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ramelteon

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Description

ramelteon: melatonin MT1/MT2 receptor agonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID208902
CHEMBL ID1218
CHEBI ID109549
SCHEMBL ID29237
MeSH IDM0480272

Synonyms (91)

Synonym
AC-5275
HY-A0014
BRD-K28761891-001-01-0
gtpl1356
n-[2-[(8s)-2,6,7,8-tetrahydro-1h-cyclopenta[e][1]benzoxol-8-yl]ethyl]propanamide
tak-375
rozerem
ramelteon
tak-375sl
ramelteon (jan/usan/inn)
196597-26-9
D02689
rozerem (tn)
BSPBIO_002318
DB00980
SPECTRUM1505817
propanamide, n-(2-((8s)-1,6,7,8-tetrahydro-2h-indeno(5,4-b)furan-8-yl)ethyl)-
(-)-n-(2-(((8s)-1,6,7,8-tetrahydro-2h-indeno(5,4-b)furan-8-yl)ethyl)propanamide
ramelteon [usan]
(s)-n-(2-(1,6,7,8-tetrahydro-2h-indeno-(5,4)furan-8-yl)ethyl)propionamide
n-[2-[(8s)-2,6,7,8-tetrahydro-1h-cyclopenta[e]benzofuran-8-yl]ethyl]propanamide
CHEBI:109549
HMS2093F12
tak375
CHEMBL1218 ,
n-[2-(1,6,7,8-tetrahydro-2h-3-oxa-as-indacen-8-yl)-ethyl]-propionamide(s)-(-)-22b
bdbm50118470
HMS1922H18
n-[2-[(8s)-2,6,7,8-tetrahydro-1h-cyclopenta[e][1]benzofuran-8-yl]ethyl]propanamide
hsdb 7787
901as54i69 ,
unii-901as54i69
ramelteon [usan:inn:ban:jan]
dtxcid4025951
dtxsid6045951 ,
(s)-n-[2-(1,6,7,8-tetrahydro-2h-indeno-[5,4-b]furan-8-yl)ethyl]propionamide
smr002544684
MLS003915619
NCGC00178707-03
ramelteon [hsdb]
ramelteon [who-dd]
ramelteon [jan]
(-)-n-(2-(((8s)-1,6,7,8-tetrahydro-2h-indeno(5,4-.beta.)furan-8-yl)ethyl)propanamide
ramelteon [orange book]
ramelteon [mart.]
propanamide, n-(2-((8s)-1,6,7,8-tetrahydro-2h-indeno(5,4-.beta.)furan-8-yl)ethyl)-
ramelteon [inn]
ramelteon [vandf]
AM84670
CS-0382
S1259
AKOS015895741
CCG-213557
YLXDSYKOBKBWJQ-LBPRGKRZSA-N
(s)-n-(2-[1,6,7,8-tetrahydro-2h-indeno[5,4-b]furan-8-yl]ethyl)propionamide
MLS006010029
SCHEMBL29237
AB01274760-01
J-502508
(s)-n-[2-(1,6,7,8-tetrahydro-2h-indeno[5,4-b]furan-8-yl)ethyl]propionamide
1-boc-2-[(4-fluoro-phenylamino)-methyl]-piperidine
(s)-n-(2-(1,6,7,8-tetrahydro-2h-indeno[5,4-b]furan-8-yl)ethyl)propionamide
AB01274760_02
AB01274760_03
n-{2-[(8s)-1h,2h,6h,7h,8h-indeno[5,4-b]furan-8-yl]ethyl}propanamide
n-[2-[(8s)-1,6,7,8-tetrahydro-2h-indeno[5,4-b]furan-8-yl]ethyl]propanamide
SR-05000001957-3
sr-05000001957
Z2037281108
mfcd08067736
SR-05000001957-1
ramelteon 1.0 mg/ml in acetonitrile
SBI-0206874.P001
ramelteon (tak-375)
SW219712-1
Q417689
JEV ,
n-{2-[(8s)-1,6,7,8-tetrahydro-2h-indeno[5,4-b]furan-8-yl]ethyl}propanamide
AS-15740
BRD-K28761891-001-04-4
tak 375
HMS3884K07
NCGC00178707-05
EN300-219936
R0216
ramelteon (mart.)
(-)-n-(2-(((8s)-1,6,7,8-tetrahydro-2h-indeno(5,4-beta)furan-8-yl)ethyl)propanamide
n05ch02
propanamide, n-(2-((8s)-1,6,7,8-tetrahydro-2h-indeno(5,4-beta)furan-8-yl)ethyl)-
n-(2-((8s)-1,6,7,8-tetrahydro-2h-indeno(5,4-b)furan-8-yl)ethyl)propanamide
ramelteonum

Research Excerpts

Overview

Ramelteon (TAK-375) is a novel melatonin receptor agonist currently under investigation for the treatment of insomnia. Ramelteon is an oral hypnotic drug and in the present study, we investigated its protective effect on BBB damage.

