Page last updated: 2024-12-05

methoxyhydroxyphenylglycol

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Description

Methoxyhydroxyphenylglycol: Synthesized from endogenous epinephrine and norepinephrine in vivo. It is found in brain, blood, CSF, and urine, where its concentrations are used to measure catecholamine turnover. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID10805
CHEMBL ID1322392
CHEBI ID1576
SCHEMBL ID43536
MeSH IDM0013606

Synonyms (45)

Synonym
methoxyhydroxyphenylglycol
unii-98lk01183z
98lk01183z ,
3-methoxy-4-hydroxyphenylethyleneglycol
C05594
NCGC00162188-01
mhpg
3-methoxy-4-hydroxyphenylglycol
hydroxymethoxyphenylglycol
mopeg
hmpg
NCGC00015498-03
vanylglycol
1-(4-hydroxy-3-methoxyphenyl)ethane-1,2-diol
FT-0669755
FT-0669754
1,2-ethanediol, 1-(4-hydroxy-3-methoxyphenyl)-
534-82-7
NCGC00015498-02
4-hydroxy-3-methoxyphenyl glycol
rac 4-hydroxy-3-methoxyphenylethylene glycol
1-(4-hydroxy-3-methoxyphenyl)-1,2-ethanediol
vanilethanediol
(4-hydroxy-3-methoxyphenyl)ethylene glycol
SCHEMBL43536
CHEMBL1322392
CHEBI:1576 ,
1-(4-hydroxy-3-methoxyphenyl)-1,2-ethanediol #
FBWPWWWZWKPJFL-UHFFFAOYSA-N
3-methoxy-4-hydroxyphenylglycol [mi]
3-methoxy-4-hydroxyphenyl glycol
3-methoxy-4-hydroxyphenylglycol, (+/-)-
4-hydroxy-3-methoxy-beta-phenylglycol
4-hydroxy-3-methoxy-b-phenylglycol
3-methoxy-4-hydroxyphenylethylene glycol
SR-01000075158-1
sr-01000075158
4-hydroxy-3-methoxy-d3-phenylethylene glycol
Q223097
DTXSID20862142
SDCCGSBI-0633731.P001
NCGC00015498-05
CS-0059602
HY-113323
EN300-1830443

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Thus formation of a toxic metabolite by the action of MAO B may be involved in DSP-4 induced neural damage."( Inhibition of MAO B, but not MAO A, blocks DSP-4 toxicity on central NE neurons.
Gibson, CJ, 1987
)
0.27

