., Pharmacogenomics J
Uhr M et al., 2008, Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression., Neuron
Punke et al., 2007, Amitriptyline is a potent blocker of human Kv1.1 and Kv7.2/7.3 channels., Anesth. Analg.
Freysoldt A et al., 2009, Low concentrations of amitriptyline inhibit nicotinic receptors in unmyelinated axons of human peripheral nerve., Br J Pharmacol
Lesch KP et al., 1990, 5-HT1A receptor function in depression: effect of chronic amitriptyline treatment., J Neural Transm Gen Sect
Jenck F et al., 1993, Evidence for a role of 5-HT1C receptors in the antiserotonergic properties of some antidepressant drugs., Eur J Pharmacol
Rossi DV et al., 2006, Chronic administration of venlafaxine fails to attenuate 5-HT1A receptor function at the level of receptor-G protein interaction., Int J Neuropsychopharmacol
Richelson E, 1979, Tricyclic antidepressants and histamine H1 receptors., Mayo Clin Proc
Kachur JF et al., 1988, Antihistaminic and antimuscarinic effects of amitriptyline on guinea pig ileal electrolyte transport and muscle contractility in vitro., J Pharmacol Exp Ther
Carydakis C et al., 1986, [Direct interaction of tricyclic antidepressants with opiate binding sites in the bovine adrenal medulla]., C R Acad Sci III
Hamon et al., 1987, Opioid receptors and neuropeptides in the CNS in rats treated chronically with amoxapine or amitriptyline., Neuropharmacology
Wahlström et al., 1994, Tricyclic antidepressants inhibit opioid receptor binding in human brain and hepatic morphine glucuronidation., Pharmacol. Toxicol.
Jang et al., 2009, Amitriptyline is a TrkA and TrkB receptor agonist that promotes TrkA/TrkB heterodimerization and has potent neurotrophic activity., Chem. Biol.
Zheng X et al., 2016, Amitriptyline Activates TrkA to Aid Neuronal Growth and Attenuate Anesthesia-Induced Neurodegeneration in Rat Dorsal Root Ganglion Neurons., Medicine (Baltimore)
Rantamäki T et al., 2011, Antidepressant drugs transactivate TrkB neurotrophin receptors in the adult rodent brain independently of BDNF and monoamine transporter blockade., PLoS One
Nguyen et al., 2001, Discovery of a novel member of the histamine receptor family., Mol. Pharmacol.
Connelly WM et al., 2009, The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS., Br J Pharmacol
Kucia et al., Effect of antidepressants on the phospholipase A2 activity in plasma membranes of the rat brain cortex., Pol J Pharmacol
Syeda R et al., 2016, The Sensorless Pore Module of Voltage-gated K+ Channel Family 7 Embodies the Target Site for the Anticonvulsant Retigabine., J Biol Chem
Di Matteo et al., 2001, Role of 5-HT(2C) receptors in the control of central dopamine function., Trends Pharmacol. Sci.
Pälvimäki et al., 1996, Interactions of selective serotonin reuptake inhibitors with the serotonin 5-HT2c receptor., Psychopharmacology (Berl.)
Kubera et al., 2000, The effect of repeated amitriptyline and desipramine administration on cytokine release in C57BL/6 mice., Psychoneuroendocrinology
Pandey DK et al., 2010, A novel 5-HT(2A) receptor antagonist exhibits antidepressant-like effects in a battery of rodent behavioural assays: approaching early-onset antidepressants., Pharmacol Biochem Behav
Schlienger et al., [Different effects of tricyclic (clomipramine and amitriptyline) and tetracyclic (maprotiline) antidepressors on the release of thyroid stimulating hormone, prolactin and growth hormone to thyrostimulating releasing hormone in patients with psychoaffective disorders (author's transl)]., Acta Psychiatr Belg
Linkowski et al., 1983, Prolactin and growth hormone response to levodopa in affective illness., Neuropsychobiology
Ozdoğan et al., 2004, Loss of amitriptyline analgesia in alpha 2A-adrenoceptor deficient mice., Eur. J. Pharmacol.
Cottingham C et al., 2014, Tricyclic antidepressants exhibit variable pharmacological profiles at the α(2A) adrenergic receptor., Biochem Biophys Res Commun
Charney DS et al., 1983, Alpha-2 adrenergic receptor sensitivity and the mechanism of action of antidepressant therapy. The effect of long-term amitriptyline treatment., Br J Psychiatry
Gray AM et al., 1999, Do alpha2-adrenoceptors play an integral role in the antinociceptive mechanism of action of antidepressant compounds?, Eur J Pharmacol
Ozgocmen et al., 2006, Antioxidant status, lipid peroxidation and nitric oxide in fibromyalgia: etiologic and therapeutic concerns., Rheumatol. Int.
Cai J et al., 2014, Potential therapeutic effects of neurotrophins for acute and chronic neurological diseases., Biomed Res Int
O'Neill E et al., 2016, Amitriptyline protects against TNF-α-induced atrophy and reduction in synaptic markers via a Trk-dependent mechanism., Pharmacol Res Perspect
Jo SH et al., 2000, Blockade of the HERG human cardiac K(+) channel by the antidepressant drug amitriptyline., Br J Pharmacol
Teschemacher et al., 1999, Inhibition of the current of heterologously expressed HERG potassium channels by imipramine and amitriptyline., Br. J. Pharmacol.

