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doxepin

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Description

Doxepin is a tricyclic antidepressant (TCA) medication that is used to treat depression, anxiety, and insomnia. It is also used off-label to treat certain types of chronic pain, such as neuropathic pain. Doxepin works by increasing the levels of serotonin and norepinephrine in the brain. It was first synthesized in 1960 and approved by the FDA in 1968. Doxepin has a wide range of therapeutic effects, including antidepressant, anxiolytic, antihistamine, and sedative effects. It is also effective in treating a variety of conditions, including depression, anxiety, insomnia, chronic pain, and allergic reactions. Doxepin is studied for its potential to treat a variety of conditions, including chronic pain, anxiety, depression, and insomnia. Research is ongoing to understand the mechanisms of action of doxepin and to develop new and improved treatments for these conditions.'

Doxepin: A dibenzoxepin tricyclic compound. It displays a range of pharmacological actions including maintaining adrenergic innervation. Its mechanism of action is not fully understood, but it appears to block reuptake of monoaminergic neurotransmitters into presynaptic terminals. It also possesses anticholinergic activity and modulates antagonism of histamine H(1)- and H(2)-receptors. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

doxepin : A dibenzooxepine that is 6,11-dihydrodibenzo[b,e]oxepine substituted by a 3-(dimethylamino)propylidene group at position 11. It is used as an antidepressant drug. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID3158
CHEMBL ID1628227
CHEBI ID4710
SCHEMBL ID28054
MeSH IDM0006782

Synonyms (43)

Synonym
sinequan
OPREA1_473232
DIVK1C_000431
KBIO1_000431
CHEBI:4710 ,
1-propanamine, 3-dibenz(b,e)oxepin-11(6h)-ylidene-n,n-dimethyl-
zonalon
SPECTRUM_000805
1-propanamine, 3-dibenz[b,e]oxepin-11(6h)-ylidene-n,n-dimethyl-
doxepin
1668-19-5
KBIO2_001285
KBIO2_006421
KBIOGR_001131
KBIO3_001154
KBIOSS_001285
KBIO2_003853
SPBIO_000206
SPECTRUM3_000407
SPBIO_002325
PRESTWICK0_000263
SPECTRUM2_000133
SPECTRUM4_000526
PRESTWICK1_000263
NINDS_000431
(3e)-3-(6h-benzo[c][1]benzoxepin-11-ylidene)-n,n-dimethylpropan-1-amine
3-(6h-benzo[c][1]benzoxepin-11-ylidene)-n,n-dimethylpropan-1-amine
CHEMBL1628227
FT-0601521
NCGC00015344-05
SCHEMBL28054
11-(3-dimethylamino-propylidene)-6,11-dihydrodibenzo-[b,e]-oxepine
ODQWQRRAPPTVAG-UHFFFAOYSA-N
11-(3-dimethylamino-propylidene)- 6,11-dihydrodibenzo- [b,e]-oxepine
nsc 108160
3-(6,11-dihydrodibenz[b,e]oxepin-11-yliden)-n,n-dimethylpropylamin
3-(dibenzo[b,e]oxepin-11(6h)-ylidene)-n,n-dimethylpropan-1-amine
DTXSID7022966 ,
AKOS028110197
(e)-3-(dibenzo[b,e]oxepin-11(6h)-ylidene)-n,n-dimethylpropan-1-amine
(z)-3-(dibenzo[b,e]oxepin-11(6h)-ylidene)-n,n-dimethylpropan-1-amine
bdbm50225488
sinepin

Research Excerpts

Overview

Doxepin is a traditional tricyclic antidepressant with analgesic and anesthetic properties when applied topically to the mucosa. It has been used extensively for the treatment of depressive and anxiety disorders for approximately thirty years.

ExcerptReferenceRelevance
"Doxepin is an old tricyclic antidepressant, whose efficacy in chronic urticaria had been well documented until 1990. "( Doxepin in difficult-to-treat chronic urticaria: A retrospective, cross-sectional study from Turkey.
Babuna Kobaner, G; Kutlay, A; Özkaya, E; Yılmaz, Z, 2019
)
3.4
"Doxepin is a traditional tricyclic antidepressant with analgesic and anesthetic properties when applied topically to the mucosa. "( Modified biomolecule as potential vehicle for buccal delivery of doxepin.
Laffleur, F; Shuwisitkul, D; Zilio, M, 2016
)
2.11
"Doxepin is a tricyclic compound that has been used extensively for the treatment of depressive and anxiety disorders for approximately thirty years. "( Low-dose doxepin for the treatment of insomnia: emerging data.
Goforth, HW, 2009
)
2.21
"Doxepin is a tricyclic antidepressant with a subnanomolar affinity for the histamine H(1) (H(1)) receptor. "( Selective histamine H(1) antagonism: a novel approach to insomnia using low-dose doxepin.
Owen, RT, 2009
)
2.02
"Doxepin is a tricyclic antidepressant from the group of dibenzoxepines. "( [Prolonged toxic coma and anisocoria secondary to doxepin, lorazepam and phenobarbital poisoning--case study].
Kołodziej, M; Krajewska, A; Majewska, M; Szponar, J, 2012
)
2.07
"Doxepin is a tricyclic antidepressant formulated as a mixture of E-(trans) and Z-(cis) stereoisomers. "( Doxepin inhibits CYP2D6 activity in vivo.
Beszłej, JA; Kiejna, A; Milejski, P; Orzechowska-Juzwenko, K; Szewczuk-Bogusławska, M,
)
3.02
"Doxepin is a tricyclic antidepressant marketed as an irrational mixture of cis- and trans-geometric isomers in the ratio of 15:85. "( Stereoselective and simultaneous measurement of cis- and trans-isomers of doxepin and N-desmethyldoxepin in plasma or urine by high-performance liquid chromatography.
Hubbard, JW; McKay, G; Midha, KK; Yan, J, 1997
)
1.97
"Doxepin is a tricyclic antidepressant that is widely prescribed for the treatment of mild depression. "( Detection of doxepin and its major metabolite desmethyldoxepin in hair following drug therapy.
Moore, CM; Negrusz, A; Perry, JL, 1998
)
2.11

Effects

Doxepin has two saturable binding sites with higher and lower affinities in brains of wild-type mice. Oral doxepin rinse has been reported to provide pain relief in patients with oral mucosal lesions due to cancer or cancer therapy.

ExcerptReferenceRelevance
"Oral doxepin rinse has been reported to provide pain relief in patients with oral mucosal lesions due to cancer or cancer therapy. "( Oral topical doxepin rinse: anesthetic effect in normal subjects.
Epstein, JB; Epstein, MS; Le, ND; Oien, H; Truelove, EL, 2003
)
1.2
"[3H]Doxepin has two saturable binding sites with higher and lower affinities in brains of wild-type mice, but H1R-deficient mice showed only the weak labeling of [3H]doxepin that corresponds to lower-affinity binding sites."( Impaired locomotor activity and exploratory behavior in mice lacking histamine H1 receptors.
Inoue, I; Kitamura, D; Kobayashi, T; Niimura, K; Taniuchi, I; Watanabe, T; Yanai, K, 1996
)
0.77
"Doxepin has only a negative chronotropic effect."( Relationships between chronotropic effect, 1-3H-noradrenaline uptake and tissue concentrations of desipramine, protripyline and doxepin in rat isolated atria.
Bonaccorsi, A; Castelli, MG; Franco, R; Garattini, S; Morselli, PL, 1976
)
1.18
"Doxepin has gained favour for use in the geriatric population due to claims of low cardiovascular side effects."( Comparative plasma levels of doxepin and desipramine in the elderly.
Ancill, RJ; Gosselin, C, 1989
)
1.29

Treatment

Doxepin treatment over 3 days reduced ACH provoked flare size more than 53% (P<0.005) and wheal size about 48%. The maximal antipruritic effect was similiar to the basic therapy. Treatment with doxepin is a contraindication to driving during the first two weeks or up to the time when amelioration of symptoms is recorded.

ExcerptReferenceRelevance
"doxepine in the treatment of in-patients with severe depression."( A double-blind comparison of amitriptylinoxide versus doxepine in the treatment of severe depression.
Diehl, B; Heinrich, T; König, W, 1994
)
1.26
"Doxepin treatment over 3 days reduced ACH provoked flare size more than 53% (P<0.005) and wheal size about 48% (P<0.005) whereas the maximal antipruritic effect was similiar to the basic therapy. "( Doxepin affects acetylcholine induced cutaneous reactions in atopic eczema.
Groene, D; Heyer, G; Martus, P, 2001
)
3.2
"Doxepin-treated subjects experienced fewer lesions (p less than 0.001), less waking hours with lesions (p less than 0.01), lesser degree of itch and/or discomfort (p less than 0.001), and less swelling or angioedema (p less than 0.001) as compared to placebo-treated subjects."( Efficacy of doxepin in the treatment of chronic idiopathic urticaria.
Barr, RJ; Drayton, G; Goldsobel, AB; Indianer, L; Katz, RM; Peter, JB; Rachelefsky, GS; Rohr, AS; Siegel, SC; Spector, SL, 1986
)
1.37
"Treatment with doxepin is a contraindication to driving during the first two weeks or up to the time when amelioration of symptoms is recorded."( Psychomotor skills in depressed out-patients treated with L-tryptophan, doxepin, or chlorimipramine.
Linnoila, M; Mattila, MJ; Seppälä, T, 1978
)
0.83
"Treatment with doxepin results in clinical improvement, but no changes in mediator release were seen."( Cold urticaria as a model of mediator release: platelet factor 4, eosinophil cationic protein and histamine.
Benda, H; Götz, M; Hippmann, G; Jarisch, R; Rosenkranz, AR; Wekkeli, M, 1992
)
0.62

Toxicity

Doxepin was more neurotoxic than amitriptyline, and both imipramine and trimipramines were more toxic than desiprams. All 3 doxepin doses had side effect profiles comparable to placebo, with no spontaneously reported anticholinergic effects.