Pharmacokinetics

ExcerptReferenceRelevance
"A series of studies on the pharmacokinetic and pharmacodynamic properties of some tricyclic antidepressants is reviewed."( Treatment of depression with tricyclic drugs--pharmacokinetic and pharmacodynamic aspects.
Asberg, M, 1976
)
0.26
" Such pharmacokinetic behavior appeared to be related to the contractive effect of morphine on the bile duct, and naloxone facilitated the excretion of morphine via this route."( Naloxone affects both pharmacokinetics and pharmacodynamics of morphine. Application of direct correlation analysis.
Ishikawa, K; Kogure, M; Kubo, T; Shibanoki, S, 1991
)
0.28
" Pretreatment with desipramine did not alter any of the pharmacokinetic parameters of ISO."( Haemodynamics as a determinant of the pharmacokinetics of and the plasma catecholamine responses to isoprenaline.
Graefe, KH; Halbrügge, T; Ludwig, J; Vey, G; Walter, J, 1989
)
0.28
" The assessment of TCA actions that may be additive, synergistic, or antagonistic requires precise knowledge of pharmacodynamic potency and control of pharmacokinetic behavior."( Active metabolites of antidepressants: pharmacodynamics and relevant pharmacokinetics.
Lane, EA; Potter, WZ; Rudorfer, MV, 1984
)
0.27
" Evaluation of free, instead of total levels did not help to clarify the relationship between clinical and pharmacokinetic variables."( Antidepressive effect and pharmacokinetics of amitriptyline with consideration of unbound drug and 10-hydroxynortriptyline plasma levels.
Breyer-Pfaff, U; Brinkschulte, M; Gaertner, HJ; Kreuter, F; Scharek, G; Wiatr, R, 1982
)
0.26
"The pharmacodynamic equipotency of 2 dose regimens (5 mg twice daily versus 10 mg once daily) of befloxatone, a new reversible and selective monoamine oxidase A (MAO-A) inhibitor, after single and multiple doses for 6 days was examined in a randomized, double-blind, three-way crossover, placebo-controlled trial of 12 healthy volunteers."( Pharmacodynamics and pharmacokinetics of two dose regimens of befloxatone, a new reversible and selective monoamine oxidase inhibitor, at steady state in healthy volunteers.
Allain, H; Cimarosti, I; Curet, O; Dubruc, C; Durrieu, G; Gandon, JM; Jezequel, S; le Coz, F; Patat, A; Rosenzweig, P; Zieleniuk, I, 1996
)
0.29
" A moment analysis was also made to obtain pharmacokinetic parameters."( In vivo microdialysis to determine the relative pharmacokinetics of drugs.
Ichikawa, M; Matsuyama, K; Nakashima, M; Nakashima, MN; Sakurai, M; Sasaki, H; Zhao, MF, 1996
)
0.29
"The objectives of this study were to assess potential pharmacokinetic and pharmacodynamic interactions between moclobemide and selegiline."( Pharmacokinetic-pharmacodynamic interactions between two selective monoamine oxidase inhibitors: moclobemide and selegiline.
Dingemanse, J; Kettler, R; Kneer, J; Korn, A; Koulu, M; Wallnöfer, A; Zürcher, G, 1996
)
0.29
" Adverse events and vital signs were recorded and pharmacokinetic parameters of fluoxetine and moclobemide were determined."( Pharmacokinetic and pharmacodynamic interactions between fluoxetine and moclobemide in the investigation of development of the "serotonin syndrome".
Amrein, R; Dingemanse, J; Gieschke, R; Guentert, T; Wallnöfer, A, 1998
)
0.3
" 3,4-Dihydroxyphenylglycol, 5-hydroxyindoleacetic acid, and 3,4-dihydroxyphenylacetic acid plasma levels and serotonin uptake did not reveal a pharmacodynamic interaction."( Pharmacokinetic and pharmacodynamic interactions between fluoxetine and moclobemide in the investigation of development of the "serotonin syndrome".
Amrein, R; Dingemanse, J; Gieschke, R; Guentert, T; Wallnöfer, A, 1998
)
0.3
" Estimated pharmacokinetic parameters were CL (41."( Mechanistic pharmacokinetic and pharmacodynamic modeling of CHF3381 (2-[(2,3-dihydro-1H-inden-2-yl)amino]acetamide monohydrochloride), a novel N-methyl-D-aspartate antagonist and monoamine oxidase-A inhibitor in healthy subjects.
Csajka, C; Dostert, P; Imbimbo, BP; Piccinno, A; Verotta, D, 2005
)
0.33
" The pharmacokinetic and pharmacodynamic profile of these drugs in plasma and cerebrospinal fluid (CSF) was assessed."( A pharmacokinetic/pharmacodynamic investigation: assessment of edivoxetine and atomoxetine on systemic and central 3,4-dihydroxyphenylglycol, a biochemical marker for norepinephrine transporter inhibition.
Kielbasa, W; Pan, A; Pereira, A, 2015
)
0.42
" Pharmacokinetic and pharmacodynamic data were obtained from healthy subjects (n = 160) from 5 clinical trials."( Pharmacodynamics of norepinephrine reuptake inhibition: Modeling the peripheral and central effects of atomoxetine, duloxetine, and edivoxetine on the biomarker 3,4-dihydroxyphenylglycol in humans.
Kielbasa, W; Lobo, E, 2015
)
0.42
" In an ADHD population treated with dasotraline 4 or 8 mg/day, dasotraline was characterized by a mean apparent half-life of 47 h and plasma concentrations reached steady-state by 10 days of dosing."( Pharmacokinetics and Exposure-Response Relationships of Dasotraline in the Treatment of Attention-Deficit/Hyperactivity Disorder in Adults.
Hing, J; Hopkins, SC; Koblan, KS; Loebel, A; Passarell, JA; Skende, E; Sunkaraneni, S, 2016
)
0.43
" The purpose of this study was to characterize the pharmacokinetic and pharmacodynamic profiles of ampreloxetine in this target population."( Pharmacokinetics and pharmacodynamics of ampreloxetine, a novel, selective norepinephrine reuptake inhibitor, in symptomatic neurogenic orthostatic hypotension.
Bourdet, D; Kanodia, J; Lo, A; Norcliffe-Kaufmann, L; Vickery, R, 2021
)
0.62

