Page last updated: 2024-12-08

esketamine

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Description

esketamine : The S- (more active) enantiomer of ketamine. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID182137
CHEMBL ID395091
CHEBI ID60799
SCHEMBL ID5512024

Synonyms (55)

Synonym
(s)-2-(o-chlorophenyl)-2-(methylamino)cyclohexanone
(2s)-2-(2-chlorophenyl)-2-(methylamino)cyclohexanone
D07283
esketamine (usan/inn)
(s)-(-)-ketamine
cyclohexanone, 2-(2-chlorophenyl)-2-(methylamino)-, (s)-
l-ketamine
(s)-ketamine
esketamine
cyclohexanone, 2-(o-chlorophenyl)-2-(methylamino)-, (-)- (8ci)
33643-46-8
cyclohexanone, 2-(2-chlorophenyl)-2-(methylamino)-, (2s)-
(-)-ketamine
cyclohexanone, 2-(2-chlorophenyl)-2-(methylamino)-, (2s)- (9ci)
s-ketamine
ketaved
CHEMBL395091
ketamine, (s)-
keta-s
chebi:60799 ,
jnj-54135419
ketamine, s-
s-(-)-ketamine
(2s)-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one
unii-50lfg02txd
spravato
kataved
esketamine [usan:inn:ban]
50lfg02txd ,
cas-33643-46-8
dtxcid4027787
tox21_113206
NCGC00185910-01
dtxsid6047810 ,
esketamine [usan]
cyclohexanone, 2-(o-chlorophenyl)-2-(methylamino)-, (-)-
esketamine [who-dd]
esketamine [inn]
SCHEMBL5512024
gtpl9152
(2s)-2-(2-chlorophenyl)-2-methylaminocyclohexan-1-one
AKOS027321219
YQEZLKZALYSWHR-ZDUSSCGKSA-N
s-ketamin
DB11823
Q2365493
33643-46-8 (free base)
esketamine free base
(s)-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one
JC9 ,
(2~{s})-2-(2-chlorophenyl)-2-(methylamino)cyclohexan-1-one
esketaminum
n06ax27
n01ax14
esketamina

Research Excerpts

Overview

Esketamine is a novel treatment for treatment resistant depression (TRD) and was approved by the FDA in early 2019. Esketamine, which is an S-enantiomer of ketamine, is better than conventional antidepressants and even better than R-ketamine.

ExcerptReferenceRelevance
"Esketamine is an N-methyl-D-aspartic acid (NMDA) receptor antagonist, which has stronger sedative and analgesic effects and fewer adverse events than ketamine. "( Clinical effects of low-dose esketamine for anaesthesia induction in the elderly: A randomized controlled trial.
Li, J; Wang, A; Wang, Z, 2022
)
2.46
"Esketamine is an antagonist of the N-methyl-D-aspartate receptor (NMDA receptor) that is widely used for multimodal analgesia. "( Subanaesthetic dose of esketamine during induction delays anaesthesia recovery a randomized, double-blind clinical trial.
Bao, F; He, J; Shi, Q; Xu, J; Zhang, C, 2022
)
2.47
"Esketamine is a new anesthetic, sedative, and analgesic drug."( Efficacy of Analgesic Propofol/Esketamine and Propofol/Fentanyl for Painless Induced Abortion: A Randomized Clinical Trial.
Jin, S; Xin, N; Yan, W, 2022
)
1.73
"Esketamine is a novel treatment for treatment resistant depression (TRD) and was approved by the FDA in early 2019. "( Adjunctive dopaminergic enhancement of esketamine in treatment-resistant depression.
Cook, J; Halaris, A, 2022
)
2.43
"Esketamine, which is an S-enantiomer of ketamine, is better than conventional antidepressants and even better than R-ketamine. "( Esketamine-A quick-acting novel antidepressant without the disadvantages of ketamine.
Javed, S; Kotra, M; Malathesh, BC; Nguyen, VS; Shoib, S, 2022
)
3.61
"Esketamine is a N-methyl-D-aspartate receptor (NMDA) antagonist and a common analgesic."( Effect of different doses of esketamine compared with fentanyl combined with propofol on hypotension in patients undergoing painless abortion surgery: a prospective, randomized, double-blind controlled clinical trial.
Chen, J; Hu, B; Shen, M; Wang, F; Yang, Y; Zhou, Q; Zou, X, 2022
)
1.73
"Esketamine is an S (+) enantiomer of ketamine with greater potency and similar psychomimetic effects compared to racemic ketamine. "( Safety and tolerability of esketamine in propofol based sedation for endoscopic variceal ligation with or without injection sclerotherapy: Randomized controlled trial.
Chen, J; Chen, X; Chen, Y; Dan, L; Duan, G; Huang, H; Liu, R; Lyu, H; Wang, Q; Wang, T, 2023
)
2.65
"Esketamine is a NMDA antagonist that has been proven to be beneficial for ameliorating respiratory depression owing to its sympathomimetic effect; however, there are no relevant reports on its use in patients with obesity."( Efficacy and Safety of a Subanesthetic Dose of Esketamine Combined with Propofol in Patients with Obesity Undergoing Painless Gastroscopy: A Prospective, Double-Blind, Randomized Controlled Trial.
Fan, G; Li, Y; Liang, W; Ma, Q; Meng, F; Qin, W; Ren, Z; Wang, Y; Yin, N; Zhang, X; Zheng, L, 2023
)
1.89
"Esketamine is a new N-methyl-D-aspartate receptor antagonist, with enhanced analgesic effects."( Efficacy of Patient-Controlled Intravenous Analgesia with Esketamine for Herpes Zoster Associated with Breakthrough Pain.
Fei, Y; Huang, B; Tang, J; Yao, M; Zhang, E, 2023
)
1.88
"Esketamine nasal spray is a novel therapy for treatment-resistant depression (TRD). "( Access and real-world use patterns of esketamine nasal spray among patients with treatment-resistant depression covered by private or public insurance.
Caron-Lapointe, G; Joshi, K; Lefebvre, P; Pilon, D; Teeple, A; Zhdanava, M, 2023
)
2.62
"Esketamine is an NMDA receptor antagonist inducing antidepressant effects within hours."( The effects of esketamine and treatment expectation in acute major depressive disorder (Expect): study protocol for a pharmacological fMRI study using a balanced placebo design.
Bitsch, F; Falkenberg, I; Kircher, T; Liu, W; Matsingos, A; Noor, L; Vogelbacher, C; Yildiz, C, 2023
)
1.98
"Esketamine is a commonly used drug in pediatric general anesthesia due to its good analgesic and sedative effects."( Effect of intravenous induction with different doses of Esketamine combined with propofol and sufentanil on intraocular pressure among pediatric strabismus surgery: a randomized clinical trial.
Luo, J; Sun, R; Yin, K; Zhang, Z; Zhao, D, 2023
)
1.88
"Esketamine appears to be an effective therapy when combined with oral antidepressants in patients with TRD."( Esketamine: a glimmer of hope in treatment-resistant depression.
Chakrabarti, SS; Kaur, U; Pathak, BK; Singh, A, 2021
)
2.79
"Esketamine nasal spray is a novel, fast-acting agent that provides an additional treatment option for patients with TRD who have previously failed several therapies. "( Practical recommendations for the management of treatment-resistant depression with esketamine nasal spray therapy: Basic science, evidence-based knowledge and expert guidance.
Cubała, WJ; Fagiolini, A; Kasper, S; Ramos-Quiroga, JA; Souery, D; Young, AH, 2021
)
2.29
"Esketamine is a promising drug which can induce antidepressant effects in Major Depression Disorder (MDD). "( Adverse Effects of Esketamine for the Treatment of Major Depression Disorder: Findings from Randomized Controlled Trials.
Chen, G; Li, X; Wang, J; Wang, T; Xu, X; Xu, Z; Yang, S; Zhou, X, 2022
)
2.49

Effects

Esketamine has been approved as a rapid-acting intranasal treatment for treatment-resistant depression (TRD) Esketamine and ketamine have been shown to decrease inflammation in numerous ways principally through reducing pro-inflammatory cytokines.