ExcerptReferenceRelevance
" The effect of pretreatment with five different beta-adrenoceptor blocking drugs (propranolol, alprenolol, practolol, metoprolol or tolamolol), p physostigmine, or atropine on these toxic actions of doxepin was investigated."( Effect of beta-adrenoceptor blocking drugs, physostigmine, and atropine on the toxicity of doxepin in mice.
Elonen, E, 1975
)
0.66
" Since tricyclic antidepressants and lithium are the most commonly used psychotropic drugs in the treatment of depression, their side effects and adverse reactions are discussed specifically as these relate to the elderly."( Antidepressant drug therapy in the elderly: enhancing safety and compliance.
Halaris, A,
)
0.13
" The toxic arrhythmogenic effects of the tricyclic antidepressants can be measured by RET and are partly autonomic tone manipulation."( Cardiotoxicity of amitriptyline and doxepin.
Aronow, WS; Tobis, JM, 1981
)
0.54
" Dx infused intravenously to conscious or anaesthetized guinea-pigs proved as cardiotoxic as amitriptyline but more toxic than protriptyline, thus confirming our previous results in rabbits."( Prostaglandins and the cardiotoxic effects of doxepin in rabbits and guinea-pigs.
Elonen, E; Eränkö, P; Mattila, MJ; Puisto, EL, 1980
)
0.52
" Physical exams, lab tests, cognitive functions (Buschke Selective Reminding Test, Hierarchic Dementia Scale, Word Fluency) and adverse reactions were also noted."( A comparison of the cardiac safety and therapeutic efficacy of trimipramine versus doxepin in geriatric depressed patients.
Amin, M; Dastoor, D; MacDonald, C; Mirmiran, J; Nair, NP; Phillips, R; Schwartz, G; Thavundayil, JX, 1993
)
0.51
"Trimipramine and doxepin are equally safe and effective antidepressants in the young-elderly."( A comparison of the cardiac safety and therapeutic efficacy of trimipramine versus doxepin in geriatric depressed patients.
Amin, M; Dastoor, D; MacDonald, C; Mirmiran, J; Nair, NP; Phillips, R; Schwartz, G; Thavundayil, JX, 1993
)
0.85
"To report adverse effects in a newborn infant whose mother had been treated with doxepin during pregnancy and while breast-feeding."( Adverse effects in a newborn infant breast-fed by a mother treated with doxepin.
Frey, OR; Scheidt, P; von Brenndorff, AI, 1999
)
0.76
" All adverse effects subsided within 48 hours after breast-feeding was stopped."( Adverse effects in a newborn infant breast-fed by a mother treated with doxepin.
Frey, OR; Scheidt, P; von Brenndorff, AI, 1999
)
0.54
"Despite the small doses of doxepin and its active metabolite ingested by breast-fed babies, there is a risk of accumulation and resultant adverse effects."( Adverse effects in a newborn infant breast-fed by a mother treated with doxepin.
Frey, OR; Scheidt, P; von Brenndorff, AI, 1999
)
0.83
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
0.32
" Specifically, doxepin was more neurotoxic than amitriptyline, and both imipramine and trimipramine were more toxic than desipramine or amitriptyline."( Differential neurotoxicity of tricyclic antidepressants and novel derivatives in vitro in a dorsal root ganglion cell culture model.
Gerner, P; Haller, I; Keller, C; Klimaschewski, L; Lirk, P; Wang, GK, 2007
)
0.69
" Safety analyses included measures of residual sedation and adverse events."( Efficacy and safety of doxepin 1 mg, 3 mg, and 6 mg in adults with primary insomnia.
Corser, B; Hull, S; Koshorek, G; Lankford, A; Rogowski, R; Roth, T; Schwartz, H; Seiden, D, 2007
)
0.65
" The side-effect profile was comparable to placebo, with no reported anticholinergic effects, no memory impairment, and no significant hangover/next-day residual effects."( Efficacy and safety of doxepin 1 mg, 3 mg, and 6 mg in adults with primary insomnia.
Corser, B; Hull, S; Koshorek, G; Lankford, A; Rogowski, R; Roth, T; Schwartz, H; Seiden, D, 2007
)
0.65
" All 3 doxepin doses had side effect profiles comparable to placebo, with no spontaneously reported anticholinergic effects, no memory impairment, and no significant next-day residual effects."( Efficacy and safety of doxepin 1 mg, 3 mg, and 6 mg in elderly patients with primary insomnia: a randomized, double-blind, placebo-controlled crossover study.
Cohn, M; Ereshefsky, L; Feldman, N; Hull, S; Lankford, A; Mayleben, D; Rogowski, R; Roth, T; Scharf, M, 2008
)
1.11
" The incidence of adverse events was comparable to placebo."( Efficacy and safety of doxepin 6 mg in a model of transient insomnia.
Heith Durrence, H; Jochelson, P; Lankford, A; Ludington, E; Peterson, G; Rogowski, R; Roth, T; Scharf, M, 2010
)
0.67
" These improvements were not accompanied by evidence of next-day residual sedation or other significant adverse effects."( Efficacy and Safety of Doxepin 1 mg and 3 mg in a 12-week Sleep Laboratory and Outpatient Trial of Elderly Subjects with Chronic Primary Insomnia.
Durrence, HH; Jochelson, P; Krystal, AD; Ludington, E; Rogowski, R; Roth, T; Scharf, M, 2010
)
0.67

Pharmacokinetics

We retrospectively analysed pharmacokinetic therapeutic drug-monitoring data in 114 psychiatric patients treated with doxepine for a period of 22-306 days. Stereoselective analysis showed a significant effect of the UM genotype on (E)-doxepin pharmacokinetics parameters. Those of (Z)-d Oxepin did not differ between CYP2D6 genotype groups.

ExcerptReferenceRelevance
" Results for total doxepin showed wide intersubject variation in all pharmacokinetic parameters except tmax and Cmax."( Stereoselective pharmacokinetics of doxepin isomers.
Cooper, JK; Gurnsey, T; Hawes, EM; Hubbard, JW; Korchinski, ED; McKay, G; Midha, KK; Schwede, R, 1992
)
0.89
"The selection of a starting dose for an antidepressant, and subsequent clinical titration to an appropriate therapeutic dosage, should be based on pharmacokinetic and pharmacodynamic principles."( Pharmacokinetic factors affecting antidepressant drug clearance and clinical effect: evaluation of doxepin and imipramine--new data and review.
Davis, CM; Ereshefsky, L; LeRoy, A; Tran-Johnson, T, 1988
)
0.49
"In eight healthy young volunteers, 15 g of activated charcoal administered orally 30 min after 50 mg of doxepin, reduced the achieved peak concentration of the drug in serum by 70% and total availability by 49%."( Effect of single and repeated doses of activated charcoal on the pharmacokinetics of doxepin.
Iisalo, E; Scheinin, M; Virtanen, R, 1985
)
0.71
" Serum samples were obtained and pharmacokinetic parameters estimated from the dose-normalized serum concentrations of doxepin and desmethyldoxepin."( Pharmacokinetics of doxepin in subjects with pruritic atopic dermatitis.
Cohen, L; Drake, LA; Flood, JG; Gillies, R; Phillips, SB; Riordan, AT; Stiller, MJ, 1999
)
0.84
"We retrospectively analysed pharmacokinetic therapeutic drug-monitoring data in 114 psychiatric patients (79 females, 35 males) treated with doxepine for a period of 22-306 days, mostly due to major depression."( Pharmacokinetics of doxepin and desmethyldoxepin: an evaluation with the population approach.
Gleiter, CH; Meineke, I; Meyer-Barner, M; Schreeb, KH, 2002
)
0.84
" The present pharmacokinetic study was a balanced, randomized, two-treatment, two-period, two-sequence crossover design in which 12 healthy male volunteers were given single doses of commercial doxepin intravenously and orally on two occasions separated by a washout period."( Absolute bioavailability and stereoselective pharmacokinetics of doxepin.
Hubbard, JW; Korchinski, ED; McKay, G; Midha, KK; Yan, JH, 2002
)
0.74
" Stereoselective analysis showed a significant effect of the UM genotype on (E)-doxepin pharmacokinetic parameters whereas those of (Z)-doxepin did not differ between the CYP2D6 genotype groups."( Impact of the CYP2D6 ultra-rapid metabolizer genotype on doxepin pharmacokinetics and serotonin in platelets.
Brockmöller, J; Franke, L; Henckel, HB; Kirchheiner, J; Meineke, I; Roots, I; Tzvetkov, M; Uebelhack, R, 2005
)
0.8
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
0.35
" One of these compounds, 10a, showed equivalent efficacy in a rat EEG/EMG model to a previously identified clinical candidate and a potentially superior pharmacokinetic profile as determined from a human microdose study."( Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
Beaton, G; Bradbury, MJ; Coon, T; Crowe, PD; Hernandez, LM; Hoare, SR; Huang, C; Jalali, K; Li, BF; Madan, A; Malany, S; Marinkovic, D; Moree, WJ; Petroski, RE; Sacaan, A; Tucci, FC; Wang, H; Wen, J; Yang, C; Yu, J; Zamani-Kord, S, 2010
)
0.36
"To uncover pharmacokinetic interactions between venlafaxine and doxepin or mirtazapine in a naturalistic sample."( Antidepressant polypharmacy and the potential of pharmacokinetic interactions: Doxepin but not mirtazapine causes clinically relevant changes in venlafaxine metabolism.
Fay, B; Gründer, G; Haen, E; Hiemke, C; Paulzen, M; Schoretsanitis, G; Unholzer, S, 2018
)
0.95

Bioavailability

The authors recommend routine monitoring of doxepin levels in the elderly. EMs had about 2-fold lower bioavailability compared with PMs indicating significant contribution of CYP2D6 to E-doxepin first-pass metabolism.

ExcerptReferenceRelevance
" The authors recommend routine monitoring of doxepin levels in the elderly and question poor bioavailability or absorption of this tricyclic antidepressant in some patients."( Comparative plasma levels of doxepin and desipramine in the elderly.
Ancill, RJ; Gosselin, C, 1989
)
0.83
" Relative bioavailability during concurrent cimetidine treatment was 123% of that during the control trial."( Doxepin-cimetidine interaction: increased doxepin bioavailability during cimetidine treatment.
Abernethy, DR; Todd, EL, 1986
)
1.71
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" The method is sensitive enough to be used in drug bioavailability studies with doxepin."( Determination of doxepin and desmethyldoxepin in human plasma using liquid chromatography-tandem mass spectrometry.
Badenhorst, D; de Jager, AD; Hundt, AF; Hundt, HK; Scanes, T; Sutherland, FC; Swart, KJ, 2000
)
0.87
" In addition, EMs had about 2-fold lower bioavailability compared with PMs indicating significant contribution of CYP2D6 to E-doxepin first-pass metabolism."( Contributions of CYP2D6, CYP2C9 and CYP2C19 to the biotransformation of E- and Z-doxepin in healthy volunteers.
Brockmöller, J; Kirchheiner, J; Meineke, I; Müller, G; Roots, I, 2002
)
0.75
" Diltiazem HCl ER tablets administered in the evening exhibited 17% and 22% greater bioavailability compared to morning administration under single-dose and steady-state conditions, respectively."( Pharmacokinetics of a novel diltiazem HCl extended-release tablet formulation for evening administration.
Albert, KS; Eradiri, O; Lai, JC; Sista, S, 2003
)
0.32

Dosage Studied

Doxepin had a cardiodepressant action, or favoured or initiated arrhythmias and/or ventricular conduction disorders. The method has been applied to analyses of plasma and urine samples from human volunteers and animals dosed with doxepin.

