PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 25533960-3 2015 The human OX2 receptor (OX2R) belongs to the beta branch of the rhodopsin family of GPCRs, and can bind to diverse compounds including the native agonist peptides orexin-A and orexin-B and the potent therapeutic inhibitor suvorexant. suvorexant 222-232 hypocretin receptor 2 Homo sapiens 10-22 25969666-0 2015 Suvorexant: The first orexin receptor antagonist to treat insomnia. suvorexant 0-10 hypocretin neuropeptide precursor Homo sapiens 22-28 25969666-2 2015 A novel approach to treat insomnia has been introduced recently, with the approval of suvorexant, the first in a new class of orexin receptor antagonists. suvorexant 86-96 hypocretin neuropeptide precursor Homo sapiens 126-132 25533960-3 2015 The human OX2 receptor (OX2R) belongs to the beta branch of the rhodopsin family of GPCRs, and can bind to diverse compounds including the native agonist peptides orexin-A and orexin-B and the potent therapeutic inhibitor suvorexant. suvorexant 222-232 hypocretin receptor 2 Homo sapiens 24-28 25291725-1 2014 Suvorexant is a pharmacologically novel dual antagonist of orexin receptors OX1R and OX2R, which has an effect that promotes sleep by reducing arousal and wakefulness. suvorexant 0-10 hypocretin receptor 1 Homo sapiens 76-80 25397996-3 2015 Suvorexant helps in decreasing wakefulness by counteracting orexin activity. suvorexant 0-10 hypocretin neuropeptide precursor Homo sapiens 60-66 25227290-1 2014 Suvorexant (Belsomra( )), a first-in-class, orally active dual orexin-1 receptor and orexin-2 receptor antagonist, has been developed by Merck for the treatment of insomnia. suvorexant 0-10 hypocretin neuropeptide precursor Homo sapiens 63-69 25227290-1 2014 Suvorexant (Belsomra( )), a first-in-class, orally active dual orexin-1 receptor and orexin-2 receptor antagonist, has been developed by Merck for the treatment of insomnia. suvorexant 0-10 hypocretin neuropeptide precursor Homo sapiens 85-91 25291725-1 2014 Suvorexant is a pharmacologically novel dual antagonist of orexin receptors OX1R and OX2R, which has an effect that promotes sleep by reducing arousal and wakefulness. suvorexant 0-10 hypocretin receptor 2 Homo sapiens 85-89 23359095-6 2013 Indeed, phase III clinical trials were completed last year of suvorexant, a non-selective (dual) antagonist for orexin receptors, for the treatment of primary insomnia, and demonstrate promising results. suvorexant 62-72 hypocretin neuropeptide precursor Homo sapiens 112-118 25197807-1 2014 STUDY OBJECTIVES: Suvorexant, an orexin receptor antagonist, improves sleep in healthy subjects (HS) and patients with insomnia. suvorexant 18-28 hypocretin neuropeptide precursor Homo sapiens 33-39 24680372-1 2014 BACKGROUND: Suvorexant (MK-4305) is an orexin receptor antagonist shown to be efficacious for insomnia over 3 months. suvorexant 12-22 hypocretin neuropeptide precursor Homo sapiens 39-45 24680372-1 2014 BACKGROUND: Suvorexant (MK-4305) is an orexin receptor antagonist shown to be efficacious for insomnia over 3 months. suvorexant 24-31 hypocretin neuropeptide precursor Homo sapiens 39-45 24592206-3 2014 The filing to FDA of the dual-activity orexin receptor antagonist (DORA) suvorexant for the indication of insomnia further corroborates the robustness of such evidences. suvorexant 73-83 hypocretin neuropeptide precursor Homo sapiens 39-45 23382047-7 2013 These results establish that p38 signaling is critical for SUV-induced skin carcinogenesis. suvorexant 59-62 mitogen-activated protein kinase 14 Mus musculus 29-32 23024835-1 2012 Suvorexant is a dual orexin antagonist currently in Phase III clinical trials for the modulation of sleep and is being developed by Merck. suvorexant 0-10 hypocretin neuropeptide precursor Homo sapiens 21-27 22725839-1 2012 A concise, enantioselective synthesis of the potent dual orexin inhibitor suvorexant (1) is reported. suvorexant 74-84 hypocretin neuropeptide precursor Homo sapiens 57-63 22920041-4 2012 Merck"s suvorexant (MK-4305) is the first compound of the so-called dual orexin receptor antagonist (DORA) class expected to be submitted for FDA approval, with a new drug application anticipated in 2012. suvorexant 8-18 hypocretin neuropeptide precursor Homo sapiens 73-79 22920041-4 2012 Merck"s suvorexant (MK-4305) is the first compound of the so-called dual orexin receptor antagonist (DORA) class expected to be submitted for FDA approval, with a new drug application anticipated in 2012. suvorexant 20-27 hypocretin neuropeptide precursor Homo sapiens 73-79 21528938-0 2011 Reaction development and mechanistic study of a ruthenium catalyzed intramolecular asymmetric reductive amination en route to the dual Orexin inhibitor Suvorexant (MK-4305). suvorexant 152-162 hypocretin neuropeptide precursor Homo sapiens 135-141 21528938-0 2011 Reaction development and mechanistic study of a ruthenium catalyzed intramolecular asymmetric reductive amination en route to the dual Orexin inhibitor Suvorexant (MK-4305). suvorexant 164-171 hypocretin neuropeptide precursor Homo sapiens 135-141 21528938-1 2011 The first example of an intramolecular asymmetric reductive amination of a dialkyl ketone with an aliphatic amine has been developed for the synthesis of Suvorexant (MK-4305), a potent dual Orexin antagonist under development for the treatment of sleep disorders. suvorexant 154-164 hypocretin neuropeptide precursor