Compound-Compound Interactions

ExcerptReferenceRelevance
"The time course of the effects of ethanol alone and in combination with the selective alpha 2-adrenoceptor agonist dexmedetomidine and the alpha-adrenoceptor antagonist atipamezole was studied in NIH-Swiss mice."( The effects of ethanol in combination with the alpha 2-adrenoceptor agonist dexmedetomidine and the alpha 2-adrenoceptor antagonist atipamezole on brain monoamine metabolites and motor performance of mice.
Björn, M; Idänpään-Heikkilä, JJ; Seppälä, T, 1995
)
0.29

Bioavailability

ExcerptReferenceRelevance
" Relative bioavailability of conjugated tyramine was elevated sixfold by brofaromine and 11."( Monoamine oxidase inhibition by phenelzine and brofaromine in healthy volunteers.
Antonin, KH; Bieck, PR; Firkusny, L; Nilsson, E; Schick, C; Schulz, R; Schwenk, M; Wollmann, H, 1989
)
0.28
" This was in line with the limited (less than 30%) oral bioavailability of the active, unconjugated form of the drug, estimated in the same subjects."( Noradrenergic and dopaminergic effects of nomifensine in healthy volunteers.
Hietala, J; Lindberg, R; Pihlajamäki, K; Scheinin, H; Scheinin, M; Syvälahti, E, 1987
)
0.27
" The pharmacokinetic bioavailability at steady state of both dose regimens was also similar."( Pharmacodynamics and pharmacokinetics of two dose regimens of befloxatone, a new reversible and selective monoamine oxidase inhibitor, at steady state in healthy volunteers.
Allain, H; Cimarosti, I; Curet, O; Dubruc, C; Durrieu, G; Gandon, JM; Jezequel, S; le Coz, F; Patat, A; Rosenzweig, P; Zieleniuk, I, 1996
)
0.29