ExcerptRelevanceReference
"This work was aimed at clarifying whether the anti-depressant doxepin had a cardiodepressant action, or favoured or initiated arrhythmias and/or ventricular conduction disorders, when administered orally for 14 days at a daily dosage of 75 mg."( [The influence of doxepin on the efficiancy of the human heart (author's transl)].
Frisch, P; Klepzig, H; Wolter, H, 1977
)
0.83
" Dosage ranged from 50-225 mg daily, and treatment lasted from 2-26 weeks."( A review of controlled studies with nomifensine, performed outside the UK.
Habermann, W, 1977
)
0.26
"), and repeated after changing the dosage schedule to a single daily bedtime (h."( Dosage schedule and plasma levels of doxepin and desmethyldoxepin.
Biggs, JT; Meyer, DA; Preskorn, SH; Rosen, SH; Ziegler, VE, 1978
)
0.53
" Dose-response graphs for the tyramine pressor effect were shifted to the right during the antidepressant treatment, indicating a blockade of the membrane pump in peripheral sympathetic terminals."( Effect of tricyclic antidepressants and alcohol in psychomotor skills related to driving.
Elonen, E; Linnoila, M; Mäki, M; Mattila, MJ; Seppälä, T, 1975
)
0.25
" The following methods were used: a) gastric acid hypersecretion induced by histamine and carbachol in the pylorus-ligated rat preparation; b) contractile dose-response curves to histamine and carbachol in the guinea pig ileum; c) dimaprit-stimulated guinea pig atrium in vitro."( Mechanism of action of doxepin in the treatment of chronic urticaria.
Almeida, L; Figueiredo, A; Gonçalo, M; Poiares-Baptista, A; Ribeiro, CA; Teixeira, F, 1990
)
0.59
"A 46-year-old man suffering from neurotic depression complicated by alcohol and benzodiazepine dependence developed Coombs'-positive hemolytic anemia and thrombocytopenia with acute renal failure after 5 weeks of monotherapy with doxepin at a final dosage of 100 mg daily."( A case of immune complex hemolytic anemia, thrombocytopenia, and acute renal failure associated with doxepin use.
Conradty, M; Grohmann, R; Londong, V; Rüther, E; Witzgall, H; Wolf, B, 1989
)
0.68
" In the past decade, therapeutic monitoring of antidepressant drugs and use of pharmacokinetic principles have been shown to be an improvement over the dose-response approach."( Pharmacokinetic factors affecting antidepressant drug clearance and clinical effect: evaluation of doxepin and imipramine--new data and review.
Davis, CM; Ereshefsky, L; LeRoy, A; Tran-Johnson, T, 1988
)
0.49
" Regardless of the reason for use, nonpsychiatric physicians were found to use relatively low dosages, rarely plan or effect dosage increases, and rarely discontinue medication."( Antidepressant treatment of medical-surgical inpatients by nonpsychiatric physicians.
Callies, AL; Popkin, MK, 1987
)
0.27
" If these phenomena can be more carefully documented they may assume clinical importance; indeed for 2 of the patients studied the falling plasma concentrations on a steady dosage were associated with a recurrence of depression."( Doxepin plasma concentrations in clinical practice. Could there be a pharmacokinetic explanation for low concentrations?
Joyce, PR; Sharman, JR,
)
1.57
" Some improvements were observed after 1 week of treatment; the most improvement occurred at 6 weeks, when the mean doxepin dosage was approximately 200 mg/day and plasma doxepin and nordoxepin averaged 80 ng/ml."( Doxepin's effects on chronic pain and depression: a controlled study.
Cork, RC; Crago, BR; Davis, TP; Hameroff, SR; Lerman, JC; Neuman, CP; Watts, KS; Weiss, JL; Womble, JR, 1984
)
1.92
" A significant positive correlation was obtained between dosage and blood levels of maprotiline and doxepin, but there was no correlation between blood levels and clinical response."( Therapeutic superiority of maprotiline versus doxepin in geriatric depression.
Ahles, S; DeMet, E; Gwirtsman, HE; Halaris, A; Hill, MA, 1983
)
0.74
" Dose-response studies were carried out on different days with increasing doses of doxepin on a constant background stimulation with pentagastrin and with increasing doses of pentagastrin in combination with a constant dose of doxepin."( Effect of doxepin on gastric secretion in man.
Andersen, OK; Burhol, P; Giercksky, KE; Oyen, D, 1984
)
0.9
" Mean DMD t1/2 was not significantly affected by multiple dosing (34."( Multiple-dose doxepin kinetics in depressed patients.
Fann, WE; Faulkner, RD; Lee, CS; Lewis, WA; Pitts, WM, 1983
)
0.63
" The dialysis experiments show that modification of the usual dosage regimen is not necessary during hemodialysis or on dialysis days."( Hemodialysis of doxepin and desmethyldoxepin in uremic patients.
Faulkner, RD; Lee, CS; Senekjian, HO, 1984
)
0.61
"A study of 23 patients (16 females, 7 males), diagnosed as suffering from anxiety, was carried out using a flexible dosage regimen of doxepin."( Doxepin plasma levels and anxiolytic response.
Bianchi, GN; Burrows, GD; Maguire, KP; Norman, TR; Wurm, JM, 1980
)
1.91
" Doxepin daily dosage (administered in four divided doses) subsequently was reduced from 175 to 150 to 125 mg, then both drugs were discontinued."( Doxepin-induced acute glossitis.
Ives, TJ; Stewart, RB, 1980
)
2.61
"Placebo for 1 week, 2 weeks of titration with either drug in the dosage range of 75 mg/day up to a maximum of 200 mg/day."( A comparison of the cardiac safety and therapeutic efficacy of trimipramine versus doxepin in geriatric depressed patients.
Amin, M; Dastoor, D; MacDonald, C; Mirmiran, J; Nair, NP; Phillips, R; Schwartz, G; Thavundayil, JX, 1993
)
0.51
"Doctors' prescription and dosing behaviour was investigated using data from 9 clinical trials in 550 patients treated with psychotropics."( Correct titration of non-drugs and some other methodological issues.
Beneke, M; Fritze, J; Rasmus, W; Rød, IS, 1994
)
0.29
" Two groups of 22 patients each received amitriptylinoxide and doxepine respectively at a daily dosage of 120-360 mg for a period of 4 weeks."( A double-blind comparison of amitriptylinoxide versus doxepine in the treatment of severe depression.
Diehl, B; Heinrich, T; König, W, 1994
)
0.78
" Additional information is given on drug selection and dosage titration."( A guide to the understanding and use of tricyclic antidepressants in the overall management of fibromyalgia and other chronic pain syndromes.
Godfrey, RG, 1996
)
0.29
" The method has been applied to analyses of plasma and urine samples from human volunteers and animals dosed with doxepin."( Stereoselective and simultaneous measurement of cis- and trans-isomers of doxepin and N-desmethyldoxepin in plasma or urine by high-performance liquid chromatography.
Hubbard, JW; McKay, G; Midha, KK; Yan, J, 1997
)
0.74
" Marked sedation occurred in three of the first 10 subjects treated with topical doxepin, necessitating a reduction in dosage for the remaining six subjects."( The effects of topical doxepin on responses to histamine, substance P and prostaglandin E2 in human skin.
Archer, CB; Kennedy, CT; Sabroe, RA, 1997
)
0.83
"A sensitive spectrophotometric method for the determination of amitriptyline hydrochloride, nortriptyline hydrochloride and doxepin hydrochloride in pure and dosage forms, is described."( Spectrophotometric determination of some antidepressant drugs using 3-methylbenzothiazolin-2-one hydrazone.
Manju, B; Revanasiddappa, HD, 1999
)
0.51
" Various dosage forms of nicotine replacement therapy increase smoking quit rates relative to placebo, but they generally do not result in 1-year quit rates of over 20%."( Effect of nonnicotine pharmacotherapy on smoking behavior.
Golding, M; Hatsukami, DK; Jamerson, BD; Kotlyar, M, 2001
)
0.31
" Patients were treated with either amitriptyline (n = 69) or doxepin (n = 15); the mean dosage at endpoint was 126 +/- 35 mg and 155 +/- 47 mg, respectively."( Therapeutic drug monitoring of tricyclic antidepressants: how does it work under clinical conditions?
Dragicevic, A; Fric, M; Gaertner, I; Grasmäder, K; Härtter, S; Hermann, E; Hiemke, C; Kuss, HJ; Laux, G; Müller, MJ; Oehl, W; Rao, ML; Rollmann, N; Weber-Labonte, M; Weigmann, H, 2003
)
0.56
"A self-control and follow-up study on subclinical dosage of antidepressants therapy (fluoxetine 10 mg/d, paroxetine 10 mg/d or doxepin 45 mg/d) for 9-12 wks in 46 patients with refractory IBS symptoms according to Rome II criteria was performed, the clinical outcomes were evaluated by scales changes of symptom-related-anxiety, severity index of symptom, and quality of life specific of IBS, as well as general psychiatric health by SCL-90 during treatment and follow-up periods."( [Treatment of refractory irritable bowel syndrome with subclinical dosage of antidepressants].
Pan, GZ; Qian, JM; Wang, WA, 2003
)
0.52
"Treatment of refractory IBS with subclinical dosage antidepressant is rational and effective, However a further study on its mechanisms is suggested."( [Treatment of refractory irritable bowel syndrome with subclinical dosage of antidepressants].
Pan, GZ; Qian, JM; Wang, WA, 2003
)
0.32
" The proposed methods have been successfully applied for the analysis of the drug in dosage forms."( Extractive spectrophotometric methods for the determination of doxepin hydrochloride in pharmaceutical preparations using titanium (IV) and iron (III) thiocyanate complexes.
Misiuk, W, 2005
)
0.57
"Average maximum daily dosage was 83 mg/d in the control and 95 mg/d in the intervention group (F=19."( A randomized controlled clinical trial comparing "guideline exposed" and "guideline naive" physicians in respect to dosage selection and treatment outcome with doxepin in depressive disorders.
Linden, M; Schotte, K, 2007
)
0.54
" It is therefore probable that the defective genotype has contributed to the death, possibly involving repeated high dosage of doxepin."( A fatal doxepin poisoning associated with a defective CYP2D6 genotype.
Koski, A; Ojanperä, I; Sajantila, A; Sistonen, J; Vuori, E, 2007
)
0.98
" Patients recalled that their pain significantly dropped within 5 minutes of rinsing over the week of repeated dosing (p < ."( Doxepin rinse for management of mucositis pain in patients with cancer: one week follow-up of topical therapy.
Epstein, JB; Epstein, JD; Epstein, MS; Oien, H; Truelove, EL,
)
1.57
" Although these clinical actions are classically attributed to blockade of the H1 receptor, recent findings with H1 selective agents and H1 selective dosing of older agents are challenging these notions and suggest that some of the clinical limitations of current H1-blocking agents at their currently utilized doses could be attributable to other properties of these drugs, especially to their simultaneous actions on muscarinic, cholinergic, and adrenergic receptors."( Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines.
Stahl, SM, 2008
)
0.35
" Rats dosed with 30 and 60 mg/kg (R)-dimethindene showed 42% and 67% occupancy of central H1 receptors, respectively."( Analytical method for simultaneously measuring ex vivo drug receptor occupancy and dissociation rate: application to (R)-dimethindene occupancy of central histamine H1 receptors.
Crowe, PD; Hernandez, LM; Hoare, SR; Malany, S; Smith, WF, 2009
)
0.35
" The evaluation of the time-course and dose-response relationships for doxepin provided evidence that the peak maximum anticonvulsant activity and acute adverse effects occurred 5 min after intraperitoneal (ip) administration."( Characterization of the anticonvulsant activity of doxepin in various experimental seizure models in mice.
Piao, HR; Quan, ZS; Sun, XY; Wei, CX; Zhang, L,
)
0.62
" Dox concentration measured from two cases was well within a concentration range considered therapeutic, whereas subtherapeutic dosing may have occurred in another two cases."( Doxepin and nordoxepin concentrations in body fluids and tissues in doxepin associated deaths.
Dettling, A; Gronewold, A; Haffner, HT; Skopp, G, 2009
)
1.8
"A novel spectrofluorimetric method has been developed for the determination of doxepin hydrochloride in commercial dosage forms."( Spectrofluorimetric method for the determination of doxepin hydrochloride in commercial dosage forms.
Azmi, SN; Rahman, N; Siddiqui, S, 2009
)
0.83
"In this investigation the effects of tricyclic drugs on cellular respiration were studied using the anaplastic astrocytoma cell line IPSB-18 by use of a Clark-type oxygen electrode which measured changes in cellular respiration rate (oxygen consumption), in a dose-response assay."( The in vitro effects of tricyclic drugs and dexamethasone on cellular respiration of malignant glioma.
Higgins, SC; Pilkington, GJ, 2010
)
0.36
" The plasma concentration of both doxepin and nordoxepin correlated significantly with the oral dosage of doxepin (doxepin: r = +0."( Doxepin concentrations in plasma and cerebrospinal fluid.
Fassbender, K; Maurer, HH; Remane, D; Schomburg, R; Spiegel, J, 2011
)
2.09
" As a consequence, if a combination of valproic acid with doxepin or venlafaxine is administered, cautious dosing is advisable and TDM should be performed."( Interaction of valproic acid and the antidepressant drugs doxepin and venlafaxine: analysis of therapeutic drug monitoring data under naturalistic conditions.
Deckert, J; Hempel, S; Pfuhlmann, B; Proft, F; Reif, A; Riederer, P; Unterecker, S, 2014
)
0.89
" One problem associated with the mucosal administration routes is the short residence time of the dosage form on the mucosal membranes."( Design, development and characterization of buccal bioadhesive films of Doxepin for treatment of odontalgia.
Castán, H; Clares, B; Morales, ME; Ruiz, MA, 2015
)
0.65
" Hence, a different dosing strategy is required among smoking and nonsmoking patients."( Analysis of smoking behavior on the pharmacokinetics of antidepressants and antipsychotics: evidence for the role of alternative pathways apart from CYP1A2.
Deckert, J; Hommers, LG; Menke, A; Samanski, L; Scherf-Clavel, M; Unterecker, S, 2019
)
0.51
" Blood level monitoring is introduced, a tool dermatologists can use to optimize doxepin dosing in patients responding subtherapeutically to typical dermatologic doses."( Optimizing doxepin therapy in dermatology: introducing blood level monitoring and genotype testing.
Brownstone, N; Chan, S; Koo, J; Myers, B; Reddy, V; Thibodeaux, Q, 2022
)
1.34
" Toxicity may result from dosing error, CYP2C19 and CYP2D6 genetic variability, and drug-drug interactions."( Chronic Doxepin Toxicity Masquerading as Epilepsy in a 10-Year-Old Boy.
Burns, MM; Watson, CJ; Whitledge, JD, 2023
)
1.34
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antidepressantAntidepressants are mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (2)