ExcerptReferenceRelevance
"Esketamine has a favorable risk-to-benefit profile, with demonstrated efficacy in reducing depressive symptoms more rapidly than monotherapy with traditional oral antidepressants."( Intranasal esketamine: A novel drug for treatment-resistant depression.
Khorassani, F; Talreja, O, 2020
)
1.67
"Esketamine (ESK) has been approved as a rapid-acting intranasal treatment for treatment-resistant depression (TRD). "( Long-Term Efficacy of Intranasal Esketamine in Treatment-Resistant Major Depression: A Systematic Review.
Buoli, M; Caldiroli, A; Capellazzi, M; Capuzzi, E; Clerici, M; Colmegna, F; Dakanalis, A; Marcatili, M; Tagliabue, I, 2021
)
2.35
"Esketamine has recently emerged as a new treatment for TRD due to its rapid antidepressant effects."( Cost-utility analysis of esketamine and electroconvulsive therapy in adults with treatment-resistant depression.
Asellus, P; Degerlund Maldi, K; Myléus, A; Norström, F, 2021
)
1.65
"Esketamine and ketamine have been shown to decrease inflammation in numerous ways principally through reducing pro-inflammatory cytokines (e.g., TNF-α, IL-6) (Loix et al., Acta Anaesthesiol Belg 62(1):47-58, 2011; Chen et al., Psychiatry Res 269:207-11, 2018; Kopra et al., J Psychopharmacol 35(8):934-45, 2021)."( The Glutamatergic System in Treatment-Resistant Depression and Comparative Effectiveness of Ketamine and Esketamine: Role of Inflammation?
Cook, J; Halaris, A, 2023
)
1.85
"Esketamine has higher potency, stronger receptor affinity, a stronger analgesic effect, a higher in vivo clearance rate, and a lower incidence of adverse reactions when compared to ketamine. "( Intraoperative intravenous low-dose esketamine improves quality of early recovery after laparoscopic radical resection of colorectal cancer: A prospective, randomized controlled trial.
Ai, Y; He, L; Liu, S; Xu, Y; Zhang, C, 2023
)
2.63
"Esketamine has been licensed for 'treatment-resistant depression' in the USA, UK and Europe. "( Are we repeating mistakes of the past? A review of the evidence for esketamine.
Horowitz, MA; Moncrieff, J, 2021
)
2.3
"Esketamine has a favorable risk-to-benefit profile, with demonstrated efficacy in reducing depressive symptoms more rapidly than monotherapy with traditional oral antidepressants."( Intranasal esketamine: A novel drug for treatment-resistant depression.
Khorassani, F; Talreja, O, 2020
)
1.67

Treatment

Esketamine is a novel treatment for treatment resistant depression (TRD) and was approved by the FDA in early 2019. Treatment with esketamine may lead to an increased risk of lower urinary tract symptoms, such as dysuria or urgency.

ExcerptReferenceRelevance
"Esketamine is a novel treatment for treatment resistant depression (TRD) and was approved by the FDA in early 2019. "( Adjunctive dopaminergic enhancement of esketamine in treatment-resistant depression.
Cook, J; Halaris, A, 2022
)
2.43
"Esketamine effectively treated postoperative depressive symptoms of patients with a missed miscarriage, decreasing propofol consumption and inflammatory response."( Evaluation of clinical effects of Esketamine on depression in patients with missed miscarriage: A randomized, controlled, double-blind trial.
Feng, S; Jiang, M; Li, Q; Mao, M; Wen, Y; Xu, C; Yuan, H; Zhou, R, 2023
)
2.63
"The esketamine treatment schedule involved a maximum of 3× weekly dosing at 0.25-0.5 mg/kg i.v."( Urothelial toxicity of esketamine in the treatment of depression.
Bauer, M; Cleare, A; Findeis, H; Ritter, P; Sauer, C, 2020
)
1.35
"Esketamine-treated patients with and without anxiety demonstrated significant reductions in MADRS (mean [SD] change from baseline at day 28: -21.0 [12.51] and -22.7 [11.98], respectively)."( The effect of esketamine in patients with treatment-resistant depression with and without comorbid anxiety symptoms or disorder.
Borentain, S; Daly, EJ; Fedgchin, M; Ionescu, DF; Salvadore, G; Singh, JB; Starr, HL; Thase, ME; Trivedi, MH; Turkoz, I, 2021
)
1.7
"Treatment with esketamine may lead to an increased risk of lower urinary tract symptoms, such as dysuria or urgency."( Long-term safety of ketamine and esketamine in treatment of depression.
Krystal, JH; Murphy, E; Nikayin, S; Wilkinson, ST, 2022
)
1.34

Toxicity

All esketamine doses were safe and tolerated. Propofol was effective and safe in painless gastrointestinal endoscopy as evidenced by less propofol consumption per minute, shorter induction time, and lower incidence of cough and body movement. Intravenous, subcutaneous, and possibly oral esketamines may offer an effective andsafe addition to the depression treatment armamentarium.