ExcerptReferenceRelevance
"Ramelteon (TAK-375) is a novel melatonin receptor agonist currently under investigation for the treatment of insomnia. "( Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist.
Fukatsu, K; Hinuma, S; Hirai, K; Kato, K; Kawamata, Y; Miyamoto, M; Nishiyama, K; Ohkawa, S; Uchikawa, O, 2005
)
2.07
"Ramelteon is a novel agonist of melatonin receptor developed for the treatment of insomnia."( Ramelteon Mitigates Free Fatty Acid (FFA)-Induced Attachment of Monocytes to Brain Vascular Endothelial Cells.
Li, Y; Liu, C; Liu, Y; Tian, F; Wang, G, 2021
)
2.79
"Ramelteon is a melatonin receptor agonist with anti-inflammatory and antioxidant effects."( Ramelteon protects against human pulmonary microvascular endothelial cell injury induced by lipopolysaccharide (LPS) via activating nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) pathway.
Gao, J; Huang, T; Lu, D; Wang, W; Yan, K; Yang, W; Zhang, Y, 2022
)
2.89
"Ramelteon is a melatonin receptor agonist with high affinity for MT1 and MT2 receptors."( A multi-centre, double-blind, randomized, placebo-controlled trial to evaluate the effectiveness and safety of ramelteon for the prevention of postoperative delirium in elderly cancer patients: a study protocol for JORTC-PON2/J-SUPPORT2103/NCCH2103.
Akechi, T; Ariyoshi, K; Furukawa, T; Hashimoto, H; Hatta, K; Hirayama, T; Iwata, Y; Kayano, A; Maeda, M; Masanori, E; Matsuda, Y; Matsuoka, H; Nakahara, R; Ogawa, A; Ogawa, Y; Okita, N; Oyamada, S; Sadahiro, R; Saito, E; Sasaki, C; Sato, T; Sekimoto, A; Shimada, K; Tokoro, A; Uchitomi, Y; Uezono, Y; Yamaguchi, T; Yamamoto, N; Yanai, Y; Yorikane, E, 2023
)
1.84
"Ramelteon is a potent and highly selective melatonin receptor agonist that has been used for the treatment of insomnia and has been reported to have an anti-inflammatory effect."( The Protective Effects of Ramelteon Against Isoflurane-Induced Insults and Inflammatory Response in Brain Microvascular Endothelial Cells.
Chen, X; Li, Z; Sun, H; Wang, T; Xia, S; Xu, Z, 2021
)
1.64
"Ramelteon is an oral hypnotic drug, and in the present study, we investigated its protective effect on BBB damage, as well as the underlying mechanism."( Ramelteon Ameliorates LPS-Induced Hyperpermeability of the Blood-Brain Barrier (BBB) by Activating Nrf2.
Du, N; Liu, Y; Shao, H; Wang, L; Yang, L; Yin, X, 2021
)
2.79
"Ramelteon is an oral hypnotic agent that specifically targets the receptors of the suprachiasmatic nucleus in the human hypothalamus."( The protective effects of Ramelteon against 6-OHDA-induced cellular senescence in human SH-SY5Y neuronal cells.
Cai, M; Gu, X; Han, F; Han, L; Liu, D; Liu, W; Ma, Q, 2021
)
1.64
"Ramelteon is a nonscheduled insomnia medication that lacks the abuse potential and residual effects common for other sedative-hypnotics. "( Autoimmune hepatitis in association with ramelteon.
Fourman, LT; Robert Meyer, B, 2013
)
2.1
"Ramelteon is a novel hypnotic characterized by its action as a melatonin receptor (MT1/MT2) agonist. "( [Effects of ramelteon on a patient with circadian rhythm sleep disorder and mood disorder].
Chiba, S; Fujimura, Y; Matsuda, M; Saito, I; Sakamoto, K; Shirata, A; Tamashiro, M; Tamura, Y; Yoshihara, S; Yoshizawa, M, 2014
)
2.22
"Ramelteon is a novel hypnotic compound that is FDA-approved for the treatment of sleep-onset difficulty. "( Efficacy and clinical safety of ramelteon: an evidence-based review.
Kirby-Long, P; Sateia, MJ; Taylor, JL, 2008
)
2.07
"Ramelteon is a selective MT1/MT2 melatonin receptor agonist approved by the US Food and Drug Administration for insomnia treatment."( Ramelteon 8 mg/d versus placebo in patients with chronic insomnia: post hoc analysis of a 5-week trial using 50% or greater reduction in latency to persistent sleep as a measure of treatment effect.
Mini, L; Wang-Weigand, S; Zhang, J, 2008
)
3.23
"Ramelteon is a novel MT(1) and MT(2) melatonergic agonist that has specific effects on melatonin receptors in the SCN and is effective in promoting sleep in experimental animals such as cats and monkeys."( Melatonin and melatonergic drugs on sleep: possible mechanisms of action.
Cardinali, DP; Hardeland, R; Pandi-Perumal, SR; Poeggeler, B; Spence, DW; Srinivasan, V; Trahkt, I, 2009
)
1.07
"Ramelteon is an MT(1)/MT(2) melatonin receptor agonist indicated for the treatment of insomnia characterized by difficulty with sleep onset. "( Effects of ramelteon 8 mg on objective sleep latency in adults with chronic insomnia on nights 1 and 2: pooled analysis.