Dosage Studied

ExcerptRelevanceReference
" Urinary MHPG dosage seems to be one of the most interesting in this field."( [Respective position of antidepressants in therapeutics (author's transl)].
Moussaoui, D, 1979
)
0.26
" Desipramine treatment instituted at a daily dosage of 75 mg for depressive equivalents of head, chest, and abdominal pain was increased to 1,000 mg daily over a 12-year interval with minimal side effects."( Withdrawal from long-term high-dose desipramine therapy. Clinical and biological changes.
Brown, GM; Gupta, RN; Harman, J; Moldofsky, H; Murphy, JT; Stancer, HC, 1978
)
0.26
" This study was initiated following significant symptomatic worsening by the patient with supplemental ascorbic acid at a dosage of 2 g/day."( Effect of supplemental ascorbic acid in a case of torsion dystonia.
Mars, H, 1976
)
0.26
" Because no obvious differences between dose-response relations of plasma NOR (believed to be a presynaptic and peripheral effect), blood pressure (believed to be mainly a central presynaptic and postsynaptic effect), and subjective sedation (believed to be a central and probably postsynaptic effect) were observed, our results do not provide simple parameters to discern the multiple mechanisms of action of CLO."( Cardiovascular, neuroendocrine, and sedative responses to four graded doses of clonidine in a placebo-controlled study.
Boomsma, F; Kruijk, MP; Man in 't Veld, AJ; Moleman, P; Tulen, JH; van de Wetering, BJ; van Steenis, HG; von Saher, RA, 1992
)
0.28
" In 46 children from this sample it was dosed plasmatic cortisol and the urinary excretion of catecholamine, VMA, HVA and 5-HIAA."( Biochemical correlate of depression in children.
Basques, JC; Fabre, ZL; Fernandes, ML; Furtado, CR; Lippi, JR; Lombardi, AB; Peixoto, CC; Queiroz, EA; Soares, TA, 1991
)
0.28
"Amiflamine, a drug reported to be a reversible inhibitor of monoamine oxidase type A (MAO-A) selective for serotonergic neurons in rodents, was administered to rhesus monkeys over a 12-fold dosage range (0."( The effects of amiflamine on cerebrospinal fluid amine metabolites in the rhesus monkey.
Garrick, NA; Linnoila, M; Murphy, DL; Seppala, T, 1985
)
0.27
" L-DOPA administration, consisting of a daily dosage of 600 mg plus 150 mg aromatic L-amino acid decarboxylase inhibitor was continued in all cases for at least 3 months."( Unresponsiveness to L-DOPA in parkinsonian patients: a study of homovanillic acid concentration in the cerebrospinal fluid.
Araki, H; Kondo, T; Muramoto, S; Narabayashi, H; Nishi, K; Takubo, H, 1989
)
0.28
"50 pmol/ml) did not change after 1 wk of Li dosing (1."( Differences in lithium effects in depressed and healthy subjects.
Karoum, F; Linnoila, M; Potter, WZ; Ross, RJ; Rudorfer, MV, 1985
)
0.27
" The dosage of both zimeldine and alaproclate was 200 mg daily."( Alaproclate a novel antidepressant? A biochemical and clinical comparison with zimeldine.
Aberg-Wistedt, A; Alvariza, M; Bertilsson, L; Malmgren, R; Wachtmeister, H, 1985
)
0.27
" In trachea and right atria of the guinea-pig, tertatolol inhibited, in a concentration-dependent manner, the dose-response curves to isoproterenol; the relative potency of tertatolol was higher than that of propranolol."( Effects of tertatolol on post- and prejunctional beta adrenoceptors.
Herman, AG; Jordaens, FH; Laekeman, G; Majchrowicz, BB; Verbeuren, TJ; Zonnekeyn, LL, 1985
)
0.27
" The dose-response relations for exogenous noradrenaline measured in the absence or presence of 50 microM amiloride indicated that the drug acted as a reversible competitive alpha-adrenergic antagonist."( Amiloride acts as an alpha-adrenergic antagonist in the isolated rat tail artery.
Palatý, V, 1986
)
0.27
"Blood pressure and heart rate responses to oral tyramine have been measured in healthy volunteers before and after administration of the selective monoamine oxidase B inhibitor selegiline at high dosage (30 mg/day)."( Enhanced pressor sensitivity to oral tyramine challenge following high dose selegiline treatment.
Glover, V; Goodwin, BL; Prasad, A; Sandler, M; Signy, M; Smith, SE, 1988
)
0.27
"The dosage of plasma 3-methoxy-4-hydroxyphényl glycol (MHPG) presents a great interest, specially in psychiatry."( [Principle methods of determining plasma 3-methoxy-4-hydroxyphenyl glycol].
Candito, M; Chambon, P,
)
0.13
" The dose-response curve of detomidine was shifted to the right in a parallel manner by the selective alpha 2-antagonist idazoxan."( Effect of detomidine on the release and turnover of noradrenaline in rat brain.
Kaisila, M; MacDonald, E; Virtanen, R, 1986
)
0.27
"In the present study, clinical interview, Visual Evoked Potentials, psychological tests, TRH test, plasmatic MHPG dosage were investigated in 30 depressed patients with major depressive disorders."( [Multidisciplinary approach to depression. Preliminary results].