ClassDescription
dibenzooxepine
tertiary amino compoundA compound formally derived from ammonia by replacing three hydrogen atoms by organyl groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (2)

PathwayProteinsCompounds
Doxepin Metabolism Pathway516
Doxepin H1-Antihistamine Action87

Protein Targets (46)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier family 22 member 1 Homo sapiens (human)IC50 (µMol)11.19000.21005.553710.0000AID1442001
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)133.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)133.00000.20005.677410.0000AID1473741
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)IC50 (µMol)0.04600.00011.00768.7800AID625218
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)Ki0.02400.00000.887110.0000AID625218
Bile salt export pumpHomo sapiens (human)IC50 (µMol)134.00000.11007.190310.0000AID1443980; AID1473738
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)0.02900.00041.877310.0000AID625207
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki0.02900.00322.28879.3160AID625207
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC50 (µMol)0.25800.00001.23267.7930AID625152
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.09200.00000.690210.0000AID625152
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC50 (µMol)0.04200.00001.15467.5858AID625154
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.00580.00000.79519.1201AID625154
5-hydroxytryptamine receptor 2CRattus norvegicus (Norway rat)IC50 (µMol)0.20000.00040.629810.0000AID6418
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC50 (µMol)0.02600.00010.99178.0000AID625155
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.01900.00000.72926.9183AID625155
Alpha-2A adrenergic receptorHomo sapiens (human)IC50 (µMol)0.66750.00001.44217.3470AID36031; AID625201
Alpha-2A adrenergic receptorHomo sapiens (human)Ki0.50100.00010.807410.0000AID625201
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)0.07700.00001.403910.0000AID625151
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.01800.00000.59729.1201AID625151
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)IC50 (µMol)0.20000.00040.908610.0000AID6418
Alpha-2B adrenergic receptorHomo sapiens (human)IC50 (µMol)0.03550.00001.23808.1590AID36031; AID625202
Alpha-2B adrenergic receptorHomo sapiens (human)Ki0.03200.00020.725710.0000AID625202
Alpha-2C adrenergic receptorHomo sapiens (human)IC50 (µMol)0.51450.00001.47257.8980AID36031; AID625203
Alpha-2C adrenergic receptorHomo sapiens (human)Ki0.15000.00030.483410.0000AID625203
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)IC50 (µMol)0.85950.00031.38338.4000AID625190; AID6418
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.86800.00010.739610.0000AID625190
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC50 (µMol)0.06900.00011.01049.9280AID625153
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.01500.00000.54057.7600AID625153
D(1A) dopamine receptorHomo sapiens (human)IC50 (µMol)0.68800.00031.84739.2250AID625252
D(1A) dopamine receptorHomo sapiens (human)Ki0.34400.00010.836310.0000AID625252
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC50 (µMol)0.02900.00081.541620.0000AID625207
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki0.02900.00031.465610.0000AID625207
Histamine H2 receptorHomo sapiens (human)IC50 (µMol)1.86700.02202.298710.0000AID625270
Histamine H2 receptorHomo sapiens (human)Ki1.83600.00062.197310.0000AID625270
Alpha-1D adrenergic receptorHomo sapiens (human)IC50 (µMol)0.11800.00020.75688.8970AID625200
Alpha-1D adrenergic receptorHomo sapiens (human)Ki0.05800.00000.360910.0000AID625200
5-hydroxytryptamine receptor 2AHomo sapiens (human)IC50 (µMol)0.03800.00010.88018.8500AID625192
5-hydroxytryptamine receptor 2AHomo sapiens (human)Ki0.01100.00000.385510.0000AID625192
5-hydroxytryptamine receptor 2CHomo sapiens (human)IC50 (µMol)0.04600.00011.03029.0000AID625218
5-hydroxytryptamine receptor 2CHomo sapiens (human)Ki0.02400.00010.954910.0000AID625218
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC50 (µMol)0.85950.00051.48357.8000AID625190; AID6418
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)Ki0.86800.00031.29679.2440AID625190
5-hydroxytryptamine receptor 1DRattus norvegicus (Norway rat)IC50 (µMol)0.20000.00311.73607.8000AID6418
5-hydroxytryptamine receptor 1FRattus norvegicus (Norway rat)IC50 (µMol)0.20000.00501.79627.8000AID6418
5-hydroxytryptamine receptor 2BRattus norvegicus (Norway rat)IC50 (µMol)0.20000.00040.615610.0000AID6418
5-hydroxytryptamine receptor 6Rattus norvegicus (Norway rat)IC50 (µMol)0.20000.00501.50894.6000AID6418
Histamine H1 receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00000.00000.32271.2589AID87513
Sodium-dependent serotonin transporterHomo sapiens (human)IC50 (µMol)0.04200.00010.86458.7096AID625222
Sodium-dependent serotonin transporterHomo sapiens (human)Ki0.02200.00000.70488.1930AID625222
5-hydroxytryptamine receptor 7 Rattus norvegicus (Norway rat)IC50 (µMol)0.20000.00501.42824.6000AID6418
5-hydroxytryptamine receptor 5ARattus norvegicus (Norway rat)IC50 (µMol)0.20000.00501.35984.6000AID6418
5-hydroxytryptamine receptor 5BRattus norvegicus (Norway rat)IC50 (µMol)0.20000.00501.35984.6000AID6418
Histamine H1 receptorHomo sapiens (human)IC50 (µMol)0.00060.00000.44365.1768AID625269
Histamine H1 receptorHomo sapiens (human)Ki0.00020.00000.511010.0000AID1327714; AID625269; AID632679
D(3) dopamine receptorHomo sapiens (human)IC50 (µMol)1.39300.00011.01788.7960AID625254
D(3) dopamine receptorHomo sapiens (human)Ki0.47300.00000.602010.0000AID625254
5-hydroxytryptamine receptor 3ARattus norvegicus (Norway rat)IC50 (µMol)0.20000.00021.13514.6000AID6418
5-hydroxytryptamine receptor 2BHomo sapiens (human)IC50 (µMol)0.08900.00011.18738.9125AID625217
5-hydroxytryptamine receptor 2BHomo sapiens (human)Ki0.05600.00030.769310.0000AID625217
Alpha-1A adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)0.00000.00001.819410.0000AID36031
Histamine H2 receptorCavia porcellus (domestic guinea pig)IC50 (µMol)1.60000.00402.15557.2000AID87880
5-hydroxytryptamine receptor 6Homo sapiens (human)IC50 (µMol)0.32000.00170.83815.4200AID625221
5-hydroxytryptamine receptor 6Homo sapiens (human)Ki0.12700.00020.522910.0000AID625221; AID691260
5-hydroxytryptamine receptor 4 Rattus norvegicus (Norway rat)IC50 (µMol)0.20000.00501.35524.6000AID6418
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
Sigma non-opioid intracellular receptor 1Homo sapiens (human)IC50 (µMol)0.63100.00030.70285.3660AID625223
Sigma non-opioid intracellular receptor 1Homo sapiens (human)Ki0.26500.00000.490110.0000AID625223
5-hydroxytryptamine receptor 3BRattus norvegicus (Norway rat)IC50 (µMol)0.20000.00041.17424.6000AID6418
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H1 receptorCavia porcellus (domestic guinea pig)K0.50.00020.00020.10290.5480AID88625
Histamine H2 receptorCavia porcellus (domestic guinea pig)K0.50.00010.00010.40364.8000AID88008
Histamine H3 receptorCavia porcellus (domestic guinea pig)K0.50.00020.00020.10290.5480AID88625
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (308)