McCue, M; Mini, L; Ogrinc, F; Wang-Weigand, S, 2009
)
2.19
"Ramelteon is a tricyclic synthetic analog of melatonin that acts specifically on MT(1) and MT(2) melatonin receptors. "( Ramelteon: a review of its therapeutic potential in sleep disorders.
Brown, GM; Cardinali, DP; Hardeland, R; Moscovitch, A; Pandi-Perumal, SR; Spence, DW; Srinivasan, V, 2009
)
3.24
"Ramelteon (Rozerem) is an orally active, highly selective melatonin MT1/MT2 receptor agonist."( [A novel therapeutic drug: ramelteon].
Miyamoto, M, 2009
)
1.37
"Ramelteon is a melatonin receptor agonist used as a treatment for insomnia. "( Metabolism of ramelteon in human liver microsomes and correlation with the effect of fluvoxamine on ramelteon pharmacokinetics.
Obach, RS; Ryder, TF, 2010
)
2.16
"Ramelteon is a melatonin MT-1/MT-2 agonist approved for the treatment of insomnia."( Effects of the melatonin MT-1/MT-2 agonist ramelteon on daytime body temperature and sleep.
Burke, TM; Lee-Chiong, TL; Markwald, RR; Snider, JA; Wright, KP, 2010
)
1.34
"Ramelteon (TAK-375) is a novel melatonin receptor agonist that is used for clinical treatment of insomnia. "( Efficient synthesis of [¹¹C]ramelteon as a positron emission tomography probe for imaging melatonin receptors involved in circadian rhythms.
Doi, H; Suzuki, M; Takahashi, K; Takashima-Hirano, M; Tazawa, S, 2011
)
2.11
"Ramelteon is an MT(1)/MT(2) melatonin receptor agonist approved in the US and Japan for the treatment of sleep-onset insomnia. "( Use of a post-sleep questionnaire-interactive voice response system (PSQ-IVRS) to evaluate the subjective sleep effects of ramelteon in adults with chronic insomnia.
Roth, T; Wang-Weigand, S; Watissée, M, 2011
)
2.02
"Ramelteon is a new class of sleep agent that selectively binds to the melatonin type 1 (MT1) and type 2 (MT2) receptors in the suprachiasmatic nucleus (SCN), instead of binding to GABA-A receptors such as with traditional hypnotics benzodiazepines. "( [New hypnotics ramelteon for the treatment of insomniacs with circadian rhythm disturbance].
Mishima, K, 2012
)
2.17
"Ramelteon (TAK-375) is an MT1/MT2 receptor agonist being studied for the treatment of insomnia and circadian rhythm sleep disorders. "( The sleep-promoting action of ramelteon (TAK-375) in freely moving cats.
Doken, Y; Hirai, K; Miyamoto, M; Nishikawa, H; Ohkawa, S; Uchikawa, O, 2004
)
2.05
"Ramelteon [TAK 375] is a melatonin (MT1/MT2) receptor agonist that is being developed by Takeda as a treatment for sleep disorders. "( Ramelteon: TAK 375.
, 2005
)
3.21
"Ramelteon is a selective MT(1)/MT(2) receptor agonist, indicated for insomnia treatment. "( Disposition kinetics and tolerance of escalating single doses of ramelteon, a high-affinity MT1 and MT2 melatonin receptor agonist indicated for treatment of insomnia.
Cao, C; Karim, A; Tolbert, D, 2006
)
2.01
"Ramelteon (TAK-375) is a novel sleep-promoting agent that acts as an agonist at these receptors; its preclinical pharmacology, mode of action, pharmacokinetics, drug interactions, clinical efficacy, and safety and tolerability are reviewed here."( Ramelteon: profile of a new sleep-promoting medication.
Owen, RT, 2006
)
2.5
"Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for insomnia treatment. "( Ramelteon: a novel hypnotic lacking abuse liability and sedative adverse effects.
Griffiths, RR; Johnson, MW; Suess, PE, 2006
)
3.22
"Ramelteon is a selective MT(1)/MT(2)-receptor agonist indicated for insomnia treatment. "( Safety of ramelteon in individuals with mild to moderate obstructive sleep apnea.
Kryger, M; Roth, T; Wang-Weigand, S, 2007
)
2.18
"Ramelteon is a selective MT(1)/MT(2) melatonin receptor agonist indicated for the treatment of insomnia characterized by difficulty with sleep onset."( Self-reported efficacy and tolerability of ramelteon 8 mg in older adults experiencing severe sleep-onset difficulty.
Mini, LJ; Wang-Weigand, S; Zhang, J, 2007
)
2.05
"Ramelteon appeared to be an effective and well-tolerated treatment for these older adults with primary, chronic insomnia."( Self-reported efficacy and tolerability of ramelteon 8 mg in older adults experiencing severe sleep-onset difficulty.
Mini, LJ; Wang-Weigand, S; Zhang, J, 2007
)
1.32
"Ramelteon is a novel MT1 and MT2 melatonin receptor selective agonist recently approved for the treatment of insomnia characterized by difficulty in sleep onset. "( Ramelteon: a melatonin receptor agonist for the treatment of insomnia.
Devi, V; Shankar, PK,
)
3.02