ExcerptReferenceRelevance
" Three of 56 (5%) esketamine-treated participants during the double-blind phase vs none receiving placebo and 1 of 57 participants (2%) during the open-label phase had adverse events that led to study discontinuation (1 event each of syncope, headache, dissociative syndrome, and ectopic pregnancy)."( Efficacy and Safety of Intranasal Esketamine Adjunctive to Oral Antidepressant Therapy in Treatment-Resistant Depression: A Randomized Clinical Trial.
Cooper, K; Daly, EJ; Drevets, WC; Fedgchin, M; Lim, P; Manji, H; Shelton, RC; Singh, JB; Thase, ME; Van Nueten, L; Winokur, A, 2018
)
1.09
" The most common adverse events among participants in the esketamine group were nausea, dizziness, dissociation, unpleasant taste, and headache."( Efficacy and Safety of Intranasal Esketamine for the Rapid Reduction of Symptoms of Depression and Suicidality in Patients at Imminent Risk for Suicide: Results of a Double-Blind, Randomized, Placebo-Controlled Study.
Alphs, L; Canuso, CM; Drevets, WC; Fedgchin, M; Hough, D; Lane, R; Lim, P; Manji, H; Pinter, C; Sanacora, G; Singh, JB, 2018
)
1
" The most common (>20%) adverse events reported for esketamine/antidepressant were nausea, dissociation, dizziness, vertigo, and headache."( Efficacy and Safety of Fixed-Dose Esketamine Nasal Spray Combined With a New Oral Antidepressant in Treatment-Resistant Depression: Results of a Randomized, Double-Blind, Active-Controlled Study (TRANSFORM-1).
Ameele, HVD; Blier, P; Daly, EJ; Drevets, WC; Fava, M; Fedgchin, M; Gaillard, R; Hough, D; Lane, R; Liebowitz, M; Lim, P; Manji, H; Melkote, R; Preskorn, S; Ravindran, A; Singh, JB; Trivedi, M; Vitagliano, D, 2019
)
1.04
"5 mg/kg was generally safe and tolerated in patients undergoing painless gastroscopy."( Pharmacokinetics and Safety of Esketamine in Chinese Patients Undergoing Painless Gastroscopy in Comparison with Ketamine: A Randomized, Open-Label Clinical Study.
Cui, C; Huang, J; Pei, Q; Wang, J; Wang, SY; Yang, GP; Yang, S; Ye, L, 2019
)
0.8
" For adverse events, odds ratio (OR) [95% confidence interval] for esketamine/antidepressant versus antidepressant/placebo was calculated."( Cardiac Safety of Esketamine Nasal Spray in Treatment-Resistant Depression: Results from the Clinical Development Program.
Doherty, T; Melkote, R; Miller, J; Singh, JB; Wajs, E; Weber, MA, 2020
)
1.13
" Common treatment-emergent adverse events (TEAEs) were dizziness (32."( Esketamine Nasal Spray Plus Oral Antidepressant in Patients With Treatment-Resistant Depression: Assessment of Long-Term Safety in a Phase 3, Open-Label Study (SUSTAIN-2).
Aluisio, L; Daly, EJ; Drevets, WC; George, JE; Grunfeld, J; Holder, R; Hough, D; Jeon, HJ; Kasper, S; Lane, R; Li, CT; Lim, P; Manji, H; Morrison, RL; Paik, JW; Sanacora, G; Singh, JB; Sulaiman, AH; Wajs, E; Wilkinson, ST; Young, AH, 2020
)
2
"Using the FDA Adverse Event Reporting System (FAERS) database (March 2019-March 2020), we analysed esketamine-related adverse events (AEs) to detect and characterize relevant safety signals."( Post-Marketing Safety Concerns with Esketamine: A Disproportionality Analysis of Spontaneous Reports Submitted to the FDA Adverse Event Reporting System.
Barbui, C; Gastaldon, C; Kane, JM; Raschi, E; Schoretsanitis, G, 2021
)
1.11
" Therefore, we carried out a meta-analysis to assess adverse effect profiles of esketamine for the treatment of MDD."( Adverse Effects of Esketamine for the Treatment of Major Depression Disorder: Findings from Randomized Controlled Trials.
Chen, G; Li, X; Wang, J; Wang, T; Xu, X; Xu, Z; Yang, S; Zhou, X, 2022
)
1.28
" The most common treatment-emergent adverse events associated with ketamine/esketamine are dissociation, anxiety, nausea, increased blood pressure, and headache."( Prevention and Management of Common Adverse Effects of Ketamine and Esketamine in Patients with Mood Disorders.
Cao, B; Ceban, F; Chau, EH; Gill, H; Ho, RC; Kratiuk, K; Kumar, A; Lee, JG; Lee, Y; Lin, K; Lipsitz, O; Lui, LMW; Mansur, RB; McIntyre, RS; Nasri, F; Rodrigues, NB; Rosenblat, JD; Subramaniapillai, M; Swainson, J, 2021
)
1.09
" The most common treatment-emergent adverse events during the DB induction phase in the combined esketamine group (incidences ranging from 12."( Efficacy and safety of fixed doses of intranasal Esketamine as an add-on therapy to Oral antidepressants in Japanese patients with treatment-resistant depression: a phase 2b randomized clinical study.
Goto, R; Shimizu, H; Shiraishi, A; Takahashi, N; Tominaga, Y; Yamada, A, 2021
)
1.09
" All esketamine doses were safe and tolerated."( Efficacy and safety of fixed doses of intranasal Esketamine as an add-on therapy to Oral antidepressants in Japanese patients with treatment-resistant depression: a phase 2b randomized clinical study.
Goto, R; Shimizu, H; Shiraishi, A; Takahashi, N; Tominaga, Y; Yamada, A, 2021
)
1.39
" Treatment-emergent adverse events (TEAEs) reported in younger versus older patients, respectively, were: induction, 86."( Comparison of Long-Term Efficacy and Safety of Esketamine Nasal Spray Plus Oral Antidepressant in Younger Versus Older Patients With Treatment-Resistant Depression: Post-Hoc Analysis of SUSTAIN-2, a Long-Term Open-Label Phase 3 Safety and Efficacy Study.
Daly, EJ; Drevets, WC; Hough, D; Jamieson, C; Lane, R; Lim, P; Manji, H; Ochs-Ross, R; Sanacora, G; Singh, JB; Steffens, DC; Wajs, E; Zhang, Y, 2022
)
0.98
" Beside adverse events that may be sought for abuse purpose (e."( Safety concerns on the abuse potential of esketamine: Multidimensional analysis of a new anti-depressive drug on the market.
Baudot, J; Mezaache, S; Micallef, J; Navarro, N; Soeiro, T; Tambon, M; Veyrac, G, 2022
)
0.99
" The most common adverse events in esketamine-treated patients were nausea, dissociation, dizziness, and vertigo, each reported at a rate higher in women than men."( Efficacy and safety of esketamine nasal spray by sex in patients with treatment-resistant depression: findings from short-term randomized, controlled trials.
Canuso, CM; Cooper, K; Daly, EJ; Freeman, MP; Jones, RR; Kornstein, SG; Nicholson, S, 2022
)
1.31
"01; I2<1%), dropouts due to adverse events (RR=1."( Efficacy and safety of racemic ketamine and esketamine for depression: a systematic review and meta-analysis.
Bahji, A; Vazquez, GH; Zarate, CA, 2022
)
0.98
"After pooling data from seven randomized controlled trials, treatment with adjunctive IN esketamine vs IN placebo was safe overall, and more effective at decreasing depressive symptoms (d = -0."( The efficacy and safety of adjunctive intranasal esketamine treatment in major depressive disorder: a systematic review and meta-analysis.
Alnafeesi, Y; Ceban, F; Di Vincenzo, JD; Gillissie, ES; Jaberi, S; Jawad, MY; Lui, LMW; McIntyre, RS; Rosenblat, JD, 2022
)
1.2
" Hence, our preclinical studies demonstrated that dry powder inhalation is a highly efficacious and safe delivery route for esketamine and may be a viable alternative administration route meriting further clinical development."( Esketamine inhaled as dry powder: Pharmacokinetic, pharmacodynamic and safety assessment in a preclinical study.
Abramski, K; Dera, P; Gajos-Draus, A; Janicka, M; Janowska, S; Kamil, K; Mach, M; Matłoka, M; Moszczyński-Pętkowski, R; Pankiewicz, P; Perko, P; Pieczykolan, J; Teska-Kamińska, M; Tratkiewicz, E; Wieczorek, M; Ziółkowski, H, 2022
)
2.37
" Finally, continuing to monitor research subjects and patients long-term for the emergence of adverse effects on cognition or other organ systems is critical."( Key considerations for the use of ketamine and esketamine for the treatment of depression: focusing on administration, safety, and tolerability.
Kritzer, MD; Masand, PS; Pae, CU, 2022
)
0.98
"Intravenous, subcutaneous, and possibly oral esketamine may offer an effective and safe addition to the depression treatment armamentarium."( The antidepressant effect and safety of non-intranasal esketamine: A systematic review.
Aan Het Rot, M; Kamphuis, J; Schoevers, RA; Smith-Apeldoorn, SY; Veraart, JK; Vischjager, M, 2022
)
1.23
" In addition to other clinical and environmental confounders, prior information on the pharmacodynamic and pharmacokinetic determinants of response variability to ketamine and esketamine may inform on dose optimization and identification of individuals at risk of adverse drug reactions."( Pharmacogenetic and drug interaction aspects on ketamine safety in its use as antidepressant - implications for precision dosing in a global perspective.
Just, KS; Langmia, IM; Müller, JP; Stingl, JC; Yamoune, S, 2022
)
0.91
" Hemodynamic index, pulse oxygen saturation, operative time, induction time, awakening status, orientation recovery time, adverse events, and Mini-Mental State Examination (MMSE) were also recorded during gastrointestinal endoscopy."( Efficacy and safety of subanesthetic doses of esketamine combined with propofol in painless gastrointestinal endoscopy: a prospective, double-blind, randomized controlled trial.
Li, J; Li, S; Li, Y; Liang, S; Liang, Z; Luo, Q; Yang, Z; Zhan, Y, 2022
)
0.98
"2 mg/kg esketamine and propofol was effective and safe in painless gastrointestinal endoscopy as evidenced by less propofol consumption per minute, shorter induction time, and lower incidence of cough and body movement relative to propofol alone."( Efficacy and safety of subanesthetic doses of esketamine combined with propofol in painless gastrointestinal endoscopy: a prospective, double-blind, randomized controlled trial.
Li, J; Li, S; Li, Y; Liang, S; Liang, Z; Luo, Q; Yang, Z; Zhan, Y, 2022
)
1.41
" Esketamine was safe and well tolerated."( Efficacy and Safety of Subcutaneous Esketamine in the Treatment of Suicidality in Major Depressive Disorder and Bipolar Depression.
Abdo, GL; Barbosa, MG; de Oliveira Cerqueira, R; Del Porto, JA; Del Sant, LC; Delfino, RS; Fava, VAR; Grossi, JD; Lacerda, ALT; Lucchese, AC; Magalhães, E; Nakahira, C; Sarin, LM; Steglich, MS; Surjan, J; Tuena, MA, 2022
)
1.91
" Frequency of response to specific CADSS items was examined to investigate qualitative differences in the pattern of symptoms reported across investigator-reported levels of adverse event severity."( Adverse Events and Measurement of Dissociation After the First Dose of Esketamine in Patients With TRD.
Borentain, S; Drevets, WC; Singh, JB; Turkoz, I; Wajs, E; Williamson, D, 2023
)
1.14
"Dissociation was reported as an adverse event in 14."( Adverse Events and Measurement of Dissociation After the First Dose of Esketamine in Patients With TRD.
Borentain, S; Drevets, WC; Singh, JB; Turkoz, I; Wajs, E; Williamson, D, 2023
)
1.14
"CADSS scores and severity of dissociation adverse events move generally in the same direction; however, there is substantial variability in this relationship."( Adverse Events and Measurement of Dissociation After the First Dose of Esketamine in Patients With TRD.
Borentain, S; Drevets, WC; Singh, JB; Turkoz, I; Wajs, E; Williamson, D, 2023
)
1.14
" The primary outcome was the incidence of sedation-related adverse events."( Safety and efficacy of the combination of esketamine and propofol in procedural sedation/analgesia: a systematic review and meta-analysis.
Chen, Q; Hu, X; Huang, X; Lin, F,
)
0.4
" Despite study limitations related to the inherent nature of the study, a limited number of patients, and a short follow-up period, ESK-NS showed to be effective and safe in patients diagnosed with TRD comorbid with a SUD."( Esketamine in treatment-resistant depression patients comorbid with substance-use disorder: A viewpoint on its safety and effectiveness in a subsample of patients from the REAL-ESK study.
Andriola, I; Barlati, S; Bassetti, R; Chiappini, S; Clerici, M; d'Andrea, G; De Filippis, S; Dell'Osso, B; Di Nicola, M; Martinotti, G; Pettorruso, M; Sensi, S; Vita, A, 2023
)
2.35
" Adverse events and satisfaction scores were also recorded."( Efficacy and Safety of a Subanesthetic Dose of Esketamine Combined with Propofol in Patients with Obesity Undergoing Painless Gastroscopy: A Prospective, Double-Blind, Randomized Controlled Trial.
Fan, G; Li, Y; Liang, W; Ma, Q; Meng, F; Qin, W; Ren, Z; Wang, Y; Yin, N; Zhang, X; Zheng, L, 2023
)
1.17
"25 mg/kg) improves the safety and reduces the incidence of adverse events in patients with obesity during painless gastroscopy."( Efficacy and Safety of a Subanesthetic Dose of Esketamine Combined with Propofol in Patients with Obesity Undergoing Painless Gastroscopy: A Prospective, Double-Blind, Randomized Controlled Trial.
Fan, G; Li, Y; Liang, W; Ma, Q; Meng, F; Qin, W; Ren, Z; Wang, Y; Yin, N; Zhang, X; Zheng, L, 2023
)
1.17
" Common treatment-emergent adverse events (≥20%) were headache, dizziness, nausea, dissociation, somnolence, and nasopharyngitis."( Long-term safety and maintenance of response with esketamine nasal spray in participants with treatment-resistant depression: interim results of the SUSTAIN-3 study.
Chen, LN; Doherty, T; Drevets, WC; Fu, DJ; Lane, R; Morrison, RL; Popova, V; Sanacora, G; Wilkinson, ST; Zaki, N, 2023
)
1.16
" Response (≥50% improvement in total score from baseline for Montgomery-Åsberg Depression Rating Scale [MADRS] and Patient Health Questionnaire 9-item [PHQ-9]), remission (MADRS score ≤12; PHQ-9 total score <5), changes in depression rating scores (measured as mean change from baseline), and safety were evaluated (incidence of treatment-emergent and serious adverse events [AE])."( Efficacy and Safety of Esketamine Nasal Spray in Patients with Treatment-Resistant Depression Who Completed a Second Induction Period: Analysis of the Ongoing SUSTAIN-3 Study.
Al Jurdi, RK; Borentain, S; Brown, B; Cabrera, P; Castro, M; Fu, DJ; Petrillo, MP; Sun, L; Turkoz, I; Wilkinson, ST; Zaki, N, 2023
)
1.22
" Adverse reaction rates were similar between groups (P > ."( Analysis of the Analgesic Effect, Emotion, and Safety of Esketamine in Cesarean Section Analgesia for Puerperae.
Chen, H; Dong, X; Jin, L; Lou, F; Lu, Y; Wang, C; Yang, Z, 2023
)
1.16