Processvia Protein(s)Taxonomy
xenobiotic metabolic processSolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin transportSolute carrier family 22 member 1 Homo sapiens (human)
establishment or maintenance of transmembrane electrochemical gradientSolute carrier family 22 member 1 Homo sapiens (human)
organic cation transportSolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transportSolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transportSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transportSolute carrier family 22 member 1 Homo sapiens (human)
putrescine transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transportSolute carrier family 22 member 1 Homo sapiens (human)
acetylcholine transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine transportSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transportSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transportSolute carrier family 22 member 1 Homo sapiens (human)
epinephrine transportSolute carrier family 22 member 1 Homo sapiens (human)
serotonin uptakeSolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
metanephric proximal tubule developmentSolute carrier family 22 member 1 Homo sapiens (human)
purine-containing compound transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
dopamine uptakeSolute carrier family 22 member 1 Homo sapiens (human)
monoatomic cation transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
acyl carnitine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transportSolute carrier family 22 member 1 Homo sapiens (human)
cellular detoxificationSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transport across blood-brain barrierSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of cytokine productionAlpha-2A adrenergic receptorHomo sapiens (human)
DNA replicationAlpha-2A adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
Ras protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
Rho protein signal transductionAlpha-2A adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2A adrenergic receptorHomo sapiens (human)
actin cytoskeleton organizationAlpha-2A adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of cell migrationAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2A adrenergic receptorHomo sapiens (human)
cellular response to hormone stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2A adrenergic receptorHomo sapiens (human)
vasodilationAlpha-2A adrenergic receptorHomo sapiens (human)
glucose homeostasisAlpha-2A adrenergic receptorHomo sapiens (human)
fear responseAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of potassium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAP kinase activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion-dependent exocytosisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2A adrenergic receptorHomo sapiens (human)
intestinal absorptionAlpha-2A adrenergic receptorHomo sapiens (human)
thermoceptionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of lipid catabolic processAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of membrane protein ectodomain proteolysisAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transportAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretion involved in cellular response to glucose stimulusAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of uterine smooth muscle contractionAlpha-2A adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
adenylate cyclase-inhibiting adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
phospholipase C-activating adrenergic receptor signaling pathwayAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of wound healingAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionAlpha-2A adrenergic receptorHomo sapiens (human)
negative regulation of calcium ion transmembrane transporter activityAlpha-2A adrenergic receptorHomo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
angiogenesisAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of vascular associated smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2B adrenergic receptorHomo sapiens (human)
female pregnancyAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2B adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2B adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2B adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of blood pressureAlpha-2B adrenergic receptorHomo sapiens (human)
positive regulation of uterine smooth muscle contractionAlpha-2B adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2B adrenergic receptorHomo sapiens (human)
regulation of smooth muscle contractionAlpha-2C adrenergic receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of norepinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
regulation of vasoconstrictionAlpha-2C adrenergic receptorHomo sapiens (human)
platelet activationAlpha-2C adrenergic receptorHomo sapiens (human)
activation of protein kinase B activityAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of epinephrine secretionAlpha-2C adrenergic receptorHomo sapiens (human)
receptor transactivationAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-2C adrenergic receptorHomo sapiens (human)
positive regulation of neuron differentiationAlpha-2C adrenergic receptorHomo sapiens (human)
adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-2C adrenergic receptorHomo sapiens (human)
negative regulation of insulin secretionAlpha-2C adrenergic receptorHomo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
temperature homeostasisD(1A) dopamine receptorHomo sapiens (human)
conditioned taste aversionD(1A) dopamine receptorHomo sapiens (human)
behavioral fear responseD(1A) dopamine receptorHomo sapiens (human)
regulation of protein phosphorylationD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(1A) dopamine receptorHomo sapiens (human)
response to amphetamineD(1A) dopamine receptorHomo sapiens (human)
protein import into nucleusD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
activation of adenylate cyclase activityD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
synapse assemblyD(1A) dopamine receptorHomo sapiens (human)
memoryD(1A) dopamine receptorHomo sapiens (human)
mating behaviorD(1A) dopamine receptorHomo sapiens (human)
grooming behaviorD(1A) dopamine receptorHomo sapiens (human)
adult walking behaviorD(1A) dopamine receptorHomo sapiens (human)
visual learningD(1A) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(1A) dopamine receptorHomo sapiens (human)
astrocyte developmentD(1A) dopamine receptorHomo sapiens (human)
dopamine transportD(1A) dopamine receptorHomo sapiens (human)
transmission of nerve impulseD(1A) dopamine receptorHomo sapiens (human)
neuronal action potentialD(1A) dopamine receptorHomo sapiens (human)
dentate gyrus developmentD(1A) dopamine receptorHomo sapiens (human)
striatum developmentD(1A) dopamine receptorHomo sapiens (human)
cerebral cortex GABAergic interneuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of cell migrationD(1A) dopamine receptorHomo sapiens (human)
peristalsisD(1A) dopamine receptorHomo sapiens (human)
operant conditioningD(1A) dopamine receptorHomo sapiens (human)
synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
vasodilationD(1A) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(1A) dopamine receptorHomo sapiens (human)
maternal behaviorD(1A) dopamine receptorHomo sapiens (human)
positive regulation of potassium ion transportD(1A) dopamine receptorHomo sapiens (human)
glucose importD(1A) dopamine receptorHomo sapiens (human)
habituationD(1A) dopamine receptorHomo sapiens (human)
sensitizationD(1A) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(1A) dopamine receptorHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolD(1A) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicD(1A) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(1A) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic potentiationD(1A) dopamine receptorHomo sapiens (human)
long-term synaptic depressionD(1A) dopamine receptorHomo sapiens (human)
cellular response to catecholamine stimulusD(1A) dopamine receptorHomo sapiens (human)
modification of postsynaptic structureD(1A) dopamine receptorHomo sapiens (human)
presynaptic modulation of chemical synaptic transmissionD(1A) dopamine receptorHomo sapiens (human)
positive regulation of neuron migrationD(1A) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(1A) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
dopamine receptor signaling pathwayD(1A) dopamine receptorHomo sapiens (human)
monoamine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transportSodium-dependent noradrenaline transporter Homo sapiens (human)
chemical synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
response to xenobiotic stimulusSodium-dependent noradrenaline transporter Homo sapiens (human)
response to painSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine uptakeSodium-dependent noradrenaline transporter Homo sapiens (human)
neuron cellular homeostasisSodium-dependent noradrenaline transporter Homo sapiens (human)
amino acid transportSodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine transportSodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine uptake involved in synaptic transmissionSodium-dependent noradrenaline transporter Homo sapiens (human)
sodium ion transmembrane transportSodium-dependent noradrenaline transporter Homo sapiens (human)
gastric acid secretionHistamine H2 receptorHomo sapiens (human)
immune responseHistamine H2 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H2 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H2 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cell population proliferationAlpha-1D adrenergic receptorHomo sapiens (human)
neuron-glial cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
cell-cell signalingAlpha-1D adrenergic receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of vasoconstrictionAlpha-1D adrenergic receptorHomo sapiens (human)
positive regulation of MAPK cascadeAlpha-1D adrenergic receptorHomo sapiens (human)
temperature homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytokine production involved in immune response5-hydroxytryptamine receptor 2AHomo sapiens (human)
glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2AHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cytosolic calcium ion concentration5-hydroxytryptamine receptor 2AHomo sapiens (human)
memory5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2AHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
regulation of dopamine secretion5-hydroxytryptamine receptor 2AHomo sapiens (human)
artery smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
urinary bladder smooth muscle contraction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of heat generation5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of potassium ion transport5-hydroxytryptamine receptor 2AHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of neuron apoptotic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein localization to cytoskeleton5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of glycolytic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of vasoconstriction5-hydroxytryptamine receptor 2AHomo sapiens (human)
symbiont entry into host cell5-hydroxytryptamine receptor 2AHomo sapiens (human)
sensitization5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral response to cocaine5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of inflammatory response5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylation5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of temperature stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
detection of mechanical stimulus involved in sensory perception of pain5-hydroxytryptamine receptor 2AHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2AHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergic5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic modulation of chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of execution phase of apoptosis5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of platelet aggregation5-hydroxytryptamine receptor 2AHomo sapiens (human)
positive regulation of DNA biosynthetic process5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2AHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2AHomo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 2CHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
locomotory behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
feeding behavior5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2CHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of nervous system process5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of appetite5-hydroxytryptamine receptor 2CHomo sapiens (human)
regulation of corticotropin-releasing hormone secretion5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of fat cell differentiation5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of calcium-mediated signaling5-hydroxytryptamine receptor 2CHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2CHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2CHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2CHomo sapiens (human)
monoamine transportSodium-dependent serotonin transporterHomo sapiens (human)
response to hypoxiaSodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transportSodium-dependent serotonin transporterHomo sapiens (human)
response to nutrientSodium-dependent serotonin transporterHomo sapiens (human)
memorySodium-dependent serotonin transporterHomo sapiens (human)
circadian rhythmSodium-dependent serotonin transporterHomo sapiens (human)
response to xenobiotic stimulusSodium-dependent serotonin transporterHomo sapiens (human)
response to toxic substanceSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of gene expressionSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of serotonin secretionSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of cerebellar granule cell precursor proliferationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of synaptic transmission, dopaminergicSodium-dependent serotonin transporterHomo sapiens (human)
response to estradiolSodium-dependent serotonin transporterHomo sapiens (human)
social behaviorSodium-dependent serotonin transporterHomo sapiens (human)
vasoconstrictionSodium-dependent serotonin transporterHomo sapiens (human)
sperm ejaculationSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of neuron differentiationSodium-dependent serotonin transporterHomo sapiens (human)
positive regulation of cell cycleSodium-dependent serotonin transporterHomo sapiens (human)
negative regulation of organ growthSodium-dependent serotonin transporterHomo sapiens (human)
behavioral response to cocaineSodium-dependent serotonin transporterHomo sapiens (human)
enteric nervous system developmentSodium-dependent serotonin transporterHomo sapiens (human)
brain morphogenesisSodium-dependent serotonin transporterHomo sapiens (human)
serotonin uptakeSodium-dependent serotonin transporterHomo sapiens (human)
membrane depolarizationSodium-dependent serotonin transporterHomo sapiens (human)
platelet aggregationSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to retinoic acidSodium-dependent serotonin transporterHomo sapiens (human)
cellular response to cGMPSodium-dependent serotonin transporterHomo sapiens (human)
regulation of thalamus sizeSodium-dependent serotonin transporterHomo sapiens (human)
conditioned place preferenceSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion transmembrane transportSodium-dependent serotonin transporterHomo sapiens (human)
amino acid transportSodium-dependent serotonin transporterHomo sapiens (human)
inflammatory responseHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
memoryHistamine H1 receptorHomo sapiens (human)
visual learningHistamine H1 receptorHomo sapiens (human)
regulation of vascular permeabilityHistamine H1 receptorHomo sapiens (human)
positive regulation of vasoconstrictionHistamine H1 receptorHomo sapiens (human)
regulation of synaptic plasticityHistamine H1 receptorHomo sapiens (human)
cellular response to histamineHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayHistamine H1 receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerHistamine H1 receptorHomo sapiens (human)
chemical synaptic transmissionHistamine H1 receptorHomo sapiens (human)
response to ethanolD(3) dopamine receptorHomo sapiens (human)
synaptic transmission, dopaminergicD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor internalizationD(3) dopamine receptorHomo sapiens (human)
intracellular calcium ion homeostasisD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-inhibiting dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
learning or memoryD(3) dopamine receptorHomo sapiens (human)
learningD(3) dopamine receptorHomo sapiens (human)
locomotory behaviorD(3) dopamine receptorHomo sapiens (human)
visual learningD(3) dopamine receptorHomo sapiens (human)
response to xenobiotic stimulusD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine secretionD(3) dopamine receptorHomo sapiens (human)
positive regulation of cytokinesisD(3) dopamine receptorHomo sapiens (human)
circadian regulation of gene expressionD(3) dopamine receptorHomo sapiens (human)
response to histamineD(3) dopamine receptorHomo sapiens (human)
social behaviorD(3) dopamine receptorHomo sapiens (human)
response to cocaineD(3) dopamine receptorHomo sapiens (human)
dopamine metabolic processD(3) dopamine receptorHomo sapiens (human)
response to morphineD(3) dopamine receptorHomo sapiens (human)
negative regulation of blood pressureD(3) dopamine receptorHomo sapiens (human)
positive regulation of mitotic nuclear divisionD(3) dopamine receptorHomo sapiens (human)
acid secretionD(3) dopamine receptorHomo sapiens (human)
behavioral response to cocaineD(3) dopamine receptorHomo sapiens (human)
negative regulation of oligodendrocyte differentiationD(3) dopamine receptorHomo sapiens (human)
arachidonic acid secretionD(3) dopamine receptorHomo sapiens (human)
negative regulation of protein secretionD(3) dopamine receptorHomo sapiens (human)
musculoskeletal movement, spinal reflex actionD(3) dopamine receptorHomo sapiens (human)
regulation of dopamine uptake involved in synaptic transmissionD(3) dopamine receptorHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionD(3) dopamine receptorHomo sapiens (human)
prepulse inhibitionD(3) dopamine receptorHomo sapiens (human)
positive regulation of dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of adenylate cyclase activityD(3) dopamine receptorHomo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
negative regulation of voltage-gated calcium channel activityD(3) dopamine receptorHomo sapiens (human)
regulation of potassium ion transportD(3) dopamine receptorHomo sapiens (human)
phospholipase C-activating dopamine receptor signaling pathwayD(3) dopamine receptorHomo sapiens (human)
positive regulation of MAPK cascadeD(3) dopamine receptorHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationD(3) dopamine receptorHomo sapiens (human)
negative regulation of synaptic transmission, glutamatergicD(3) dopamine receptorHomo sapiens (human)
neural crest cell migration5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cytokine production5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of endothelial cell proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor internalization5-hydroxytryptamine receptor 2BHomo sapiens (human)
heart morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
cardiac muscle hypertrophy5-hydroxytryptamine receptor 2BHomo sapiens (human)
intracellular calcium ion homeostasis5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
activation of phospholipase C activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
phospholipase C-activating serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 2BHomo sapiens (human)
response to xenobiotic stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of phosphatidylinositol biosynthetic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
neural crest cell differentiation5-hydroxytryptamine receptor 2BHomo sapiens (human)
intestine smooth muscle contraction5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphorylation5-hydroxytryptamine receptor 2BHomo sapiens (human)
calcium-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cGMP-mediated signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
vasoconstriction5-hydroxytryptamine receptor 2BHomo sapiens (human)
negative regulation of apoptotic process5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of MAP kinase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transduction5-hydroxytryptamine receptor 2BHomo sapiens (human)
embryonic morphogenesis5-hydroxytryptamine receptor 2BHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of nitric-oxide synthase activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
release of sequestered calcium ion into cytosol5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of cell division5-hydroxytryptamine receptor 2BHomo sapiens (human)
ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascade5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein kinase C signaling5-hydroxytryptamine receptor 2BHomo sapiens (human)
cellular response to temperature stimulus5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 2BHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 2BHomo sapiens (human)
cerebral cortex cell migration5-hydroxytryptamine receptor 6Homo sapiens (human)
positive regulation of TOR signaling5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 6Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 6Homo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
lipid transportSigma non-opioid intracellular receptor 1Homo sapiens (human)
nervous system developmentSigma non-opioid intracellular receptor 1Homo sapiens (human)
G protein-coupled opioid receptor signaling pathwaySigma non-opioid intracellular receptor 1Homo sapiens (human)
regulation of neuron apoptotic processSigma non-opioid intracellular receptor 1Homo sapiens (human)
protein homotrimerizationSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (88)