Effects

Ramelteon has neuroprotection for chronic ischemia animals, but the effect and the biological mechanism of it on PSD is still unclear. Ramelteon also has a substantially longer half-life than melatonin.

ExcerptReferenceRelevance
"Ramelteon also has a substantially longer half-life than melatonin."( Melatonergic drugs in clinical practice.
Cardinali, DP; Hardeland, R; Pandi-Perumal, SR; Poeggeler, B; Srinivasan, V; Trakht, I, 2008
)
1.07
"Ramelteon has neuroprotection for chronic ischemia animals, but the effect and the biological mechanism of it on PSD is still unclear."( Ramelteon improves blood-brain barrier of focal cerebral ischemia rats to prevent post-stroke depression via upregulating occludin.
He, L; Li, M; Qi, X; Shao, X; Tang, Z; Wang, J; Wang, Z; Yu, X; Zhang, X, 2023
)
3.07
"Ramelteon has few adverse effects and higher affinity for MT1 and MT2 receptors than melatonin."( Ramelteon for the treatment of delirium in elderly patients: a consecutive case series study.
Ishigooka, J; Naganawa, E; Nishimura, K; Otsubo, T; Tsuda, A, 2014
)
2.57
"Ramelteon has demonstrated sleep-promoting effects in clinical trials and clinical practice, and it is not associated with the adverse effects typical of other class of hypnotics."( Pharmacokinetic and pharmacodynamic evaluation of ramelteon : an insomnia therapy.
Bedini, A; Lucarini, S; Mor, M; Rivara, S; Spadoni, G, 2015
)
1.39
"Ramelteon has demonstrated sleep-promoting effects in clinical trials, and coupled with its favorable safety profile and lack of abuse potential or dependence, this chronohypnotic provides an important treatment option for insomnia."( Pharmacology of ramelteon, a selective MT1/MT2 receptor agonist: a novel therapeutic drug for sleep disorders.
Miyamoto, M, 2009
)
1.42
"Ramelteon has demonstrated sleep-promoting effects in clinical trials, and coupled with its favorable safety profile and lack of abuse potential or dependence, this chronohypnotic provides an important treatment option for insomnia."( [A novel therapeutic drug: ramelteon].
Miyamoto, M, 2009
)
1.37
"Ramelteon has negligible affinity for the MT3 binding sites and other receptors in the brain, including the opiate, dopamine, benzodiazepine and serotonin receptors, which may explain the lack of significant adverse events and lack of abuse or dependence potential observed with ramelteon."( Ramelteon.
McGechan, A; Wellington, K, 2005
)
2.49
"Ramelteon has been shown to induce sleep initiation and maintenance in various animal models and in clinical trials."( Drug Insight: the use of melatonergic agonists for the treatment of insomnia-focus on ramelteon.
Cardinali, DP; Hardeland, R; Pandi-Perumal, SR; Poeggeler, B; Srinivasan, V, 2007
)
1.28
"Ramelteon also has a substantially longer half-life than melatonin."( Melatonergic drugs in clinical practice.
Cardinali, DP; Hardeland, R; Pandi-Perumal, SR; Poeggeler, B; Srinivasan, V; Trakht, I, 2008
)
1.07

Actions

Ramelteon did not produce respiratory depressant effects as measured by oxygenation or abnormal breathing events in subjects with moderate to severe COPD. Ramelteon didn't produce benzodiazepine-like discriminative stimulus effects at doses up to 10 mg/kg.

ExcerptReferenceRelevance
"The ramelteon group had a lower incidence of PRN antipsychotic use compared to those not given ramelteon (60 vs. "( Role of Ramelteon in Reduction of As-Needed Antipsychotics in Elderly Patients with Delirium in a General Hospital Setting.
Fazzari, M; James, SA; Lam, S; Pinkhasov, A; Singh, D, 2017
)
1.45
"Ramelteon did not produce respiratory depressant effects as measured by oxygenation or abnormal breathing events in subjects with moderate to severe COPD. "( The effects of ramelteon on respiration during sleep in subjects with moderate to severe chronic obstructive pulmonary disease.
Kryger, M; Roth, T; Wang-Weigand, S; Zhang, J, 2009
)
2.15
"Ramelteon did not produce benzodiazepine-like discriminative stimulus effects at doses up to 10 mg/kg."( Acute and chronic effects of ramelteon in rhesus monkeys (Macaca mulatta): dependence liability studies.
Cruź, CM; France, CP; Koek, W; McMahon, LR; Weltman, RH, 2006
)
1.35

Treatment

Ramelteon treatment did not have a clear effect on REM sleep without atonia or an RBD severity scale measured by video-supported polysomnography. Treatment also activated the Nrf2/HO-1 signaling pathway in LPS-induced HPMECs.

ExcerptReferenceRelevance
"Ramelteon treatment also activated the Nrf2/HO-1 signaling pathway in LPS-induced HPMECs."( Ramelteon protects against human pulmonary microvascular endothelial cell injury induced by lipopolysaccharide (LPS) via activating nuclear factor erythroid 2-related factor 2 (Nrf2)/heme oxygenase-1 (HO-1) pathway.
Gao, J; Huang, T; Lu, D; Wang, W; Yan, K; Yang, W; Zhang, Y, 2022
)
2.89
"Ramelteon treatment markedly reduced lung edema, serum malondialdehyde levels, the concentration of inflammatory cytokines in bronchoalveolar lavage fluid (BALF), NF-κB activation, iNOS levels, and apoptosis in the lung tissue. "( Melatonin receptor agonist protects against acute lung injury induced by ventilator through up-regulation of IL-10 production.
Chu, SJ; Huang, KL; Liao, WI; Pao, HP; Peng, CK; Wu, GC, 2020
)
2
"Ramelteon treatment did not have a clear effect on REM sleep without atonia or an RBD severity scale measured by video-supported polysomnography. "( An Open-Labeled Trial of Ramelteon in Idiopathic Rapid Eye Movement Sleep Behavior Disorder.
Esaki, Y; Fujishiro, H; Hirose, M; Iwata, N; Iwata, Y; Kitajima, T; Koike, S; Tsuchiya, A, 2016
)
2.18
"Ramelteon 8 mg treatment significantly reduced latency to persistent sleep compared with placebo (12.2 min vs. "( The effects of ramelteon in a first-night model of transient insomnia.
Roth, T; Sainati, S; Schwartz, H; Wang-Weigand, S; Zammit, G; Zhang, J, 2009
)
2.15
"Ramelteon treatment was associated with a statistically significant difference in sleep onset latency (SOL) as measured by polysomnography of 28.5 min (± 16.2 min) compared to placebo (95% C.I. "( Effectiveness of ramelteon for insomnia symptoms in older adults with obstructive sleep apnea: a randomized placebo-controlled pilot study.
Al-Shehabi, E; Gehrman, P; Gooneratne, NS; Gurubhagavatula, I; Marie, E; Schwab, R, 2010
)
2.14
"Treatment with ramelteon (0.03 and 0.3 mg/kg, p.o.) significantly shortened latency to sleep onset and significantly increased total duration of sleep."( Effects of ramelteon (TAK-375) on nocturnal sleep in freely moving monkeys.
Kimura, H; Miyamoto, M; Nishikawa, H; Ohkawa, S; Yoshikubo, S; Yukuhiro, N, 2004
)
1.05