Pharmacokinetics

Esketamine showed high bioavailability (62%) and relatively low maximum concentration peaks. A population pharmacokinetic (popPK) model of esketamine and its metabolite (noresketamine) was previously developed.

ExcerptReferenceRelevance
" Blood samples were collected for pharmacokinetic analysis."( Pharmacokinetics and Safety of Esketamine in Chinese Patients Undergoing Painless Gastroscopy in Comparison with Ketamine: A Randomized, Open-Label Clinical Study.
Cui, C; Huang, J; Pei, Q; Wang, J; Wang, SY; Yang, GP; Yang, S; Ye, L, 2019
)
0.8
"The model is of adequate quality for use in future pharmacokinetic and pharmacodynamic studies into the efficacy and side-effects of ketamine and metabolites."( Pharmacokinetics of ketamine and its major metabolites norketamine, hydroxynorketamine, and dehydronorketamine: a model-based analysis.
Aarts, L; Dahan, A; Jonkman, K; Kamp, J; Niesters, M; Olofsen, E; van Velzen, M, 2020
)
0.56
" Esketamine showed a clinically relevant pharmacokinetic profile, with high bioavailability (62%) and relatively low maximum concentration peaks."( Esketamine inhaled as dry powder: Pharmacokinetic, pharmacodynamic and safety assessment in a preclinical study.
Abramski, K; Dera, P; Gajos-Draus, A; Janicka, M; Janowska, S; Kamil, K; Mach, M; Matłoka, M; Moszczyński-Pętkowski, R; Pankiewicz, P; Perko, P; Pieczykolan, J; Teska-Kamińska, M; Tratkiewicz, E; Wieczorek, M; Ziółkowski, H, 2022
)
3.07
"The simulated and observed (171 healthy volunteers) plasma pharmacokinetic profiles of intranasal esketamine/noresketamine showed a good match."( Prediction of Drug-Drug Interactions After Esketamine Intranasal Administration Using a Physiologically Based Pharmacokinetic Model.
de Zwart, L; Mannens, G; Snoeys, J; Willemin, ME; Zannikos, P, 2022
)
1.2
" A population pharmacokinetic (popPK) model of esketamine and its metabolite (noresketamine) has been previously developed, which included Asian race and Japanese ethnicity as covariates on their exposures."( Evaluation of Ethnicity Effect on Intranasal Esketamine Pharmacokinetics by Population Pharmacokinetic Modeling Using Data From a Japanese Phase 2b Study.
Kurosawa, K; Pérez-Ruixo, C; Shibuya, M; Shimizu, H, 2023
)
1.43

Compound-Compound Interactions

Remimazolam combined with esketamine anesthesia has the sa. A subanesthetic dose of esketamines combined with hip capsule PNB for elderly patients undergoing THA has better postoperative analgesic effects.