Arnaud-Castiglioni, R; Bougerol, T; Carayon, P; Chakroun, H; Cornu, L; Louvel, E; Scotto, JC; Valli, M; Warnery, F,
)
0.13
" Dose-response regression lines showed that exercise in the heat increased the slope and shifted the Tco-NE dose relation to the left."( Heat acclimation: role of norepinephrine in the anterior hypothalamus.
Christman, JV; Gisolfi, CV, 1985
)
0.27
" The daily dosage ceiling was increased to 10 mg."( Some biochemical correlates of panic attacks with agoraphobia and their response to a new treatment.
Coleman, JH; Greenblatt, DJ; Jones, KJ; Levine, PH; Orsulak, PJ; Peterson, M; Schildkraut, JJ; Sheehan, DV; Uzogara, E; Watkins, D, 1984
)
0.27
" The dosage of urinary MHPG seems to be a valuable index for the choice of the drug."( [Therapeutic implications of the biochemical features about depressive illness (author's transl)].
Lôo, H, 1981
)
0.26
"In a single-blind study, 12 men (mean age 63 years) with senile dementia were given nafronyl in a dosage of 100 mg eight times daily for a week, followed by 100 mg four times daily for 12 weeks."( Effect of nafronyl on lactate and pyruvate in the cerebrospinal fluid of patients with senile dementia.
Berger, PA; Hollister, LE; Tinklenberg, JR; Yesavage, JA, 1982
)
0.26
" Male Sprague-Dawley rats dosed once with chlordecone at 100 mg/kg were sacrificed after 24 hr, then brain norepinephrine (NE) and dopamine (DA) levels were assayed."( Lack of effects of chlordecone on synthesis rates, steady state levels and metabolites of catecholamines in rat brain.
Aldous, CN; Chetty, CS; Desaiah, D; Mehendale, HM, 1984
)
0.27
" Apomorphine does not produce the shaped dose-response activity curve found with systemic injections."( Intracerebroventricular apomorphine alleviates spontaneous forgetting and increases cortical noradrenaline.
Grecksch, G; Leviel, V; Sara, SJ, 1984
)
0.27
"The neurochemical background of clinical experiences that the patients receiving high dosage haloperidol showed no extrapyramidal side effects was investigated by using rats."( [High dosage haloperidol reduces cataleptic response with increased noradrenaline metabolism in the rat brain areas].
Takashima, M; Toru, M, 1983
)
0.27
" The dose-response curve for verapamil was bell-shaped and the activity resided in the l form."( An inhibitory effect of verapamil and diltiazem on the release of noradrenaline from ischaemic and reperfused hearts.
Nayler, WG; Sturrock, WJ, 1984
)
0.27
" We hypothesized that selegiline, at a dosage of 60 mg/d, would be at least partially effective but that the higher doses would not maintain the monoamine oxidase B selectivity observed with the lower doses of selegiline."( High-dose selegiline in treatment-resistant older depressive patients.
Cohen, RM; Lawlor, BA; Mellow, AM; Molchan, S; Mueller, EA; Murphy, DL; Newhouse, PA; Sunderland, T; Tariot, PN, 1994
)
0.29
"3 years) entered a double-blind, randomized, crossover study of placebo vs 3 weeks of selegiline at a dosage of 60 mg/d."( High-dose selegiline in treatment-resistant older depressive patients.
Cohen, RM; Lawlor, BA; Mellow, AM; Molchan, S; Mueller, EA; Murphy, DL; Newhouse, PA; Sunderland, T; Tariot, PN, 1994
)
0.29
" However, the dose-response in the di/di Brattleboro rat was biphasic with a decrease at a low dose of vasopressin."( Early postnatal appearance of enhanced noradrenaline content in the brain of vasopressin-deficient Brattleboro rat; normal adrenoceptor densities and aberrant influences of vasopressin treatment.
Boer, GJ; Botterblom, MJ; Feenstra, MG; Korse, V; Te Riele, P, 1995
)
0.29
" Oral dosing with amiodarone has no such effect."( Sympatholytic action of intravenous amiodarone in the rat heart.
Dart, AM; Du, XJ; Esler, MD, 1995
)
0.29
" Blood pressure, heart rate, ECG, and plasma concentrations of unconjugated adrenaline and noradrenaline were not influenced after single and repeated dosing of entacapone."( COMT inhibition by high-dose entacapone does not affect hemodynamics but changes catecholamine metabolism in healthy volunteers at rest and during exercise.
Gordin, A; Heinävaara, S; Illi, A; Koulu, M; Scheinin, M; Sundberg, S, 1994
)
0.29
" Both dose regimens provided equipotent extent and duration of MAO-A inhibition at steady state, suggesting a once daily dosage should be sufficient for most patients."( Pharmacodynamics and pharmacokinetics of two dose regimens of befloxatone, a new reversible and selective monoamine oxidase inhibitor, at steady state in healthy volunteers.
Allain, H; Cimarosti, I; Curet, O; Dubruc, C; Durrieu, G; Gandon, JM; Jezequel, S; le Coz, F; Patat, A; Rosenzweig, P; Zieleniuk, I, 1996
)
0.29
" The pharmacokinetic parameters of moclobemide and its metabolites changed on multiple dosing but were not influenced to a relevant extent by concomitant administration of selegiline."( Pharmacokinetic-pharmacodynamic interactions between two selective monoamine oxidase inhibitors: moclobemide and selegiline.