AMITRIPTYLINE KCNQ3

Interaction Score: 0.38

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17456683 26627826

Sources:
DrugBank
AMITRIPTYLINE KCNA1

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17456683 19694730

Sources:
DrugBank
AMITRIPTYLINE KCNQ2

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17456683

Sources:
DrugBank
AMITRIPTYLINE SIGMAR1

Interaction Score: 0.19

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
17689532 21427517

Sources:
DrugBank
AMITRIPTYLINE SLC6A4

Interaction Score: 0.19

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16079297 17689532 14744476 15877309 9537821 16032412 16140280 8736630

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology
AMITRIPTYLINE IFNG

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
10996474

Sources:
NCI
AMITRIPTYLINE PRL

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
6786002 6621850

Sources:
NCI
AMITRIPTYLINE ADA

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16283318

Sources:
NCI
AMITRIPTYLINE SLC6A2

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
14744476 9537821 8736630

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology
AMITRIPTYLINE HRH4

Interaction Score: 0.12

Interaction Types & Directionality:

binder

Interaction Info:

PMIDs:
11179435 19413571

Sources:
DrugBank
AMITRIPTYLINE HRH2

Interaction Score: 0.12

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

PMIDs:
6103762 1351926

Sources:
DrugBank
AMITRIPTYLINE NTRK2

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
19549602 24818146 27069625

Sources:
DrugBank
AMITRIPTYLINE HTR6

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
7696602 8522988

Sources:
DrugBank GuideToPharmacology
AMITRIPTYLINE NTRK1

Interaction Score: 0.09

Interaction Types & Directionality:

agonist (activating)

activator (activating)

Interaction Info:

PMIDs:
19549602 27149473 21666748

Sources:
DrugBank
AMITRIPTYLINE PLA2G1B

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12856820

Sources:
NCI
AMITRIPTYLINE HTR7

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
10997731 23142373

Sources:
DrugBank
AMITRIPTYLINE ADRA2A

Interaction Score: 0.06

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

Interaction Info:

PMIDs:
7855217 14757140 25128275 6305451 10478628

Sources:
DrugBank
AMITRIPTYLINE CHRM1

Interaction Score: 0.05

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
7855217 3567263 14603 20504448

Sources:
DrugBank GuideToPharmacology
AMITRIPTYLINE OPRD1

Interaction Score: 0.05

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
19828880 17693391

Sources:
DrugBank
AMITRIPTYLINE HTR1A

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

inducer (activating)

Interaction Info:

PMIDs:
7855217 2317317 8453978 16035959

Sources:
DrugBank
AMITRIPTYLINE HTR1D

Interaction Score: 0.04

Interaction Types & Directionality:

binder

Interaction Info:

PMIDs:
17689532

Sources:
DrugBank
AMITRIPTYLINE ADRA1D

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
20363235

Sources:
DrugBank
AMITRIPTYLINE HRH1

Interaction Score: 0.04

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Antagonism of [<sup>3</sup>H]mepyramine binding