ExcerptReferenceRelevance
" This study was designed to evaluate the feasibility and safety of sedation with inhaled sevoflurane in combination with intravenous esketamine during PP in patients with COVID-19-ARDS (CARDS)."( Sevoflurane in combination with esketamine is an effective sedation regimen in COVID-19 patients enabling assisted spontaneous breathing even during prone positioning.
Bansbach, J; Heinrich, S; Kalbhenn, J; Kaufmann, K; Wenz, J, 2022
)
1.21
" Patients were sedated with inhaled sevoflurane in combination with eske-tamine during PP and not or only lightly sedated during the supine position."( Sevoflurane in combination with esketamine is an effective sedation regimen in COVID-19 patients enabling assisted spontaneous breathing even during prone positioning.
Bansbach, J; Heinrich, S; Kalbhenn, J; Kaufmann, K; Wenz, J, 2022
)
1
" Inhaled sedation with sevoflurane in combination with esketamine, however, safely enables prolonged prone positioning in patients with CARDS."( Sevoflurane in combination with esketamine is an effective sedation regimen in COVID-19 patients enabling assisted spontaneous breathing even during prone positioning.
Bansbach, J; Heinrich, S; Kalbhenn, J; Kaufmann, K; Wenz, J, 2022
)
1.25
"The objective of this study was to determine which symptoms measured by the Patient Health Questionnaire (PHQ-9) and Montgomery-Asberg Depression Rating Scale (MADRS) improve in those treated with esketamine nasal spray in combination with oral antidepressant (AD) compared with those treated with placebo plus AD for adult patients with treatment-resistant depression (TRD)."( Evaluation of Individual Items of the Patient Health Questionnaire (PHQ-9) and Montgomery-Asberg Depression Rating Scale (MADRS) in Adults with Treatment-Resistant Depression Treated with Esketamine Nasal Spray Combined with a New Oral Antidepressant.
Cooper, K; Drevets, WC; Floden, L; Hudgens, S; Jamieson, C; Popova, V; Singh, J, 2022
)
1.1
"The TRANSFORM 2 study evaluated the efficacy and safety of esketamine nasal spray in combination with AD."( Evaluation of Individual Items of the Patient Health Questionnaire (PHQ-9) and Montgomery-Asberg Depression Rating Scale (MADRS) in Adults with Treatment-Resistant Depression Treated with Esketamine Nasal Spray Combined with a New Oral Antidepressant.
Cooper, K; Drevets, WC; Floden, L; Hudgens, S; Jamieson, C; Popova, V; Singh, J, 2022
)
1.16
" In antidepressant drug therapy, usually multiple drugs are administered which are substrates of CYP enzymes, increasing the risk for drug-drug interactions."( Pharmacogenetic and drug interaction aspects on ketamine safety in its use as antidepressant - implications for precision dosing in a global perspective.
Just, KS; Langmia, IM; Müller, JP; Stingl, JC; Yamoune, S, 2022
)
0.72
" Studies have shown that the application of propofol combined with ketamine in painless gastrointestinal endoscopy is beneficial to reduce the dosage of propofol and the incidence of related complications."( Efficacy and safety of subanesthetic doses of esketamine combined with propofol in painless gastrointestinal endoscopy: a prospective, double-blind, randomized controlled trial.
Li, J; Li, S; Li, Y; Liang, S; Liang, Z; Luo, Q; Yang, Z; Zhan, Y, 2022
)
0.98
"To investigate the effect of applying remimazolam combined with esketamine for anesthesia in painless gastroenteroscopy on patients' circulatory and respiratory function."( Effects of Remimazolam Combined with Esketamine Anesthesia on Circulatory and Respiratory Function during Painless Gastroenteroscopy.
Guo, X; Lu, C; Qian, J; Ren, J, 2022
)
1.23
"Remimazolam combined with esketamine anesthesia has the same advantages of rapid awakening compared with propofol anesthesia."( Effects of Remimazolam Combined with Esketamine Anesthesia on Circulatory and Respiratory Function during Painless Gastroenteroscopy.
Guo, X; Lu, C; Qian, J; Ren, J, 2022
)
1.29
"Propofol combined with opioids can reduce the dosage of propofol and improve the safety of endoscopy."( Sedative effect and safety of different doses of S-ketamine in combination with propofol during gastro-duodenoscopy in school-aged children: a prospective, randomized study.
Hu, W; Huang, X; Ren, W; Wang, J; Zhang, B; Zhao, X, 2022
)
0.72
"To explore the effects and safety of low dose of esketamine combined with propofol in elderly patients undergoing fibronchoscopy."( Low dose of esketamine combined with propofol in painless fibronchoscopy in elderly patients.
Chen, Z; Du, T; Feng, Y; Wang, J, 2022
)
1.35
"This is a protocol for a randomized double-blind controlled trial to evaluate the effect of esketamine combined with pregabalin on postsurgical pain in spinal surgery."( Esketamine combined with pregabalin on acute postoperative pain in patients undergoing resection of spinal neoplasms: study protocol for a randomized controlled trial.
Fan, J; Han, R; Sun, W; Wang, J; Wang, Y; Zhou, Y, 2023
)
2.57
"The aim of this study was to evaluate the effect of esketamine combined with pregabalin on acute postsurgical pain in patients undergoing resection of spinal neoplasms."( Esketamine combined with pregabalin on acute postoperative pain in patients undergoing resection of spinal neoplasms: study protocol for a randomized controlled trial.
Fan, J; Han, R; Sun, W; Wang, J; Wang, Y; Zhou, Y, 2023
)
2.6
" For children aged 2-6 years with dental anxiety who require dental surgery, anesthesiologists may consider using midazolam oral solution combined with esketamine nasal drops for noninvasive sedation after a preoperative anxiety scale evaluation."( Intranasal esketamine combined with oral midazolam provides adequate sedation for outpatient pediatric dental procedures: a prospective cohort study.
Chen, S; Chen, Z; Liao, J; Ran, H; Wang, J; Yu, C; Zeng, J; Zhao, N, 2023
)
1.5
" Low dose of remimazolam when combined with esketamine has favorable profiles with rapid onset and recovery, but mild hemodynamic side effects and adverse events."( Remimazolam versus propofol in combination with esketamine for surgical abortion: A double-blind randomized controlled trial.
Chen, J; Li, N; Ma, X; Wan, Z; Wang, J; Yang, L; Yue, L, 2023
)
1.43
" The effect of esketamine combined with other common anesthetics on IOP has been underinvestigated."( Effect of intravenous induction with different doses of Esketamine combined with propofol and sufentanil on intraocular pressure among pediatric strabismus surgery: a randomized clinical trial.
Luo, J; Sun, R; Yin, K; Zhang, Z; Zhao, D, 2023
)
1.51
"Propofol combined with sufentanil significantly decreased IOP during the induction of general anesthesia."( Effect of intravenous induction with different doses of Esketamine combined with propofol and sufentanil on intraocular pressure among pediatric strabismus surgery: a randomized clinical trial.
Luo, J; Sun, R; Yin, K; Zhang, Z; Zhao, D, 2023
)
1.16
"This study aims to observe the postoperative anesthetic effect of esketamine combined with hip capsule peripheral nerve block (PNB) in elderly patients undergoing total hip arthroplasty (THA)."( A subanesthetic dose of esketamine combined with hip peripheral nerve block has good sedative and analgesic effects in elderly patients undergoing total hip arthroplasty: A randomized-controlled trial.
Dai, B; Huo, Y, 2023
)
1.45
" The observation group (Group A) was treated with a subanesthetic dose of esketamine combined with hip capsule PNB; control group (Group B) was treated with a subanesthetic dose of esketamine combined with lumbar plexus block; and control group (Group C) was treated with a subanesthetic dose of esketamine for general anesthesia."( A subanesthetic dose of esketamine combined with hip peripheral nerve block has good sedative and analgesic effects in elderly patients undergoing total hip arthroplasty: A randomized-controlled trial.
Dai, B; Huo, Y, 2023
)
1.45
"A subanesthetic dose of esketamine combined with hip capsule PNB for elderly patients undergoing THA has better postoperative analgesic effects."( A subanesthetic dose of esketamine combined with hip peripheral nerve block has good sedative and analgesic effects in elderly patients undergoing total hip arthroplasty: A randomized-controlled trial.
Dai, B; Huo, Y, 2023
)
1.52

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
" Esketamine showed a clinically relevant pharmacokinetic profile, with high bioavailability (62%) and relatively low maximum concentration peaks."( Esketamine inhaled as dry powder: Pharmacokinetic, pharmacodynamic and safety assessment in a preclinical study.
Abramski, K; Dera, P; Gajos-Draus, A; Janicka, M; Janowska, S; Kamil, K; Mach, M; Matłoka, M; Moszczyński-Pętkowski, R; Pankiewicz, P; Perko, P; Pieczykolan, J; Teska-Kamińska, M; Tratkiewicz, E; Wieczorek, M; Ziółkowski, H, 2022
)
3.07

Dosage Studied

Esketamine is cheap, requires less frequent dosing (once a week), and is a simpler procedure compared to intravenous infusions. This study compared the efficacy and safety of switching patients with treatment-resistant depression from an ineffective antidepressant to flexibly dosed esketamine nasal spray plus a newly initiated antidepressant.