Toxicity

Ramelteon produced significant reductions in latency to persistent sleep and increases in total sleep time and sleep efficacy. Adverse events were reported by three subjects in the ramelteon group: headache (n = 2) and urinary tract infection ( n = 1)

ExcerptReferenceRelevance
" There were no differences in the number or type of adverse events between any active treatment and placebo group."( An efficacy, safety, and dose-response study of Ramelteon in patients with chronic primary insomnia.
Erman, M; Sainati, S; Seiden, D; Zammit, G; Zhang, J, 2006
)
0.59
" Adverse events were reported by three subjects in the ramelteon group: headache (n = 2) and urinary tract infection (n = 1)."( Safety of ramelteon in individuals with mild to moderate obstructive sleep apnea.
Kryger, M; Roth, T; Wang-Weigand, S, 2007
)
0.99
" Incidences of adverse events considered treatment related were placebo (7%), ramelteon 4 mg (11%), and ramelteon 8 mg (5%)."( A 2-night, 3-period, crossover study of ramelteon's efficacy and safety in older adults with chronic insomnia.
Roth, T; Seiden, D; Wang-Weigand, S; Zhang, J, 2007
)
0.84
"In older adults with chronic primary insomnia, ramelteon produced significant reductions in latency to persistent sleep and increases in total sleep time and sleep efficacy, and showed no evidence of adverse next-day psychomotor or cognitive effects."( A 2-night, 3-period, crossover study of ramelteon's efficacy and safety in older adults with chronic insomnia.
Roth, T; Seiden, D; Wang-Weigand, S; Zhang, J, 2007
)
0.86
" Safety data indicate no evidence of clinically significant next-day performance effects and a reasonably low side effect profile."( Efficacy and clinical safety of ramelteon: an evidence-based review.
Kirby-Long, P; Sateia, MJ; Taylor, JL, 2008
)
0.63
"There were no noteworthy changes in vital signs, physical examinations, clinical chemistry, hematology, or urinalysis values and no electrocardiogram changes to suggest adverse cardiac effects."( Safety and subjective sleep effects of ramelteon administration in adults and older adults with chronic primary insomnia: a 1-year, open-label study.
Richardson, GS; Wang-Weigand, S; Zammit, G; Zhang, J, 2009
)
0.62
" Next-morning residual effects as well as adverse effects and vital signs were recorded at each visit."( Efficacy and safety of 6-month nightly ramelteon administration in adults with chronic primary insomnia.
Lehmann, R; Mayer, G; Partinen, M; Roth-Schechter, B; Staner, C; Wang-Weigand, S, 2009
)
0.62
" Most adverse events were mild or moderate in severity."( Efficacy and safety of 6-month nightly ramelteon administration in adults with chronic primary insomnia.
Lehmann, R; Mayer, G; Partinen, M; Roth-Schechter, B; Staner, C; Wang-Weigand, S, 2009
)
0.62
"Most NBZHs can be effective and safe agents for selected BD outpatients with episodic or chronic insomnia."( Efficacy and safety of nonbenzodiazepine hypnotics for chronic insomnia in patients with bipolar disorder.
Hang, E; Miller, AR; Nordahl, TE; Schaffer, CB; Schaffer, LC, 2011
)
0.37
" Adverse events were generally mild and transient."( Evaluation of subjective efficacy and safety of ramelteon in Japanese subjects with chronic insomnia.
Hamamura, M; Kuwano, T; Nagata, H; Nishiyama, H; Uchimura, N; Uchiyama, M, 2011
)
0.62
" Primary endpoints included adverse events, residual effects, rebound insomnia, withdrawal symptoms, and dependence."( Long-term safety and efficacy of ramelteon in Japanese patients with chronic insomnia.
Hamamura, M; Hashimoto, T; Kuwano, T; Nagata, H; Ogawa, A; Uchimura, N; Uchiyama, M, 2011
)
0.65
"Drug-related adverse events occurred in 11."( Long-term safety and efficacy of ramelteon in Japanese patients with chronic insomnia.
Hamamura, M; Hashimoto, T; Kuwano, T; Nagata, H; Ogawa, A; Uchimura, N; Uchiyama, M, 2011
)
0.65
" Ramelteon up to 16 mg nightly was safe and well tolerated."( Efficacy and safety of ramelteon in Japanese adults with chronic insomnia: a randomized, double-blind, placebo-controlled study.
Hamamura, M; Hashimoto, T; Nagata, H; Ogawa, A; Uchimura, N; Uchiyama, M, 2011
)
1.59
" Regarding safety, enteral SPM administration did not increase adverse events, including self-extubation."( Effect of enterally administered sleep-promoting medication on the intravenous sedative dose and its safety and cost profile in mechanically ventilated patients: A retrospective cohort study.
Hashimoto, T; Kataoka, Y; Matsumoto, M; Suzuki, T; Tsunemitsu, T, 2021
)
0.62
"Early enteral SPM administration reduced the average daily propofol dose per body weight without increasing adverse events."( Effect of enterally administered sleep-promoting medication on the intravenous sedative dose and its safety and cost profile in mechanically ventilated patients: A retrospective cohort study.
Hashimoto, T; Kataoka, Y; Matsumoto, M; Suzuki, T; Tsunemitsu, T, 2021
)
0.62