Dingemanse, J; Kettler, R; Kneer, J; Korn, A; Koulu, M; Wallnöfer, A; Zürcher, G, 1996
)
0.29
"A 79-year-old male suffering from Shy-Drager syndrome was treated with a daily dosage of 300 mg of L-threo-3,4-dihydroxyphenylserine (L-DOPS)."( [Monoamine imbalance of the central nervous system in a case of Shy-Drager syndrome with recurrent attacks of a neuroleptic malignant syndrome].
Hamamoto, M; Miyazaki, T; Otsubo, K; Terashi, A; Ueda, M, 1996
)
0.29
" Maintenance dosage was linearly related to plasma levels of clozapine and its metabolites."( Correlated changes in symptoms and neurotransmitter indices during maintenance treatment with clozapine or conventional neuroleptics in adolescents and young adults with schizophrenia.
Fleischhaker, C; Remschmidt, HE; Schulz, E, 1996
)
0.29
" However, multiple dosing of moclobemide did not lead the excessive accumulation."( Pharmacokinetic and pharmacodynamic interactions between fluoxetine and moclobemide in the investigation of development of the "serotonin syndrome".
Amrein, R; Dingemanse, J; Gieschke, R; Guentert, T; Wallnöfer, A, 1998
)
0.3
" TYR PD30 increased significantly with desipramine dosing (p<0."( Duloxetine increases serotonin and norepinephrine availability in healthy subjects: a double-blind, controlled study.
Bieck, PR; Bymaster, FP; Chalon, SA; Granier, LA; Hirth, C; Joliat, MJ; Potter, WZ; Vandenhende, FR, 2003
)
0.32
" These mGluRs are functionally active on catecholamine (CA) secretion in chromaffin cells because both (1S, 3R)-1-aminocyclopentane-1,3-dicarboxylic acid (t-ACPD) and the specific agonist of Group I mGluRs, (S)-3,5-dihydroxyphenylglycine (DHPG), were able to stimulate the release of CAs (adrenaline and noradrenaline) in a dose-response manner."( Expression and functional properties of group I metabotropic glutamate receptors in bovine chromaffin cells.
Aránguez, I; Arce, C; Del Campo, AB; Figueroa, S; González, MP; López, E; Oset-Gasque, MJ, 2004
)
0.32
" The dose of intravenous tyramine required to raise systolic blood pressure by 30 mm Hg (PD30) increased dose-dependently with duloxetine and was significant at the end of the 120-mg/d dosage (P<0."( Clinical assessment of norepinephrine transporter blockade through biochemical and pharmacological profiles.
Bieck, PR; Black, BK; Bymaster, FP; Garland, EM; Gonzales, C; Loghin, C; Potter, WZ; Robertson, D; Vincent, S, 2004
)
0.32
" Here, the in vivo effects of dosing with duloxetine 60 mg once daily for 11 days in healthy subjects were assessed in 2 studies: (1) centrally (n = 11), by measuring concentrations of 5-hydroxyindoleacetic acid, 3,4-dihydroxyphenylglycol (DHPG), and NE in cerebrospinal fluid, and (2) versus escitalopram 20 mg/d (n = 32) in a 2-period crossover study by assessing the ΔDHPG/ΔNE ratio in plasma during orthostatic testing and by pharmacokinetic/pharmacodynamic modeling of reuptake inhibition using subjects' serum in cell lines expressing cloned human 5-HTT or NET."( Effects of duloxetine on norepinephrine and serotonin transporter activity in healthy subjects.
Chappell, JC; Dean, RA; Detke, MJ; Eisenhofer, G; Haber, H; Iyengar, S; Knadler, MP; Lachno, DR; Lobo, ED; Mitchell, MI; Nemeroff, CB; Owens, MJ; Pangallo, B, 2014
)
0.4
"These results related dasotraline pharmacokinetics to pharmacological activity in ADHD, and support the novel concept that maintaining constant, steady-state dopamine and norepinephrine reuptake inhibition throughout a 24-h dosing interval is a novel pharmacological approach to the management of ADHD symptoms."( Pharmacokinetics and Exposure-Response Relationships of Dasotraline in the Treatment of Attention-Deficit/Hyperactivity Disorder in Adults.
Hing, J; Hopkins, SC; Koblan, KS; Loebel, A; Passarell, JA; Skende, E; Sunkaraneni, S, 2016
)
0.43
" six years) showed dose-response declines in learning across groups with elevated NE-metabolite 3-methoxy-4-hydroxyphenylethyleneglycol (MHPG) with no, one, or two Alzheimer's disease biomarkers; and no decline in the low MHPG group."( Elevated Norepinephrine Metabolism Gauges Alzheimer's Disease-Related Pathology and Memory Decline.
Jacobs, HIL; Riphagen, JM; van Egroo, M, 2021
)
0.62
" The findings are consistent with long-lasting NET inhibition, which may increase vasoconstrictor tone, supporting once-daily ampreloxetine dosing in patients with nOH."( Pharmacokinetics and pharmacodynamics of ampreloxetine, a novel, selective norepinephrine reuptake inhibitor, in symptomatic neurogenic orthostatic hypotension.
Bourdet, D; Kanodia, J; Lo, A; Norcliffe-Kaufmann, L; Vickery, R, 2021
)
0.62
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
phenolsOrganic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring.
methoxybenzenesAny aromatic ether that consists of a benzene skeleton substituted with one or more methoxy 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 (9)