ExcerptRelevanceReference
"To assess the efficacy, safety, and dose-response of intranasal esketamine hydrochloride in patients with treatment-resistant depression (TRD)."( Efficacy and Safety of Intranasal Esketamine Adjunctive to Oral Antidepressant Therapy in Treatment-Resistant Depression: A Randomized Clinical Trial.
Cooper, K; Daly, EJ; Drevets, WC; Fedgchin, M; Lim, P; Manji, H; Shelton, RC; Singh, JB; Thase, ME; Van Nueten, L; Winokur, A, 2018
)
1
" During the open-label phase, dosing frequency was reduced from twice weekly to weekly, and then to every 2 weeks."( Efficacy and Safety of Intranasal Esketamine Adjunctive to Oral Antidepressant Therapy in Treatment-Resistant Depression: A Randomized Clinical Trial.
Cooper, K; Daly, EJ; Drevets, WC; Fedgchin, M; Lim, P; Manji, H; Shelton, RC; Singh, JB; Thase, ME; Van Nueten, L; Winokur, A, 2018
)
0.76
"001), with a significant ascending dose-response relationship (P < ."( Efficacy and Safety of Intranasal Esketamine Adjunctive to Oral Antidepressant Therapy in Treatment-Resistant Depression: A Randomized Clinical Trial.
Cooper, K; Daly, EJ; Drevets, WC; Fedgchin, M; Lim, P; Manji, H; Shelton, RC; Singh, JB; Thase, ME; Van Nueten, L; Winokur, A, 2018
)
0.76
" Response appeared to persist for more than 2 months with a lower dosing frequency."( Efficacy and Safety of Intranasal Esketamine Adjunctive to Oral Antidepressant Therapy in Treatment-Resistant Depression: A Randomized Clinical Trial.
Cooper, K; Daly, EJ; Drevets, WC; Fedgchin, M; Lim, P; Manji, H; Shelton, RC; Singh, JB; Thase, ME; Van Nueten, L; Winokur, A, 2018
)
0.76
" The site-based MADRS interviews were recorded at the baseline and 2 h post-dose assessments on the first intranasal dosing day."( Comparability of blinded remote and site-based assessments of response to adjunctive esketamine or placebo nasal spray in patients with treatment resistant depression.
Cooper, K; Daly, E; Fedgchin, M; Singh, JB; Targum, SD, 2019
)
0.74
" This study compared the efficacy and safety of switching patients with treatment-resistant depression from an ineffective antidepressant to flexibly dosed esketamine nasal spray plus a newly initiated antidepressant or to a newly initiated antidepressant (active comparator) plus placebo nasal spray."( Efficacy and Safety of Flexibly Dosed Esketamine Nasal Spray Combined With a Newly Initiated Oral Antidepressant in Treatment-Resistant Depression: A Randomized Double-Blind Active-Controlled Study.
Bajbouj, M; Cooper, K; Daly, EJ; Drevets, WC; Hough, D; Lane, R; Lim, P; Manji, H; Mazzucco, C; Molero, P; Popova, V; Shelton, RC; Singh, JB; Thase, ME; Trivedi, M; Vieta, E, 2019
)
0.98
"This phase 3 double-blind study randomized patients with treatment-resistant depression (TRD) ≥65 years (1:1) to flexibly dosed esketamine nasal spray and new oral antidepressant (esketamine/antidepressant) or new oral antidepressant and placebo nasal spray (antidepressant/placebo)."( Efficacy and Safety of Esketamine Nasal Spray Plus an Oral Antidepressant in Elderly Patients With Treatment-Resistant Depression-TRANSFORM-3.
Adler, C; Daly, EJ; Drevets, WC; Gaillard, R; Hough, D; Lane, R; Lim, P; Manji, H; McShane, R; Morrison, RL; Ochs-Ross, R; Sanacora, G; Singh, JB; Steffens, DC; Wilkinson, ST; Zhang, Y, 2020
)
1.07
" BP increases reached the maximum postdose value within ~ 40 min of esketamine dosing and returned to the predose range by ~ 1."( Cardiac Safety of Esketamine Nasal Spray in Treatment-Resistant Depression: Results from the Clinical Development Program.
Doherty, T; Melkote, R; Miller, J; Singh, JB; Wajs, E; Weber, MA, 2020
)
1.13
"BP elevations following esketamine dosing are generally transient, asymptomatic, and not associated with serious cardiovascular safety sequalae."( Cardiac Safety of Esketamine Nasal Spray in Treatment-Resistant Depression: Results from the Clinical Development Program.
Doherty, T; Melkote, R; Miller, J; Singh, JB; Wajs, E; Weber, MA, 2020
)
1.2
" However, IV administration is associated with a number of drawbacks and advanced delivery platforms could provide an alternative parenteral route of esketamine dosing in patients."( Hydrogel-forming microneedle arrays as a therapeutic option for transdermal esketamine delivery.
Courtenay, AJ; Donnelly, RF; Kearney, MC; Levin, G; Levy-Nissenbaum, E; McAlister, E; McCarthy, HO; McCrudden, MTC; Shterman, N; Steiner, L; Vora, L, 2020
)
0.99
" Most TEAEs occurred on dosing days, were mild or moderate in severity, and resolved on the same day."( Esketamine Nasal Spray Plus Oral Antidepressant in Patients With Treatment-Resistant Depression: Assessment of Long-Term Safety in a Phase 3, Open-Label Study (SUSTAIN-2).
Aluisio, L; Daly, EJ; Drevets, WC; George, JE; Grunfeld, J; Holder, R; Hough, D; Jeon, HJ; Kasper, S; Lane, R; Li, CT; Lim, P; Manji, H; Morrison, RL; Paik, JW; Sanacora, G; Singh, JB; Sulaiman, AH; Wajs, E; Wilkinson, ST; Young, AH, 2020
)
2
"This study aimed to estimate the cost-effectiveness of esketamine, a novel intranasally dosed antidepressant, for patients in the United States with treatment-resistant depression."( Cost-Effectiveness of Esketamine Nasal Spray for Patients With Treatment-Resistant Depression in the United States.
Ross, EL; Soeteman, DI, 2020
)
1.12
" esketamine is cheap, requires less frequent dosing (once a week), and is a simpler procedure compared to intravenous infusions, it might have an impact on public health."( Effects of subcutaneous esketamine on blood pressure and heart rate in treatment-resistant depression.
Abdo, G; Barbosa, M; Cohrs, FM; de Jesus Mari, J; Del Porto, JA; Del Sant, LC; Delfino, R; Fava, VAR; Lacerda, ALT; Liberatori, A; Lucchese, AC; Magalhães, EJM; Nakahira, C; Sarin, LM; Steiglich, MS; Surjan, J; Tuena, MA, 2020
)
1.78
"Intranasal drug delivery offers a non-invasive and convenient dosing option for patients and physicians, especially for conditions requiring chronic/repeated-treatment administration."( Effect of Esketamine Nasal Spray on Olfactory Function and Nasal Tolerability in Patients with Treatment-Resistant Depression: Results from Four Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase III Studies.
Cooper, K; Daly, E; Doty, RL; Drevets, WC; Fedgchin, M; Jamieson, C; Janik, A; Lane, R; Lim, P; Melkote, R; Ochs-Ross, R; Popova, V; Singh, J; Wylie, C, 2021
)
1.02
"Most trials of adding lithium involved older, mainly tricyclic, antidepressants, and the dosing of adjunctive treatments were not optimized."( Efficacy and Tolerability of Combination Treatments for Major Depression: Antidepressants plus Second-Generation Antipsychotics vs. Esketamine vs. Lithium.
Bahji, A; Baldessarini, RJ; Tondo, L; Undurraga, J; Vázquez, GH, 2021
)
0.83
" The dose-response relationship calls for caution with higher doses of tranylcypromine."( Cardiovascular Effects of Combining Subcutaneous or Intravenous Esketamine and the MAO Inhibitor Tranylcypromine for the Treatment of Depression: A Retrospective Cohort Study.
Bauer, M; Findeis, H; Ludwig, VM; Ritter, P; Rucker, J; Sauer, C; Young, AH, 2021
)
0.86
" Since then, intravenous ketamine and intranasal S-ketamine have been validated for the treatment of depression and suicidal ideation following dose-response and double-blind placebo-controlled clinical trials."( Key considerations for the use of ketamine and esketamine for the treatment of depression: focusing on administration, safety, and tolerability.
Kritzer, MD; Masand, PS; Pae, CU, 2022
)
0.98
"We recommend further investigation into treatment dosing and frequency strategies as well as approaches that prolong the therapeutic effects."( Key considerations for the use of ketamine and esketamine for the treatment of depression: focusing on administration, safety, and tolerability.
Kritzer, MD; Masand, PS; Pae, CU, 2022
)
0.98
" Dosage of propofol required in group E (1."( The effectiveness of esketamine and propofol versus dezocine and propofol sedation during gastroscopy: A randomized controlled study.
Chen, L; Tang, T; Xu, Y; Zhang, Y; Zhang, Z; Zheng, Y, 2022
)
1.04
" Therefore, taking a look at individual patient risks and potential underlying variability in pharmacokinetics may improve safety and dosing of these new antidepressant drugs in clinical practice."( Pharmacogenetic and drug interaction aspects on ketamine safety in its use as antidepressant - implications for precision dosing in a global perspective.
Just, KS; Langmia, IM; Müller, JP; Stingl, JC; Yamoune, S, 2022
)
0.72
" The secondary outcomes included injection pain score, vital signs, total dosage of vasoactive drugs used within 5 minutes after induction, and adverse events related to drugs."( Pretreatment with Low-Dose Esketamine for Reduction of Propofol Injection Pain: A Randomized Controlled Trial.
Fu, D; Han, Y; Jia, J; Li, W; Wang, D, 2022
)
1.02
" Studies have shown that the application of propofol combined with ketamine in painless gastrointestinal endoscopy is beneficial to reduce the dosage of propofol and the incidence of related complications."( Efficacy and safety of subanesthetic doses of esketamine combined with propofol in painless gastrointestinal endoscopy: a prospective, double-blind, randomized controlled trial.
Li, J; Li, S; Li, Y; Liang, S; Liang, Z; Luo, Q; Yang, Z; Zhan, Y, 2022
)
0.98
"Propofol combined with opioids can reduce the dosage of propofol and improve the safety of endoscopy."( Sedative effect and safety of different doses of S-ketamine in combination with propofol during gastro-duodenoscopy in school-aged children: a prospective, randomized study.
Hu, W; Huang, X; Ren, W; Wang, J; Zhang, B; Zhao, X, 2022
)
0.72
"Comparison of cumulated dosage of sufentanil, times of effective press and rescue analgesia at 48 hours after operation: Group H was significantly lower than Group M, Group L, and Group C (P < ."( Effects of esketamine on analgesia and postpartum depression after cesarean section: A randomized, double-blinded controlled trial.
Chen, Q; Ling, B; Lv, J; Wang, W; Xu, H; Yu, W, 2022
)
1.11
" Compared with the control group, the total dosage of propofol in the experimental group was significantly lower, and the number of vasoactive drugs, the incidence of respiratory depression and bronchospasm were significantly lower (P < ."( Low dose of esketamine combined with propofol in painless fibronchoscopy in elderly patients.
Chen, Z; Du, T; Feng, Y; Wang, J, 2022
)
1.1
"0035) and the dosage of propofol used during operation (198."( Evaluation of clinical effects of Esketamine on depression in patients with missed miscarriage: A randomized, controlled, double-blind trial.
Feng, S; Jiang, M; Li, Q; Mao, M; Wen, Y; Xu, C; Yuan, H; Zhou, R, 2023
)
1.19
"The majority of patients completed ESK induction phase, and most dosing intervals were longer than the label recommendation."( Treatment patterns, healthcare utilization, and costs of patients with treatment-resistant depression initiated on esketamine intranasal spray and covered by US commercial health plans.
Holiday, C; Joshi, K; Karkare, S; Pilon, D; Shah, A; Zhdanava, M,
)
0.34
"In this RCT, the primary objective is to demonstrate that an intermittent esketamine dosing regimen is non-inferior to a continuous esketamine dosing regimen at 3 months follow-up."( Intermittent versus continuous esketamine infusions for long-term pain modulation in complex regional pain syndrome: protocol of a randomized controlled non-inferiority study (KetCRPS-2).
Baart, SJ; Bharwani, KD; de Vos, CC; Dik, WA; Dirckx, M; Huygen, FJPM; Mangnus, TJP; Redekop, K; Siepman, TAM, 2023
)
1.43
" However, the proper dosage for intranasal use in children with congenital heart disease (CHD) has not been determined."( Median effective dose of esketamine for intranasal premedication in children with congenital heart disease.
Bai, J; Gu, H; Huang, J; Liu, D, 2023
)
1.21
"Data from TRANSFORM-2, a phase 3, randomized, double-blind, short-term flexibly dosed study, were analyzed."( Assessment of health-related quality of life and health status in patients with treatment-resistant depression treated with esketamine nasal spray plus an oral antidepressant.
Cooper, K; Daly, E; Drevets, WC; Jamieson, C; Popova, V; Rozjabek, HM; Singh, J, 2023
)
1.12
" Intranasal esketamine dosing was flexible, twice-weekly during induction and individualized to depression severity during optimization/maintenance."( Long-term safety and maintenance of response with esketamine nasal spray in participants with treatment-resistant depression: interim results of the SUSTAIN-3 study.
Chen, LN; Doherty, T; Drevets, WC; Fu, DJ; Lane, R; Morrison, RL; Popova, V; Sanacora, G; Wilkinson, ST; Zaki, N, 2023
)
1.54
" For propofol dosage, the administration of esketamine required a lower propofol dosage compared to the NS group and opioids group]."( Efficacy and safety of esketamine for sedation among patients undergoing gastrointestinal endoscopy: a systematic review and meta-analysis.
Guo, Y; Jing, Y; Lian, X; Lin, Y; Luo, T; Yuan, H, 2023
)
1.48
" The dosage of propofol in the PR group was significantly higher than that in the PK group (144 ± 38 mg vs."( Comparison of remifentanil and esketamine in combination with propofol for patient sedation during fiberoptic bronchoscopy.
Chen, W; Jia, Y; Nie, J; Wang, H; Zhang, Y, 2023
)
1.2
"Compared with remifentanil, the combination of esketamine with propofol in fiberoptic bronchoscopy leaded to more stable intraoperative hemodynamics, lower dosage of propofol, lower transient hypoxia rate, fewer incidence of adverse events, and greater bronchoscopists satisfaction."( Comparison of remifentanil and esketamine in combination with propofol for patient sedation during fiberoptic bronchoscopy.
Chen, W; Jia, Y; Nie, J; Wang, H; Zhang, Y, 2023
)
1.45
"The optimal dosage and method of esketamine for postpartum depressive symptoms (PDS) are unclear."( Effects of different doses of esketamine intervention on postpartum depressive symptoms in cesarean section women: A randomized, double-blind, controlled clinical study.
Bai, ZH; Chen, L; Duan, KM; Gao, K; Li, QW; Mao, XY; Ping, AQ; Wang, SY; Xu, SY; Yang, SQ; Yang, ST; Zhou, YY, 2023
)
1.48
" Secondary study indicators will include (1) visual analog scale (VAS) score and HAMD-17 score prior to surgery, immediately after entering the postanesthesia care unit (PACU) and 1, 2, 3, 4, and 5 days after surgery; (2) Richmond Agitation-Sedation Scale (RASS) score at 1, 2, 3, 4, and 5 days after surgery; (3) consumed doses of sufentanil and esketamine after surgery; (4) postoperative analgesia pump effective press times, rescue analgesia times, and rescue drug dosage, recording the number of rescue analgesia and rescue drug dosage at 6, 24, 48, and 72 h after the patient enters the PACU; (5) postoperative complications and adverse events; (6) postoperative hospital stay; (7) concentrations of brain-derived neurotrophic factor (BDNP), 5-hydroxytryptamine (5-HT), tumor necrosis factor (TNF-α) and interleukin-6, at 1, 3, and, 5 days post-surgery; and (8) the patient survival rate at 6 and 12 months post-surgery."( Effect of postoperative application of esketamine on postoperative depression and postoperative analgesia in patients undergoing pancreatoduodenectomy: a randomized controlled trial protocol.
Gan, S; Pan, Q; Song, Z; Yang, Q; Yang, S; Yin, Y; Yu, K; Zhang, B; Zuo, X, 2023
)
1.35
"The aim of this study is to assess the current situation in out of hospital pain management in Germany regarding the substances, indications, dosage and the delegation of the use of analgesics to emergency medical service (EMS) staff."( Application of analgesics in emergency services in Germany: a survey of the medical directors.
Scharonow, M; Scharonow, O; Vilcane, S; Weilbach, C, 2023
)
0.91
" The levels of interleukin-6 (IL-6), interleukin-8 (IL-8), C-reactive protein (CRP), procalcitonin, tumor necrosis factor-α (TNF-α), numeric rating scales, dosage of propofol, dexmedetomidine and rocuronium, as well as the numeric rating scales score and analgesic complications were monitored in the 2 groups."( Effect of esketamine on inflammatory factors in opioid-free anesthesia based on quadratus lumborum block: A randomized trial.
Dai, J; Li, J; Li, S; Zheng, R, 2023
)
1.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
analgesicAn agent capable of relieving pain without the loss of consciousness or without producing anaesthesia. In addition, analgesic is a role played by a compound which is exhibited by a capability to cause a reduction of pain symptoms.
NMDA receptor antagonistAny substance that inhibits the action of N-methyl-D-aspartate (NMDA) receptors. They tend to induce a state known as dissociative anesthesia, marked by catalepsy, amnesia, and analgesia, while side effects can include hallucinations, nightmares, and confusion. Due to their psychotomimetic effects, many NMDA receptor antagonists are used as recreational drugs.
intravenous anaestheticnull
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (1)