Pharmacokinetics

ExcerptReferenceRelevance
" Part 2 was a double-blind, randomized, 2-trial crossover pharmacodynamic study of 16-mg ramelteon and matching placebo."( Age and gender effects on the pharmacokinetics and pharmacodynamics of ramelteon, a hypnotic agent acting via melatonin receptors MT1 and MT2.
Greenblatt, DJ; Harmatz, JS; Karim, A, 2007
)
0.79
" A physiologically based pharmacokinetic (PBPK) model was constructed using the rat and dog pharmacokinetic data."( Impact of acute fat mobilisation on the pharmacokinetics of the highly fat distributed compound TAK-357, investigated by physiologically based pharmacokinetic (PBPK) modeling and simulation.
Asahi, S; DeJongh, J; Furukawa, Y; Goto, A; Moriwaki, T; Moriya, Y; Sato, S; Tagawa, Y; Tsukamoto, T; van Steeg, TJ; Wakabayashi, T, 2017
)
0.46

Compound-Compound Interactions

Ramelteon could be a treatment option for reducing nocturia in men with BPH.

ExcerptReferenceRelevance
"Ramelteon in combination with an α1-blocker could be a treatment option for reducing nocturia in men with BPH."( Ramelteon combined with an α1-blocker decreases nocturia in men with benign prostatic hyperplasia.
Ishiguro, H; Ito, H; Kawahara, T; Kubota, Y; Matsuzaki, J; Miyamoto, H; Morita, S; Sakata, R; Tanaka, K; Terao, H; Uemura, H, 2013
)
3.28
"Our study of drug-drug interaction (DDI) started with the clarification of unusually large DDI observed between ramelteon (RAM) and fluvoxamine (FLV)."( Usefulness of Two-Compartment Model-Assisted and Static Overall Inhibitory-Activity Method for Prediction of Drug-Drug Interaction.
Iga, K; Kiriyama, A, 2017
)
0.67

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

A total of 107 patients, aged 18-64 years, were randomized into a dosing sequence that included 4, 8, 16, and 32 mg of Ramelteon and placebo. The ability of long term melatonin treatment to improve cognition and attenuate neuropathology in AD mice did not generalize to this dosage.

ExcerptRelevanceReference
" A total of 107 patients, aged 18-64 years, were randomized into a dosing sequence that included 4, 8, 16, and 32 mg of Ramelteon and placebo."( An efficacy, safety, and dose-response study of Ramelteon in patients with chronic primary insomnia.
Erman, M; Sainati, S; Seiden, D; Zammit, G; Zhang, J, 2006
)
0.8
" The recommended dosage is 8mg but studies suggest a flat response across dosage ranges from 4 to 32mg."( Efficacy and clinical safety of ramelteon: an evidence-based review.
Kirby-Long, P; Sateia, MJ; Taylor, JL, 2008
)
0.63
" Subjects were administered study medication 30 minutes before bedtime and were awakened 2 hours after dosing to evaluate balance (Sensory Organization Test), turning speed and stability, memory (immediate and delayed word recall), and adverse events."( Effect of ramelteon on middle-of-the-night balance in older adults with chronic insomnia.
Peng, X; Rosenthal, M; Wang-Weigand, S; Zammit, G, 2009
)
0.76
" Ramelteon 8 and 32 mg significantly shortened the mean latency to persistent sleep in comparison with placebo, and there was a statistically significant trend for linear dose-response for this sleep parameter."( Efficacy and tolerability of ramelteon in a double-blind, placebo-controlled, crossover study in Japanese patients with chronic primary insomnia.
Kamikawa, K; Kanemura, T; Kohsaka, M; Kuwahara, H; Mikami, A; Murasaki, M; Ogawa, A; Sugita, Y; Taniguchi, M; Uno, H, 2011
)
1.57
"5 mg), and placebo on driving performance, memory functioning, psychomotor performance, and mood in healthy adult subjects following bedtime dosing and a middle of the night awakening."( Next-day effects of ramelteon (8 mg), zopiclone (7.5 mg), and placebo on highway driving performance, memory functioning, psychomotor performance, and mood in healthy adult subjects.
de Senerpont Domis, LM; de Vries, JM; Mets, MA; Olivier, B; Verster, JC; Volkerts, ER, 2011
)
0.69
" In cases where the dosage was significant enough to refer the patient to a health care facility, adverse clinical reactions and treatments are also described."( Ramelteon ingestions reported to Texas poison centers, 2005-2009.
Forrester, MB; Todd, CM, 2012
)
1.82
" The ability of long term melatonin treatment to improve cognition and attenuate neuropathology in AD mice did not generalize to this dosage of ramelteon."( Chronic ramelteon treatment in a mouse model of Alzheimer's disease.
Christie, MA; Connolly, NP; Jeffrey, BA; Lee, E; McCoy, JG; McKenna, JT; Strecker, RE; Ward, CP, 2012
)
1.01
" In the examination at our hospital, by the dosage of ramelteon to the insomniac patients complicated with nocturia, the increase of night bladder capacity and the decrease in number of urination times during night were accepted with improvement in insomnia."( [The onset mechanism of nocturia in the elderly and the possibility of ramelteon].
Shimizu, N, 2013
)
0.87
" Further trials are necessary to determine optimal dosage and safety of ramelteon in children."( [Treatment with ramelteon for sleep disturbance in severely disabled children and young adults].
Araki, A; Cho, K; Fukuda, I; Miyamoto, A; Oka, R; Tanaka, H, 2013
)
0.97
"A nightly dosage of ramelteon (8 mg) was given over a period of 3 weeks."( Pilot Study on the Effect of Ramelteon on Sleep Disturbance After Traumatic Brain Injury: Preliminary Evidence From a Clinical Trial.
Chiaravalloti, ND; Jasey, N; Lequerica, A; Portelli Tremont, JN, 2015
)
1.03
" Using this method, the ramelteon-victimized DDI could be simulated in comparison with other victim DDIs, assuming a consistent FLV dosing regimen."( Simulation of Metabolic Drug-Drug Interactions Perpetrated by Fluvoxamine Using Hybridized Two-Compartment Hepatic Drug-Pool-Based Tube Modeling and Estimation of In Vivo Inhibition Constants.
Iga, K, 2015
)
0.72
"In a dog toxicokinetic study, an unusual plasma concentration increase of the highly lipophilic compound TAK-357 was observed 2 weeks after termination of a 2-week repeated dosing in one dog with acute body weight loss."( Impact of acute fat mobilisation on the pharmacokinetics of the highly fat distributed compound TAK-357, investigated by physiologically based pharmacokinetic (PBPK) modeling and simulation.
Asahi, S; DeJongh, J; Furukawa, Y; Goto, A; Moriwaki, T; Moriya, Y; Sato, S; Tagawa, Y; Tsukamoto, T; van Steeg, TJ; Wakabayashi, T, 2017
)
0.46
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
indanes
[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]