Processvia Protein(s)Taxonomy
acetylcholine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
neurotransmitter transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
dopamine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
norepinephrine:sodium symporter activitySolute carrier family 22 member 1 Homo sapiens (human)
protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
monoamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
secondary active organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
thiamine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
putrescine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
spermidine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
quaternary ammonium group transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
toxin transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
identical protein bindingSolute carrier family 22 member 1 Homo sapiens (human)
xenobiotic transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
(R)-carnitine transmembrane transporter activitySolute carrier family 22 member 1 Homo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein kinase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-1B adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
alpha-2C adrenergic receptor bindingAlpha-2A adrenergic receptorHomo sapiens (human)
thioesterase bindingAlpha-2A adrenergic receptorHomo sapiens (human)
heterotrimeric G-protein bindingAlpha-2A adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2A adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
norepinephrine bindingAlpha-2A adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2A adrenergic receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2B adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2B adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2B adrenergic receptorHomo sapiens (human)
alpha2-adrenergic receptor activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein bindingAlpha-2C adrenergic receptorHomo sapiens (human)
alpha-2A adrenergic receptor bindingAlpha-2C adrenergic receptorHomo sapiens (human)
protein homodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
protein heterodimerization activityAlpha-2C adrenergic receptorHomo sapiens (human)
epinephrine bindingAlpha-2C adrenergic receptorHomo sapiens (human)
guanyl-nucleotide exchange factor activityAlpha-2C adrenergic receptorHomo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via GsD(1A) dopamine receptorHomo sapiens (human)
G-protein alpha-subunit bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine neurotransmitter receptor activityD(1A) dopamine receptorHomo sapiens (human)
protein bindingD(1A) dopamine receptorHomo sapiens (human)
heterotrimeric G-protein bindingD(1A) dopamine receptorHomo sapiens (human)
dopamine bindingD(1A) dopamine receptorHomo sapiens (human)
arrestin family protein bindingD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(1A) dopamine receptorHomo sapiens (human)
actin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
neurotransmitter:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
dopamine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
norepinephrine:sodium symporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
protein bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent noradrenaline transporter Homo sapiens (human)
alpha-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
metal ion bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
beta-tubulin bindingSodium-dependent noradrenaline transporter Homo sapiens (human)
histamine receptor activityHistamine H2 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H2 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H2 receptorHomo sapiens (human)
protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
identical protein bindingAlpha-1D adrenergic receptorHomo sapiens (human)
alpha1-adrenergic receptor activityAlpha-1D adrenergic receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
virus receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein tyrosine kinase activator activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
protein-containing complex binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2AHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
identical protein binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
1-(4-iodo-2,5-dimethoxyphenyl)propan-2-amine binding5-hydroxytryptamine receptor 2CHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2CHomo sapiens (human)
integrin bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoatomic cation channel activitySodium-dependent serotonin transporterHomo sapiens (human)
neurotransmitter transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
serotonin:sodium:chloride symporter activitySodium-dependent serotonin transporterHomo sapiens (human)
protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
monoamine transmembrane transporter activitySodium-dependent serotonin transporterHomo sapiens (human)
antiporter activitySodium-dependent serotonin transporterHomo sapiens (human)
syntaxin-1 bindingSodium-dependent serotonin transporterHomo sapiens (human)
cocaine bindingSodium-dependent serotonin transporterHomo sapiens (human)
sodium ion bindingSodium-dependent serotonin transporterHomo sapiens (human)
identical protein bindingSodium-dependent serotonin transporterHomo sapiens (human)
nitric-oxide synthase bindingSodium-dependent serotonin transporterHomo sapiens (human)
actin filament bindingSodium-dependent serotonin transporterHomo sapiens (human)
serotonin bindingSodium-dependent serotonin transporterHomo sapiens (human)
histamine receptor activityHistamine H1 receptorHomo sapiens (human)
G protein-coupled serotonin receptor activityHistamine H1 receptorHomo sapiens (human)
neurotransmitter receptor activityHistamine H1 receptorHomo sapiens (human)
dopamine neurotransmitter receptor activity, coupled via Gi/GoD(3) dopamine receptorHomo sapiens (human)
protein bindingD(3) dopamine receptorHomo sapiens (human)
G protein-coupled receptor activityD(3) dopamine receptorHomo sapiens (human)
Gq/11-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
G-protein alpha-subunit binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
GTPase activator activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 2BHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 2BHomo sapiens (human)
histamine receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein binding5-hydroxytryptamine receptor 6Homo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 6Homo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
G protein-coupled opioid receptor activitySigma non-opioid intracellular receptor 1Homo sapiens (human)
protein bindingSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (69)

Processvia Protein(s)Taxonomy
plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
basal plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
membraneSolute carrier family 22 member 1 Homo sapiens (human)
basolateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
apical plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
lateral plasma membraneSolute carrier family 22 member 1 Homo sapiens (human)
presynapseSolute carrier family 22 member 1 Homo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
cytoplasmAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
basolateral plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
neuronal cell bodyAlpha-2A adrenergic receptorHomo sapiens (human)
axon terminusAlpha-2A adrenergic receptorHomo sapiens (human)
presynaptic active zone membraneAlpha-2A adrenergic receptorHomo sapiens (human)
dopaminergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
postsynaptic density membraneAlpha-2A adrenergic receptorHomo sapiens (human)
glutamatergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
GABA-ergic synapseAlpha-2A adrenergic receptorHomo sapiens (human)
receptor complexAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2A adrenergic receptorHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
cytosolAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cell surfaceAlpha-2B adrenergic receptorHomo sapiens (human)
intracellular membrane-bounded organelleAlpha-2B adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2B adrenergic receptorHomo sapiens (human)
cytoplasmAlpha-2C adrenergic receptorHomo sapiens (human)
endosomeAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-2C adrenergic receptorHomo sapiens (human)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
nucleusD(1A) dopamine receptorHomo sapiens (human)
endoplasmic reticulum membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
ciliumD(1A) dopamine receptorHomo sapiens (human)
presynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
dendritic spineD(1A) dopamine receptorHomo sapiens (human)
postsynaptic membraneD(1A) dopamine receptorHomo sapiens (human)
ciliary membraneD(1A) dopamine receptorHomo sapiens (human)
non-motile ciliumD(1A) dopamine receptorHomo sapiens (human)
glutamatergic synapseD(1A) dopamine receptorHomo sapiens (human)
GABA-ergic synapseD(1A) dopamine receptorHomo sapiens (human)
G protein-coupled receptor complexD(1A) dopamine receptorHomo sapiens (human)
plasma membraneD(1A) dopamine receptorHomo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
cell surfaceSodium-dependent noradrenaline transporter Homo sapiens (human)
membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
neuronal cell body membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
presynaptic membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneSodium-dependent noradrenaline transporter Homo sapiens (human)
axonSodium-dependent noradrenaline transporter Homo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
synapseHistamine H2 receptorHomo sapiens (human)
plasma membraneHistamine H2 receptorHomo sapiens (human)
dendriteHistamine H2 receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
plasma membraneAlpha-1D adrenergic receptorHomo sapiens (human)
neurofilament5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
caveola5-hydroxytryptamine receptor 2AHomo sapiens (human)
axon5-hydroxytryptamine receptor 2AHomo sapiens (human)
cytoplasmic vesicle5-hydroxytryptamine receptor 2AHomo sapiens (human)
presynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
neuronal cell body5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendritic shaft5-hydroxytryptamine receptor 2AHomo sapiens (human)
postsynaptic membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
cell body fiber5-hydroxytryptamine receptor 2AHomo sapiens (human)
glutamatergic synapse5-hydroxytryptamine receptor 2AHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2CHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2CHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2CHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
focal adhesionSodium-dependent serotonin transporterHomo sapiens (human)
endosome membraneSodium-dependent serotonin transporterHomo sapiens (human)
endomembrane systemSodium-dependent serotonin transporterHomo sapiens (human)
presynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
membrane raftSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
postsynaptic membraneSodium-dependent serotonin transporterHomo sapiens (human)
serotonergic synapseSodium-dependent serotonin transporterHomo sapiens (human)
synapseSodium-dependent serotonin transporterHomo sapiens (human)
plasma membraneSodium-dependent serotonin transporterHomo sapiens (human)
neuron projectionSodium-dependent serotonin transporterHomo sapiens (human)
cytosolHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
synapseHistamine H1 receptorHomo sapiens (human)
dendriteHistamine H1 receptorHomo sapiens (human)
plasma membraneHistamine H1 receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
synapseD(3) dopamine receptorHomo sapiens (human)
plasma membraneD(3) dopamine receptorHomo sapiens (human)
nucleoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
cytoplasm5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
synapse5-hydroxytryptamine receptor 2BHomo sapiens (human)
G protein-coupled serotonin receptor complex5-hydroxytryptamine receptor 2BHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 2BHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
cilium5-hydroxytryptamine receptor 6Homo sapiens (human)
synapse5-hydroxytryptamine receptor 6Homo sapiens (human)
dendrite5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 6Homo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
nuclear envelopeSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear inner membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
nuclear outer membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulum membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
lipid dropletSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytosolSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic densitySigma non-opioid intracellular receptor 1Homo sapiens (human)
membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
growth coneSigma non-opioid intracellular receptor 1Homo sapiens (human)
cytoplasmic vesicleSigma non-opioid intracellular receptor 1Homo sapiens (human)
anchoring junctionSigma non-opioid intracellular receptor 1Homo sapiens (human)
postsynaptic density membraneSigma non-opioid intracellular receptor 1Homo sapiens (human)
endoplasmic reticulumSigma non-opioid intracellular receptor 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (135)