ClassDescription
ketamineA member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group.
[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 (9)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Glutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)Ki0.49500.00030.86666.6900AID1692782; AID1692783
Glutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)Ki0.49500.00030.68056.6900AID1692782; AID1692783
Glutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)Ki0.49500.00030.70716.6900AID1692782; AID1692783
Glutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)Ki0.49500.00030.81966.6900AID1692782; AID1692783
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)IC50 (µMol)0.01140.00101.88779.8000AID1255979
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)IC50 (µMol)0.01140.00101.99589.8000AID1255979
Glutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)Ki0.49500.00030.70726.6900AID1692782; AID1692783
Glutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)Ki0.49500.00030.70726.6900AID1692782; AID1692783
Glutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)Ki0.49500.00030.70726.6900AID1692782; AID1692783
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
cellular response to amyloid-betaGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
monoatomic cation transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
visual learningGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of calcium ion transport into cytosolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
propylene metabolic processGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of membrane potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of transcription by RNA polymerase IIGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
protein heterotetramerizationGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium ion homeostasisGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of reactive oxygen species biosynthetic processGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
response to glycineGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
cellular response to amyloid-betaGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
startle responseGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to amphetamineGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
brain developmentGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
learning or memoryGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
memoryGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
visual learningGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to xenobiotic stimulusGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to woundingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
sensory perception of painGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
calcium-mediated signalingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
neurogenesisGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
protein catabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
sleepGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
directional locomotionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
ionotropic glutamate receptor signaling pathwayGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
negative regulation of protein catabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
dopamine metabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
serotonin metabolic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of apoptotic processGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
response to ethanolGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of synaptic plasticityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of neuronal synaptic plasticityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
activation of cysteine-type endopeptidase activityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
calcium ion transmembrane import into cytosolGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
excitatory chemical synaptic transmissionGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
protein localization to postsynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
regulation of monoatomic cation transmembrane transportGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
positive regulation of excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic transmission, glutamatergicGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
excitatory postsynaptic potentialGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
long-term synaptic potentiationGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium channel activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
amyloid-beta bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calcium ion bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
protein bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
calmodulin bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
glycine bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
glutamate bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
protein-containing complex bindingGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
signaling receptor activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
ligand-gated monoatomic ion channel activityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
amyloid-beta bindingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
NMDA glutamate receptor activityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
protein bindingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
zinc ion bindingGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamate-gated calcium ion channel activityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
transmitter-gated monoatomic ion channel activity involved in regulation of postsynaptic membrane potentialGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (20)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 1 Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2A Rattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2CRattus norvegicus (Norway rat)
cytoplasmGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic vesicleGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
cell surfaceGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
postsynaptic densityGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
dendriteGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic cleftGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
terminal boutonGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
dendritic spineGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
excitatory synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synaptic membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
synapseGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
neuron projectionGlutamate receptor ionotropic, NMDA 1Homo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic vesicleGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
cell surfaceGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic densityGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
NMDA selective glutamate receptor complexGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
cytoplasmic vesicle membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
presynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
dendritic spineGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
synaptic membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
glutamatergic synapseGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
plasma membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
postsynaptic density membraneGlutamate receptor ionotropic, NMDA 2AHomo sapiens (human)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 2DRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3BRattus norvegicus (Norway rat)
endoplasmic reticulum membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
plasma membraneGlutamate receptor ionotropic, NMDA 3ARattus norvegicus (Norway rat)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (23)