Protein Targets (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency2.34850.001310.157742.8575AID1259253
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
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
Bile salt export pumpHomo sapiens (human)IC50 (µMol)109.00000.11007.190310.0000AID1449628; AID1473738
Melatonin receptor type 1AHomo sapiens (human)Ki0.00000.00000.27359.1000AID107729; AID108025; AID1775663
Melatonin receptor type 1BHomo sapiens (human)Ki0.00010.00000.16289.1000AID107729; AID108057; AID1775664
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)133.00002.41006.343310.0000AID1473739
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (59)

Processvia Protein(s)Taxonomy
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 pathway, coupled to cyclic nucleotide second messengerMelatonin receptor type 1AHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayMelatonin receptor type 1AHomo sapiens (human)
mating behaviorMelatonin receptor type 1AHomo sapiens (human)
circadian rhythmMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor signaling pathwayMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMelatonin receptor type 1BHomo sapiens (human)
chemical synaptic transmissionMelatonin receptor type 1BHomo sapiens (human)
negative regulation of cGMP-mediated signalingMelatonin receptor type 1BHomo sapiens (human)
glucose homeostasisMelatonin receptor type 1BHomo sapiens (human)
camera-type eye developmentMelatonin receptor type 1BHomo sapiens (human)
negative regulation of neuron apoptotic processMelatonin receptor type 1BHomo sapiens (human)
negative regulation of vasoconstrictionMelatonin receptor type 1BHomo sapiens (human)
positive regulation of circadian sleep/wake cycle, non-REM sleepMelatonin receptor type 1BHomo sapiens (human)
negative regulation of insulin secretionMelatonin receptor type 1BHomo sapiens (human)
regulation of insulin secretionMelatonin receptor type 1BHomo sapiens (human)
negative regulation of cytosolic calcium ion concentrationMelatonin receptor type 1BHomo sapiens (human)
negative regulation of transmission of nerve impulseMelatonin receptor type 1BHomo sapiens (human)
positive regulation of transmission of nerve impulseMelatonin receptor type 1BHomo sapiens (human)
regulation of neuronal action potentialMelatonin receptor type 1BHomo sapiens (human)
G protein-coupled receptor signaling pathwayMelatonin receptor type 1BHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (28)

Processvia Protein(s)Taxonomy
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)
protein bindingMelatonin receptor type 1AHomo sapiens (human)
melatonin receptor activityMelatonin receptor type 1AHomo sapiens (human)
hormone bindingMelatonin receptor type 1AHomo sapiens (human)
organic cyclic compound bindingMelatonin receptor type 1AHomo sapiens (human)
G protein-coupled receptor activityMelatonin receptor type 1AHomo sapiens (human)
protein bindingMelatonin receptor type 1BHomo sapiens (human)
melatonin receptor activityMelatonin receptor type 1BHomo sapiens (human)
G protein-coupled receptor activityMelatonin receptor type 1BHomo 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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
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 membraneMelatonin receptor type 1AHomo sapiens (human)
receptor complexMelatonin receptor type 1AHomo sapiens (human)
plasma membraneMelatonin receptor type 1AHomo sapiens (human)
plasma membraneMelatonin receptor type 1BHomo sapiens (human)
synapseMelatonin receptor type 1BHomo sapiens (human)
plasma membraneMelatonin receptor type 1BHomo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (82)