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
7855217 39202 2896792

Sources:
DrugBank GuideToPharmacology
AMITRIPTYLINE OPRK1

Interaction Score: 0.04

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
19828880 3013380

Sources:
DrugBank
AMITRIPTYLINE HTR1B

Interaction Score: 0.04

Interaction Types & Directionality:

binder

Interaction Info:

PMIDs:
17689532

Sources:
DrugBank
AMITRIPTYLINE CHRM4

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
7855217

Sources:
GuideToPharmacology
AMITRIPTYLINE CHRM5

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
7855217

Sources:
GuideToPharmacology
AMITRIPTYLINE HTR2C

Interaction Score: 0.03

Interaction Types & Directionality:

binder

antagonist (inhibitory)

Interaction Info:

PMIDs:
11339973 8876023

Sources:
DrugBank
AMITRIPTYLINE HTR2A

Interaction Score: 0.03

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name OMS-103HP

Novel drug target Established target

PMIDs:
7855217 19800913

Sources:
DrugBank TdgClinicalTrial
AMITRIPTYLINE OPRM1

Interaction Score: 0.03

Interaction Types & Directionality:

binder

Interaction Info:

PMIDs:
3037421 7971731

Sources:
DrugBank
AMITRIPTYLINE ABCB1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
26704739 24192121 22641028 18215618

Sources:
PharmGKB
AMITRIPTYLINE ADRA1B

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
20363235

Sources:
DrugBank
AMITRIPTYLINE ADRA1A

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

PMIDs:
7855217 20363235

Sources:
DrugBank
AMITRIPTYLINE CHRM2

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
7855217

Sources:
GuideToPharmacology
AMITRIPTYLINE CHRM3

Interaction Score: 0.02

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
7855217

Sources:
GuideToPharmacology
AMITRIPTYLINE KCNH2

Interaction Score: 0.01

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

PMIDs:
10742304 10510461

Sources:
DrugBank
AMITRIPTYLINE DRD1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
AMITRIPTYLINE CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC FDA
AMITRIPTYLINE CYP2C9

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC
AMITRIPTYLINE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300 9187528

Sources:
DTC PharmGKB
AMITRIPTYLINE CYP1A2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22931300

Sources:
DTC

DrugBank: DB00321

Version: 5.1.7

Alternate Names:

AMITRIPTYLINE DrugBank Drug Name

50-48-6 CAS Number

Adepril Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Categories adrenergic alpha-1 receptor antagonists

Publications:

Vaishnavi et al., 2004, Milnacipran: a comparative analysis of human monoamine uptake and transporter binding affinity., Biol. Psychiatry

Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.

Bryson HM et al., 1996, Amitriptyline. A review of its pharmacological properties and therapeutic use in chronic pain states., Drugs Aging

TEND: AMITRIPTYLINE
- Version: 01-August-2011
Alternate Names:

AMITRIPTYLINE Primary Drug Name

Drug Info:

Drug Class antidepressive agents, tricyclic

Year of Approval 1961

Publications:
TdgClinicalTrial: AMITRIPTYLINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications analgesic

Drug Class Small Molecule

FDA Approval approved

Publications:

NCI: AMITRIPTYLINE

Version: 14-September-2017

Alternate Names:

C28819 NCI drug code

Drug Info:

Publications:

Rajtar et al., 2007, Amitriptyline affects histamine-N-methyltransferase and diamine oxidase activity in rats and guinea pigs., Eur. J. Pharmacol.

Ozgocmen et al., 2006, Antioxidant status, lipid peroxidation and nitric oxide in fibromyalgia: etiologic and therapeutic concerns., Rheumatol. Int.