Assay IDTitleYearJournalArticle
AID23975logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID610137Toxicity in human assessed as residual effect at 1 mg to 3 mg2010Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID147591Compound was tested for its inhibitory activity against Noradrenaline receptor1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID610142Antiinsomnic activity in human assessed as duration of sleep maintenance at 1 mg after 8 hrs2010Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
AID311932Inhibition of ASM in human H4 cells assessed as residual activity at 10 uM2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID23964logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID25866Protonation constant of the compound.1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID23960logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID36031Compound was tested for its inhibitory activity against Alpha-1 adrenergic receptor1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID395324Lipophilicity, log D at pH 7.4 by liquid chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1443980Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate transport preincubated for 10 mins prior to ATP addition measured after 15 mins in presence of [3H]-tauroch2010Toxicological sciences : an official journal of the Society of Toxicology, Dec, Volume: 118, Issue:2
Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID112381The effect on 24-hour mortality in mice following oral administration1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Imine analogues of tricyclic antidepressants.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID112388Effect on pupil dilation was measured in mice upon oral administration1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Imine analogues of tricyclic antidepressants.
AID23968logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID205267Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID632679Displacement of [3H]mepyramine from human histamine H1 receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID26296Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID395326Fraction unbound in rat brain2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID1442001Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay2017Journal of medicinal chemistry, 04-13, Volume: 60, Issue:7
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID88625Compound was tested for the displacement of [3H]mepyramine from Histamine H1 receptor by competition binding assay1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Synthesis, evaluation, and comparative molecular field analysis of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for histamine H(1) receptors.
AID227718Binding energy by using the equation deltaG obsd = -RT ln KD1984Journal of medicinal chemistry, Dec, Volume: 27, Issue:12
Functional group contributions to drug-receptor interactions.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID26300log P values determined at pH 7.41999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1327714Displacement of [3H]mepyramine from human wild type N-terminal hemagglutinin-tagged histamine H1 receptor expressed in HEK293T cells after 4 hrs by microbeta liquid scintillation counting analysis2016Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19
Identification of Ligand Binding Hot Spots of the Histamine H
AID610132Elimination half life in human at 50 mg by RIA2010Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
AID23973Partition coefficient (logD, measured by HPLC, log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID588214FDA HLAED, liver enzyme composite activity2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID679769TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: ? uM, Doxepin: 100 uM) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID22538Half life period is estimated1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID132000Evaluated for antagonism of reserpine induced hypothermia; 0.5-2.5 mg/kg1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines.
AID467611Dissociation constant, pKa of the compound2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID15708Plasma clearance for the compound was determined.1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID130125Compound was evaluated for maximal electroshock antagonism (MES) against mice1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID23976logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID23966logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID112642Antidepressant activity by determining the reversal of tetrabenazine-induced ptosis upon oral administration1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Imine analogues of tricyclic antidepressants.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID467612Fraction unbound in human plasma2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID467613Volume of distribution at steady state in human2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Prediction of volume of distribution values in human using immobilized artificial membrane partitioning coefficients, the fraction of compound ionized and plasma protein binding data.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID624607Specific activity of expressed human recombinant UGT1A32000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID23962logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID88008Displacement of [3H](-)-trans-H2-PAT from Guinea pig histamine H2 receptors.1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Synthesis, evaluation, and comparative molecular field analysis of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for histamine H(1) receptors.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID23708Partition coefficient (logP)1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID134955Mouse behavior activity was determined;D= Depressant1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID26310Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID112624Compound was tested for antidepressant activity by determining the decreased exploratory activity in mice upon oral administration1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Imine analogues of tricyclic antidepressants.
AID691260Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting2012Journal of medicinal chemistry, Jun-28, Volume: 55, Issue:12
Chemocentric informatics approach to drug discovery: identification and experimental validation of selective estrogen receptor modulators as ligands of 5-hydroxytryptamine-6 receptors and as potential cognition enhancers.
AID395327Dissociation constant, pKa by capillary electrophoresis2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID34293Compound was tested for its binding affinity towards brain (neocortex) Adenylate cyclase1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID1283269Inhibition of DR24 in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis2016Journal of medicinal chemistry, Feb-11, Volume: 59, Issue:3
The Effect of Small Molecules on Sterol Homeostasis: Measuring 7-Dehydrocholesterol in Dhcr7-Deficient Neuro2a Cells and Human Fibroblasts.
AID26295Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID395325Lipophilicity, log P by microemulsion electrokinetic chromatography2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID112383The effect on ataxia in mice following oral administration1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Imine analogues of tricyclic antidepressants.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID112385The effect on electroshock protection in mice following oral administration1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Imine analogues of tricyclic antidepressants.
AID23970logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID87880Inhibitory activity against brain adenylate cyclase Histamine H2 receptor1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID23972logD (measured by HPLC) (as log k')1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID139245Righting ability was determined in mice before rapid rolling (unaroused)1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines.
AID624608Specific activity of expressed human recombinant UGT1A42000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID127858Evaluated in vivo for reserpine hypothermia after oral administration in mouse. Minimum active dose was reported1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID26294Partition coefficient (logD) (HPLC)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID1245889Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19
Reengineered tricyclic anti-cancer agents.
AID632682Inverse agonist activity at human histamine H1 receptor expressed in HEK293 cells assessed as inhibition of histamine-induced [3Hinositol phosphate accumulation after 1 hr by scintillation counting2011Journal of medicinal chemistry, Dec-08, Volume: 54, Issue:23
Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor.
AID134420Lethal dose in mouse, in groups of ten1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines.
AID610138Antiinsomnic activity in human assessed as duration of sleep maintenance at 1 mg2010Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19
Identification of a novel selective H1-antihistamine with optimized pharmacokinetic properties for clinical evaluation in the treatment of insomnia.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID681116TP_TRANSPORTER: transepithelial transport (basal to apical) in MDR1-expressing MDCKII cells2002The Journal of pharmacology and experimental therapeutics, Dec, Volume: 303, Issue:3
Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs.
AID311935Partition coefficient, log P of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID311934Dissociation constant, pKa of the compound2008Journal of medicinal chemistry, Jan-24, Volume: 51, Issue:2
Identification of new functional inhibitors of acid sphingomyelinase using a structure-property-activity relation model.
AID395328Lipophilicity, log P of the compound2009Journal of medicinal chemistry, Mar-26, Volume: 52, Issue:6
Relationship between brain tissue partitioning and microemulsion retention factors of CNS drugs.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID19006Calculated membrane partition coefficient (Kmemb)2004Journal of medicinal chemistry, Mar-25, Volume: 47, Issue:7
Surface activity profiling of drugs applied to the prediction of blood-brain barrier permeability.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID34292Compound was tested for its binding affinity towards brain (Hippocampus) Adenylate cyclase1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID205268Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM1985Journal of medicinal chemistry, Mar, Volume: 28, Issue:3
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
AID26514Partition coefficient (logD7.4)1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
AID6418Compound was tested for its inhibitory activity against 5-hydroxytryptamine receptor1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID87513Compound tested for its inhibitory activity against Histamine H1 receptor1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID26538log K was measured potentiometrically in Brij35 medium1999Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16
Development of predictive retention-activity relationship models of tricyclic antidepressants by micellar liquid chromatography.
AID112387The effect on excitement was measured in mice following oral administration1981Journal of medicinal chemistry, Mar, Volume: 24, Issue:3
Imine analogues of tricyclic antidepressants.
AID139244Righting ability was determined in mice before rapid rolling (aroused)1984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Synthesis and central nervous system properties of 2-[(alkoxycarbonyl)amino]-4(5)-phenyl-2-imidazolines.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (820)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990390 (47.56)18.7374
1990's148 (18.05)18.2507
2000's138 (16.83)29.6817
2010's112 (13.66)24.3611
2020's32 (3.90)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 99.32

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index99.32 (24.57)
Research Supply Index7.00 (2.92)
Research Growth Index4.38 (4.65)
Search Engine Demand Index189.90 (26.88)
Search Engine Supply Index2.07 (0.95)