Assay IDTitleYearJournalArticle
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.
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.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
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.
AID568003Drug level in rat plasma at 10 mg/kg, ip after 1 hr2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID567995Intrinsic activity at rat MT2 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay relative to agomelatine2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
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.
AID1775390Drug concentration in Wistar Han rat brain at 100 mg/kg, po measured at 0.37 hrs by HPLC-MS/MS
AID1775664Binding affinity to human MT2 expressed in CHO cells
AID232612Ratio of IC50 against cAMP to that of Ki of human melatonin receptor (MT1).2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.
AID1775397Ratio of drug concentration in brain to plasma in Wistar Han rat at 100 mg/kg, po measured at 6 hrs by HPLC-MS/MS
AID1775672Drug concentration in Sprague-Dawley rat plasma at 1 mg/kg, po after 60 mins by LC/MS/MS analysis
AID1775674Ratio of drug concentration in brain to plasma in Sprague-Dawley rat at 1 mg/kg, po after 60 mins by LC/MS/MS analysis
AID108057Binding affinity against human Melatonin receptor type 1B (MT2)2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.
AID1775394Ratio of drug concentration in brain to plasma in Wistar Han rat at 100 mg/kg, po measured at 2 hrs by HPLC-MS/MS
AID1775392Drug concentration in Wistar Han rat plasma at 100 mg/kg, po measured at 2 hrs by HPLC-MS/MS
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.
AID1775393Drug concentration in Wistar Han rat brain at 100 mg/kg, po measured at 2 hrs by HPLC-MS/MS
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1775670Drug concentration in Sprague-Dawley rat brain at 1 mg/kg, po after 60 mins by LC/MS/MS analysis
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.
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.
AID1775668Oral bioavailability in Sprague-Dawley rat at 1 mg/kg by LC/MS/MS analysis
AID1597740Half life in human at 8 mg treated 30 mins before bedtime2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Sleep modulating agents.
AID567994Intrinsic activity at rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay relative to ramelteon2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID568001Intrinsic clearance in rat liver microsome at 1 uM by LC/MS analysis2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1775667Clearance in rat hepatic microsomes at 1 umol/L incubated for 20 mins in presence of NADPH generating system by HPLC-UV analysis
AID568000Intrinsic clearance in human liver microsome at 1 uM by LC/MS analysis2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID567992Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID1138157Half life of the compound assessed as CYP3A4 (unknown origin)-mediated drug metabolism2014Journal of medicinal chemistry, Apr-24, Volume: 57, Issue:8
MT1 and MT2 melatonin receptors: ligands, models, oligomers, and therapeutic potential.
AID1775396Drug concentration in Wistar Han rat brain at 100 mg/kg, po measured at 6 hrs by HPLC-MS/MS
AID107729Binding affinity against human Melatonin receptor type 1A (MT1) in CHO cells2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.
AID108025Binding affinity against human Melatonin receptor type 1A (MT1)2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.
AID1775389Drug concentration in Wistar Han rat plasma at 100 mg/kg, po measured at 0.37 hrs by HPLC-MS/MS
AID1775395Drug concentration in Wistar Han rat plasma at 100 mg/kg, po measured at 6 hrs by HPLC-MS/MS
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.
AID1775663Binding affinity to human MT1 expressed in CHO cells
AID568004Ratio of drug level in rat brain to plasma at 10 mg/kg, ip after 1 hr2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID567997Displacement of [3H]melatonin from rat MT2 receptor expressed in CHO-Galpha16 cells2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID1775666Clearance in human hepatic microsomes at 1 umol/L incubated for 20 mins in presence of NADPH generating system by HPLC-UV analysis
AID567996Displacement of [3H]melatonin from rat MT1 receptor expressed in CHO-Galpha16 cells2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID1775391Ratio of drug concentration in brain to plasma in Wistar Han rat at 100 mg/kg, po measured at 0.37 hrs by HPLC-MS/MS
AID179962Inhibition of forskolin stimulated cAMP production in neonatal rat pituitary2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.
AID568002Drug level in rat brain at 10 mg/kg, ip after 1 hr2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID1597726Oral bioavailability in human2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Sleep modulating agents.
AID107723Binding affinity against Melatonin receptor 3 (MT3) of Syrian hamster brain and peripheral organs2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Synthesis of a novel series of tricyclic indan derivatives as melatonin receptor agonists.
AID567993Binding affinity to rat MT2 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay2011Bioorganic & medicinal chemistry letters, Feb-15, Volume: 21, Issue:4
Design and synthesis of 4-arylpiperidinyl amide and N-arylpiperdin-3-yl-cyclopropane carboxamide derivatives as novel melatonin receptor ligands.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS 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.
AID1346274Human MT2 receptor (Melatonin receptors)2005Neuropharmacology, Feb, Volume: 48, Issue:2
Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist.
AID1346274Human MT2 receptor (Melatonin receptors)2011Chronobiology international, Feb, Volume: 28, Issue:1
Circadian periods of sensitivity for ramelteon on the onset of running-wheel activity and the peak of suprachiasmatic nucleus neuronal firing rhythms in C3H/HeN mice.
AID1346220Human MT1 receptor (Melatonin receptors)2005Neuropharmacology, Feb, Volume: 48, Issue:2
Neurochemical properties of ramelteon (TAK-375), a selective MT1/MT2 receptor agonist.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (309)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's90 (29.13)29.6817
2010's150 (48.54)24.3611
2020's69 (22.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 63.13

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 Index63.13 (24.57)
Research Supply Index5.93 (2.92)
Research Growth Index4.72 (4.65)
Search Engine Demand Index158.69 (26.88)
Search Engine Supply Index2.95 (0.95)

This Compound (63.13)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials59 (18.61%)5.53%
Reviews82 (25.87%)6.00%
Case Studies31 (9.78%)4.05%
Observational3 (0.95%)0.25%
Other142 (44.79%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]