Assay IDTitleYearJournalArticle
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
AID704017Displacement of [3H]-(+)-MK-801 from PCP binding site of NMDA receptor in pig brain cortex2012Journal of medicinal chemistry, Oct-25, Volume: 55, Issue:20
Enantiomerically pure 1,3-dioxanes as highly selective NMDA and σ₁ receptor ligands.
AID1247113Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 20 mM NH4+ to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 20 mM NH4+2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1247108Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 30 uM spermine to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 30 uM spermine2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1255979Antagonist activity against NR1-1a/NR2A NMDA receptor (unknown origin) expressed in mouse recombinant L(tk-) cells assessed as inhibition of glycine and glutamate induced excitotoxicity incubated for 12 hrs by LDH assay2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.
AID1247112Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 50 mM K+ to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 50 mM K+2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1692782Displacement of [3H]-MK801 from NMDA receptor in rat brain homogenate2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Repurposing of Drugs-The Ketamine Story.
AID1247111Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 3 to 50 mM Na+ to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 3 to 50 mM Na+2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1672601Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by SRB assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Role of the NMDA Receptor in the Antitumor Activity of Chiral 1,4-Dioxane Ligands in MCF-7 and SKBR3 Breast Cancer Cells.
AID1672602Cytotoxicity against human SK-BR-3 cells assessed as reduction in cell viability incubated for 48 hrs by SRB assay2019ACS medicinal chemistry letters, Apr-11, Volume: 10, Issue:4
Role of the NMDA Receptor in the Antitumor Activity of Chiral 1,4-Dioxane Ligands in MCF-7 and SKBR3 Breast Cancer Cells.
AID1247110Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of H+ at pH 6.4 to 8.2 to IC50 for NMDA receptor in Wistar rat brain membranes in absence of H+ at pH 6.4 to 8.22015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID353104Ratio of Ki for rat brain NMDA receptor in presence of 100 uM spermine to Ki for rat brain NMDA receptor in absence of spermine2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
NMDA receptor affinities of 1,2-diphenylethylamine and 1-(1,2-diphenylethyl)piperidine enantiomers and of related compounds.
AID1247114Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 1.3 mM Mg2+ to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 1.3 mM Mg2+2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1247109Ratio of IC50 for NMDA receptor in Wistar rat brain membranes in presence of 10 to 50 mM Tris to IC50 for NMDA receptor in Wistar rat brain membranes in absence of 10 to 50 mM Tris2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID1255978Displacement of [3H]MK801 from NMDA receptor PCP binding site in guinea pig brain cortex membranes incubated for 120 mins by scintillation counting method2015Journal of medicinal chemistry, Nov-12, Volume: 58, Issue:21
Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.
AID353103Displacement of [3H]MK801 from NMDA receptor in rat brain neuronal membrane2009Bioorganic & medicinal chemistry, May-01, Volume: 17, Issue:9
NMDA receptor affinities of 1,2-diphenylethylamine and 1-(1,2-diphenylethyl)piperidine enantiomers and of related compounds.
AID1247107Displacement of [3H]MK-801 from NMDA receptor in Wistar rat brain membranes by scintillation counting analysis2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
AID295934Displacement of [3H]MK-801 from NMDA receptor in guinea pig brain membrane2007European journal of medicinal chemistry, Oct, Volume: 42, Issue:10
Synthesis of bridged piperazines with sigma receptor affinity.
AID1692776Cmax in mouse brain at 10 mg/kg, ip measured after 10 mins2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Repurposing of Drugs-The Ketamine Story.
AID1692783Displacement of [3H]-MK801 from NMDA receptor in rat brain membranes2020Journal of medicinal chemistry, 11-25, Volume: 63, Issue:22
Repurposing of Drugs-The Ketamine Story.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (417)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (0.48)29.6817
2010's47 (11.27)24.3611
2020's368 (88.25)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 86.41

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 Index86.41 (24.57)
Research Supply Index6.34 (2.92)
Research Growth Index6.91 (4.65)
Search Engine Demand Index167.01 (26.88)
Search Engine Supply Index2.22 (0.95)

This Compound (86.41)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials131 (30.25%)5.53%
Reviews79 (18.24%)6.00%
Case Studies16 (3.70%)4.05%
Observational10 (2.31%)0.25%
Other197 (45.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]