Kubera et al., 2000, The effect of repeated amitriptyline and desipramine administration on cytokine release in C57BL/6 mice., Psychoneuroendocrinology

DTC: AMITRIPTYLINE
- Version: 02-September-2020
Alternate Names:

CHEMBL629 ChEMBL Drug ID

Drug Info:

Publications:

Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol

PharmGKB: amitriptyline

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Uhr M et al., 2008, Polymorphisms in the drug transporter gene ABCB1 predict antidepressant treatment response in depression., Neuron

de Klerk OL et al., 2013, ABCB1 gene variants influence tolerance to selective serotonin reuptake inhibitors in a large sample of Dutch cases with major depressive disorder., Pharmacogenomics J

Huang X et al., 2013, ABCB6, ABCB1 and ABCG1 genetic polymorphisms and antidepressant response of SSRIs in Chinese depressive patients., Pharmacogenomics

GuideToPharmacology: 135649939
- Version: 29-September-2020
Alternate Names:

AMITRIPTYLINE GuideToPharmacology Ligand Name

Drug Info:

Publications:
TTD: Amitriptyline
- Version: 2020.06.01
Alternate Names:

D0Y5UG TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL629
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Amitriptyline
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Specific Action of the Ligand	Inhibition
Endogenous Drug?	False
Direct Interaction?	True

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False
Direct Interaction?	True

Details of the Assay for Interaction	Antagonism of [<sup>3</sup>H]mepyramine binding
Specific Action of the Ligand	Antagonist
Endogenous Drug?	False

AMITRIPTYLINE	DrugBank Drug Name
50-48-6	CAS Number
Adepril	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Categories	adrenergic alpha-1 receptor antagonists

agonist (activating)
activator (activating)

antagonist (inhibitory)
agonist (activating)

antagonist (inhibitory)
ligand

AMITRIPTYLINE Drug Record

AMITRIPTYLINE chembl:CHEMBL629 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 17456683 26627826

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 17456683 19694730

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 17456683

Sources: DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 17689532 21427517

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Specific Action of the Ligand Inhibition Endogenous Drug? False Direct Interaction? True

PMIDs: 16079297 17689532 14744476 15877309 9537821 16032412 16140280 8736630

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 10996474

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 6786002 6621850

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16283318

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Direct Interaction? True Endogenous Drug? False Specific Action of the Ligand Inhibition

PMIDs: 14744476 9537821 8736630

Sources: DrugBank TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality: binder

Interaction Info:

PMIDs: 11179435 19413571

Sources: DrugBank

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info:

PMIDs: 6103762 1351926

Sources: DrugBank

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 19549602 24818146 27069625

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Endogenous Drug? False Specific Action of the Ligand Antagonist

PMIDs: 7696602 8522988

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating) activator (activating)

Interaction Info:

PMIDs: 19549602 27149473 21666748

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12856820

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 10997731 23142373

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory) agonist (activating)

Interaction Info:

PMIDs: 7855217 14757140 25128275 6305451 10478628

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory) ligand

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 7855217 3567263 14603 20504448

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: agonist (activating)

Interaction Info:

PMIDs: 19828880 17693391

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
17456683 26627826

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
17456683 19694730

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
17456683

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

PMIDs:
17689532 21427517

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? True

PMIDs:
16079297 17689532 14744476 15877309 9537821 16032412 16140280 8736630

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
10996474

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
6786002 6621850

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
16283318

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? True

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
14744476 9537821 8736630

Sources:
DrugBank TdgClinicalTrial TEND GuideToPharmacology

Interaction Types & Directionality:

binder

PMIDs:
11179435 19413571

Sources:
DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

PMIDs:
6103762 1351926

Sources:
DrugBank

Interaction Types & Directionality:

agonist (activating)

PMIDs:
19549602 24818146 27069625

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
7696602 8522988

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

activator (activating)

PMIDs:
19549602 27149473 21666748

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
12856820

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
10997731 23142373

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

agonist (activating)

PMIDs:
7855217 14757140 25128275 6305451 10478628

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

ligand

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
7855217 3567263 14603 20504448

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

PMIDs:
19828880 17693391

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

inducer (activating)

PMIDs:
7855217 2317317 8453978 16035959

Sources:
DrugBank

Interaction Types & Directionality:

binder

PMIDs:
17689532

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
20363235

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Details of the Assay for Interaction Antagonism of [<sup>3</sup>H]mepyramine binding

Specific Action of the Ligand Antagonist

Endogenous Drug? False

PMIDs:
7855217 39202 2896792

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

agonist (activating)

PMIDs:
19828880 3013380

Sources:
DrugBank

Interaction Types & Directionality:

binder

PMIDs:
17689532

Sources:
DrugBank