This Compound (99.32)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials207 (23.39%)5.53%
Reviews69 (7.80%)6.00%
Case Studies158 (17.85%)4.05%
Observational0 (0.00%)0.25%
Other451 (50.96%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (17)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Characterization of the Toll-like Receptor 7-agonist Imiquimod 3.75% as a New Surrogate Model of Itch [NCT03943407]0 participants (Actual)Interventional2019-11-30Withdrawn(stopped due to The Imiquimod 3.75% was ineffective)
[NCT01268709]Phase 20 participants InterventionalCompleted
Comparison of Gabapentin With Doxepin in the Management of Uremic Pruritus: Pilot Study [NCT03758079]Phase 414 participants (Actual)Interventional2018-06-01Completed
Doxepin Solution for Alleviation of Stubborn Breakthrough Pain Induced by Swallowing in Patient Receiving Radiotherapy for Nasopharyngeal Carcinoma: A Multicenter, Randomized, Controlled, Double-Blind Clinical Trial [NCT06017895]178 participants (Anticipated)Interventional2023-11-01Recruiting
Topical Doxepin for Prevention and Management of Radiation-induced Dermatitis [NCT02447211]Phase 260 participants (Anticipated)Interventional2015-05-31Recruiting
A Phase 2, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group, Multicenter Proof-of-Concept Study to Evaluate the Safety and Efficacy of Ramelteon Taken in Combination With Doxepin for the Treatment of Subjects With Chronic Insomnia [NCT00755495]Phase 2472 participants (Actual)Interventional2006-07-31Completed
A Randomized, Double-blind, Placebo Controlled Study to Assess the Efficacy and Safety of Doxepin and Temazepam in HIV Seropositive Patients With Insomnia. [NCT00465972]Phase 444 participants (Actual)Interventional2007-03-31Completed
Characterization of Bovine Adrenal Medulla (BAM8-22) as a New Surrogate Model of Non-histaminergic Itch [NCT04588532]24 participants (Actual)Interventional2020-10-01Completed
Longitudinal Comparative Effectiveness of Bipolar Disorder Therapies [NCT02893371]1,037,352 participants (Actual)Observational2016-09-30Completed
The Use of Doxepin for Urticaria in the Emergency Department [NCT05115136]Phase 3160 participants (Anticipated)Interventional2022-05-23Recruiting
A Randomized Double-Blind Study of Doxepin Rinse Versus Placebo in the Treatment of Acute Oral Mucositis Pain in Patients Receiving Radiotherapy With or Without Chemotherapy [NCT01156142]Phase 3155 participants (Actual)Interventional2010-12-31Completed
Treatments for Insomnia in Patients With Parkinson's Disease: A Pilot Study [NCT01489982]Early Phase 120 participants (Actual)Interventional2011-01-31Completed
Characterization of New Human Models of Non-histaminergic Itch and Their Interaction With the TRPM8 Receptor [NCT04554888]20 participants (Actual)Interventional2022-03-01Completed
Stigma and Efficacy of Zhizhu Kuanzhong Capsules Versus Doxepin in the Treatment of Refractory Functional Dyspepsia: a Randomized Controlled Trial [NCT05107999]76 participants (Anticipated)Interventional2021-02-01Recruiting
A Pilot, Double-Blind, Randomized, Two-Arm Crossover Study of Doxepin Versus Placebo for Esophagitis-Induced Pain in Patients Receiving Radiotherapy to the Thorax With or Without Chemotherapy [NCT02062632]Phase 25 participants (Actual)Interventional2014-04-14Terminated(stopped due to Poor accrual)
Pharmacovigilance in Gerontopsychiatric Patients [NCT02374567]Phase 3407 participants (Actual)Interventional2015-01-31Terminated
A Phase III Placebo-Controlled, Randomized Three-Arm Study of Doxepin and a Topical Rinse in the Treatment of Acute Oral Mucositis Pain in Patients Receiving Radiotherapy With or Without Chemotherapy [NCT02229539]Phase 3275 participants (Actual)Interventional2014-11-30Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00465972 (2) [back to overview]Change in Piper Fatigue Scale at 3 Months
NCT00465972 (2) [back to overview]Response: Change in Insomnia Severity Rating Scale at 3 Months.
NCT01156142 (6) [back to overview]Patient Preference for Continuing Therapy With Oral Doxepin Hydrochloride
NCT01156142 (6) [back to overview]Total Drowsiness Increase
NCT01156142 (6) [back to overview]Total Pain Reduction (Mouth and Throat)
NCT01156142 (6) [back to overview]Total Stinging or Burning From the Oral Rinse
NCT01156142 (6) [back to overview]Total Taste of the Oral Rinse
NCT01156142 (6) [back to overview]Incidence of Using Alternative Analgesics Between 2 and 4 Hours After the Initial Mouthwash
NCT02062632 (2) [back to overview]Incidence of Any Grade 3 or Higher Adverse Events Using Common Terminology Criteria for Adverse Events (CTCAE)
NCT02062632 (2) [back to overview]Change in Mouth Pain as Measured by Average Area Under the Curve Per Assessment
NCT02229539 (1) [back to overview]Mean Area Under the Curve (AUC) of Total Pain Reduction

Change in Piper Fatigue Scale at 3 Months

A 22 item scale measuring level of fatigue, with possible totals ranging from 22-220. A higher number indicates greater severity of fatigue. (NCT00465972)
Timeframe: Baseline and 3 months

Interventionunits on a scale (Mean)
Placebo12
Temazepam17

[back to top]

Response: Change in Insomnia Severity Rating Scale at 3 Months.

Insomnia Severity Index; It is a measure of Insomnia Severity; A higher number indicates greater severity of insomnia. Range of possible score totals is 0-28. (NCT00465972)
Timeframe: Baseline and 3 months

Interventionunits on a scale (Mean)
Placebo0.72
Temazepam-4.01

[back to top]

Patient Preference for Continuing Therapy With Oral Doxepin Hydrochloride

After each dose was administered, patients were asked if they would like to continue rinses with that particular agent. The percentage of patients who expressed an interest in continuing therapy are reported below. (NCT01156142)
Timeframe: Up to 9 days

Interventionpercentage of patients (Number)
Arm I (Doxepin-Placebo)77.3
Arm II (Placebo-Doxepin)51.5

[back to top]

Total Drowsiness Increase

The total drowsiness increase will be calculated by the area under the curve (AUC) adjusting for baseline, with time scale replaced by a numerical scale of 1,2,3,4,5,6. The numerical scale will be used rather than the raw time scale in order to give proper weights to more immediate patient-reported mouth pain outcomes after treatment. The AUC will be calculated by proration when there are terminal missing data. If the missing data are intermittent, simple imputation will be applied to calculate the AUC. The question ('On a scale from 0 to 10, what number best describes your DROWSINESS now?') used 11-point numerical analog scales (0 (no drowsiness) to 10 (extreme drowsiness, leading to sleep) scores) to measure total drowsiness increase. The AUCs for the two treatment arms were compared by using the Wilcoxon rank sum test with 95% CIs. The statistical analysis will be the same as the primary analysis. (NCT01156142)
Timeframe: Up to 9 days

Interventionunits on a scale (Mean)
Arm I (Doxepin-Placebo)-0.7
Arm II (Placebo-Doxepin)-2.4

[back to top]

Total Pain Reduction (Mouth and Throat)

The total pain reduction will be calculated by the (average of mouth and throat) area under the curve (AUC) adjusting for baseline, with time scale replaced by a numerical scale of 1,2,3,4,5,6. The numerical scale will be used rather than the raw time scale in order to give proper weights to more immediate patient-reported mouth pain outcomes after treatment. The AUC will be calculated by proration when there are terminal missing data. If the missing data are intermittent, simple imputation will be applied to calculate the AUC. The question ('On a scale from 0 to 10, what number best describes your MOUTH PAIN due to your radiation treatment now?') used 11-point numerical analog scales (0 (no pain) to 10 (worst pain imaginable or possible) scores) to measure pain. The AUCs for the two treatment arms were compared by using the Wilcoxon rank sum test with 95% CIs. (NCT01156142)
Timeframe: Baseline and Day 1

Interventionunits on a scale (Mean)
Arm I (Doxepin-Placebo)-9.1
Arm II (Placebo-Doxepin)-4.7

[back to top]

Total Stinging or Burning From the Oral Rinse

The total stinging or burning from the oral rinse will be calculated by the area under the curve (AUC) adjusting for baseline, with time scale replaced by a numerical scale of 1,2,3,4,5,6. The numerical scale will be used rather than the raw time scale in order to give proper weights to more immediate patient-reported mouth pain outcomes after treatment. The AUC will be calculated by proration when there are terminal missing data. If the missing data are intermittent, simple imputation will be applied to calculate the AUC. The question ('On a scale from 0 to 10, what number best describes any STINGING OR BURNING FROM THE ORAL RINSE now?') used 11-point numerical analog scales (0 (no stinging or burning) to 10 (worst stinging or burning possible) scores) to total stinging or burning from the oral rinse. The AUCs for the two treatment arms were compared by using the Wilcoxon rank sum test with 95% CIs.The statistical analysis will be the same as the primary analysis. (NCT01156142)
Timeframe: Up to 9 days

Interventionunits on a scale (Mean)
Arm I (Doxepin-Placebo)9.6
Arm II (Placebo-Doxepin)4.0

[back to top]

Total Taste of the Oral Rinse

The total taste of the oral rinse will be calculated by the area under the curve (AUC) adjusting for baseline, with time scale replaced by a numerical scale of 1,2,3,4,5,6 , and analyzed in the same way as the primary endpoint. The numerical scale will be used rather than the raw time scale in order to give proper weights to more immediate patient-reported mouth pain outcomes after treatment. The AUC will be calculated by proration when there are terminal missing data. If the missing data are intermittent, simple imputation will be applied to calculate the AUC. The question ('On a scale from 0 to 10, what number best describes the TASTE OF THE ORAL RINSE now?') used 11-point numerical analog scales (0 (acceptable taste) to 10(terrible taste), with higher values representing worse outcome) to evaluate the total taste of the oral rinse. The AUCs for the two treatment arms were compared by using the Wilcoxon rank sum test with 95% CIs. (NCT01156142)
Timeframe: Up to 9 days

Interventionunits on a scale (Mean)
Arm I (Doxepin-Placebo)7.7
Arm II (Placebo-Doxepin)5.1

[back to top]

Incidence of Using Alternative Analgesics Between 2 and 4 Hours After the Initial Mouthwash

The incidence of utilizing additional analgesics between 2 and 4 hours after the initial mouthwash will be compared between the arms by the Chi-square test . (NCT01156142)
Timeframe: Up to 9 days

,
Interventionpercentage of patients (Number)
At 2 hours after the initial mouthwashAt 4 hours after the initial mouthwash
Arm I (Doxepin-Placebo)8.816.9
Arm II (Placebo-Doxepin)2.914.5

[back to top]

Incidence of Any Grade 3 or Higher Adverse Events Using Common Terminology Criteria for Adverse Events (CTCAE)

Incidence of any grade 3 or higher adverse events using Common Terminology Criteria for Adverse Events (CTCAE). Number or patients reporting a grade 3 or higher adverse event according to CTCAE (NCT02062632)
Timeframe: Up to 4 hours after treatment

InterventionParticipants (Count of Participants)
Placebo0

[back to top]

Change in Mouth Pain as Measured by Average Area Under the Curve Per Assessment

Average Area Under the Curve per assessment (aAUCpa) of pain for the first cycle of treatment. Scores are reported on a 0-100 scale, where 100=better outcome QOL. The aAUCpa is the average of each AUC between each sequential assessment. Patients will assess their pain at baseline and at 5, 15, 30, 60, 120, and 240 minutes after treatment. The AUC calculation is based on the assessment number (1,2,3,4,5,6) instead of the actual number of minutes (5,15,30,60,120,240). This results in an AUC measure that is the average pain score across all of the measurements and is not a function of the number of minutes from treatment. The area under the curve of these 6 time points will be adjusted by their baseline pain score. The pain scores at each time point are given equal weights in the AUC calculation and the AUC calculation does not use the number of minutes after treatment. Therefore, the AUC measurement scale is the same as the original pain score scale. (NCT02062632)
Timeframe: Baseline and 5, 15, 30, 60, 120, and 240 minutes after treatment on day 1

Interventionunits on a scale (Number)
Patient #1Patient #2Patient #3
Placebo-1.60NA

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Mean Area Under the Curve (AUC) of Total Pain Reduction

Total pain reduction (mouth and throat) was measured by the numerical analogue scale of mouth pain on a scale of 0 to 10, with 0=no pain and 10=worst pain in the questionnaires taken at baseline, and 5, 15, 30, 60, 120, 240 minutes after assigned treatment for doxepin or DLA vs. placebo. The total pain reduction was calculated by the (average of mouth and throat) area under the curve (AUC) adjusting for baseline, with time scale (baseline, 5, 15, 30, 60, 120 and 240 minutes post treatment) replaced by a numerical scale of 0, 1, 2, 3, 4, 5 and 6 respectively. The AUC was prorated when there are terminal missing data. If the missing data were intermittent, simple imputation by trapezoidal rules were applied to calculate the AUC. If a patient cancelled, was missing baseline data, or only provided baseline data, he/she was excluded from the statistical analysis. (NCT02229539)
Timeframe: Baseline, 5, 15, 30, 60, 120, 240 minutes post treatment

Interventionunits on a scale*time scale (Mean)
Doxepin11.9
DLA (Diphenhydramine, Lidocaine and Antacid)11.7
Placebo8.7

[back to top]