PathwayProteinsCompounds
Tyrosine Metabolism1657
Alkaptonuria1657
Hawkinsinuria1657
Tyrosinemia Type I1657
Disulfiram Action Pathway2366
Tyrosinemia, Transient, of the Newborn1657
Dopamine beta-Hydroxylase Deficiency1657
Monoamine Oxidase-A Deficiency (MAO-A)1657
Biosynthesis and regeneration of tetrahydrobiopterin and catabolism of phenylalanine1519

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
thioredoxin reductaseRattus norvegicus (Norway rat)Potency9.46620.100020.879379.4328AID488773; AID588453
GLS proteinHomo sapiens (human)Potency4.46680.35487.935539.8107AID624146
arylsulfatase AHomo sapiens (human)Potency0.95281.069113.955137.9330AID720538
D(1A) dopamine receptorHomo sapiens (human)Potency0.73070.02245.944922.3872AID488982
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (24)

Assay IDTitleYearJournalArticle
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID588378qHTS for Inhibitors of ATXN expression: Validation
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.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1432861Anti-inflammatory activity in human U937-derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 secretion at 125 uM preincubated for 2 hrs followed by LPS addition measured after 24 hrs by ELISA relative to control2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and anti-inflammatory activity of isoquebecol.
AID1432863Anti-inflammatory activity in human U937-derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 secretion at 31.25 uM preincubated for 2 hrs followed by LPS addition measured after 24 hrs by ELISA relative to control2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and anti-inflammatory activity of isoquebecol.
AID1432864Anti-inflammatory activity in human U937-derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 secretion at 500 uM preincubated for 2 hrs followed by LPS addition measured after 24 hrs by ELISA relative to control2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and anti-inflammatory activity of isoquebecol.
AID1432860Anti-inflammatory activity in human U937-derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 secretion at 250 uM preincubated for 2 hrs followed by LPS addition measured after 24 hrs by ELISA relative to control2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and anti-inflammatory activity of isoquebecol.
AID1432859Cytotoxicity against human U937-derived macrophage-like cells assessed as reduction in cell viability after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and anti-inflammatory activity of isoquebecol.
AID1432862Anti-inflammatory activity in human U937-derived macrophage-like cells assessed as inhibition of LPS-induced IL-6 secretion at 62.5 uM preincubated for 2 hrs followed by LPS addition measured after 24 hrs by ELISA relative to control2017Bioorganic & medicinal chemistry, 04-01, Volume: 25, Issue:7
Synthesis and anti-inflammatory activity of isoquebecol.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,161)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901597 (50.52)18.7374
1990's751 (23.76)18.2507
2000's482 (15.25)29.6817
2010's293 (9.27)24.3611
2020's38 (1.20)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 6.05

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index6.05 (24.57)
Research Supply Index8.18 (2.92)
Research Growth Index4.23 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (6.05)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials275 (8.34%)5.53%
Reviews132 (4.00%)6.00%
Case Studies63 (1.91%)4.05%
Observational1 (0.03%)0.25%
Other2,826 (85.71%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]