Homo sapiens 190-196 21528938-1 2011 The first example of an intramolecular asymmetric reductive amination of a dialkyl ketone with an aliphatic amine has been developed for the synthesis of Suvorexant (MK-4305), a potent dual Orexin antagonist under development for the treatment of sleep disorders. suvorexant 166-173 hypocretin neuropeptide precursor Homo sapiens 190-196 34497544-3 2021 The present study examined the utility of magnetic resonance spectroscopy (MRS) for detecting neural and/or glial changes in the VTA to distinguish responders from non-responders before treatment with the orexin receptor antagonist suvorexant. suvorexant 232-242 hypocretin neuropeptide precursor Homo sapiens 205-211 21473737-4 2011 Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX(1)R and OX(2)R currently under clinical investigation as a novel therapy for insomnia. suvorexant 0-10 hypocretin receptor 1 Rattus norvegicus 83-89 21473737-4 2011 Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX(1)R and OX(2)R currently under clinical investigation as a novel therapy for insomnia. suvorexant 0-10 hypocretin receptor 2 Rattus norvegicus 94-100 21473737-4 2011 Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX(1)R and OX(2)R currently under clinical investigation as a novel therapy for insomnia. suvorexant 12-19 hypocretin receptor 1 Rattus norvegicus 83-89 21473737-4 2011 Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX(1)R and OX(2)R currently under clinical investigation as a novel therapy for insomnia. suvorexant 12-19 hypocretin receptor 2 Rattus norvegicus 94-100 34933185-5 2021 We, therefore, examined whether a dual orexin receptor antagonist, suvorexant, administered following evening exposure sessions, would enhance their therapeutic effectiveness for PTSD. suvorexant 67-77 hypocretin neuropeptide precursor Homo sapiens 39-45 32669442-3 2020 The nonselective orexin receptor antagonist suvorexant has been the first drug on the market targeting the orexin system and is prescribed for the treatment of insomnia. suvorexant 44-54 hypocretin neuropeptide precursor Homo sapiens 17-23 34989064-6 2022 The non-selective OX1 - and OX2 -receptor antagonist MK-4305 (suvorexant, 500.0 pg, 2.5 and 5.0 ng) enhanced dopamine efflux. suvorexant 53-60 CD200 receptor 1 Rattus norvegicus 28-41 34989064-7 2022 A 2-h tetrodotoxin infusion into nucleus accumbens through the probe or co-administration of orexin-A (500.0 pg) strongly inhibited MK-4305 (5.0 ng)-induced accumbal dopamine efflux. suvorexant 132-139 hypocretin neuropeptide precursor Rattus norvegicus 93-101 33609365-3 2021 The orexin receptor antagonist suvorexant promotes sleep by blocking both OX1R and OX2R. suvorexant 31-41 hypocretin (orexin) receptor 1 Mus musculus 74-78 33609365-3 2021 The orexin receptor antagonist suvorexant promotes sleep by blocking both OX1R and OX2R. suvorexant 31-41 hypocretin (orexin) receptor 2 Mus musculus 83-87 35022783-2 2022 We tested the efficacy of the dual orexin receptor antagonist suvorexant for chronic insomnia related to nighttime VMS. suvorexant 62-72 hypocretin neuropeptide precursor Homo sapiens 35-41 33212086-14 2021 Additionally, suvorexant ameliorated the extrahypothalamic induced upregulation of CRH-R1 in SRS-exposed rats. suvorexant 14-24 corticotropin releasing hormone receptor 1 Rattus norvegicus 83-89 30810914-2 2019 As suvorexant is metabolized primarily by Cytochrome P450 3A (CYP3A), and its pharmacokinetics may be affected by CYP3A modulators, the effects of CYP3A inhibitors (ketoconazole or diltiazem) or an inducer (rifampin [rifampicin]) on the pharmacokinetics, safety, and tolerability of suvorexant were investigated. suvorexant 3-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-60 32224066-3 2020 Our recent research revealed that suvorexant, a dual orexin receptor antagonist, could improve behavioral circadian rhythm disorders in 9-month-old APP/PS1 mice. suvorexant 34-44 hypocretin neuropeptide precursor Homo sapiens 53-59 32224066-3 2020 Our recent research revealed that suvorexant, a dual orexin receptor antagonist, could improve behavioral circadian rhythm disorders in 9-month-old APP/PS1 mice. suvorexant 34-44 presenilin 1 Mus musculus 152-155 32224066-4 2020 Here we further observed whether suvorexant could ameliorate the cognitive decline in APP/PS1 mice by using behavioral tests, and investigated the possible mechanisms by in vivo electrophysiological recording, western blot, and immunochemistry. suvorexant 33-43 presenilin 1 Mus musculus 90-93 33224245-0 2020 Suvorexant, a Dual Orexin Receptor Antagonist, Protected Seizure through Interaction with GABAA and Glutamate Receptors. suvorexant 0-10 hypocretin Mus musculus 19-25 33224245-0 2020 Suvorexant, a Dual Orexin Receptor Antagonist, Protected Seizure through Interaction with GABAA and Glutamate Receptors. suvorexant 0-10 gamma-aminobutyric acid (GABA) A receptor, subunit gamma 1 Mus musculus 90-95 31845549-12 2020 The OX1 and OX2 receptor antagonist MK-4305 and OX2 receptor antagonist EMPA, but not the OX1 receptor antagonist SB 334867, each counteracted orexin-A-induced inhibition of KCl-provoked increases in relative fluorescence intensity. suvorexant 36-43 CD200 receptor 1 Rattus norvegicus 12-24 31845549-12 2020 The OX1 and OX2 receptor antagonist MK-4305 and OX2 receptor antagonist EMPA, but not the OX1 receptor antagonist SB 334867, each counteracted orexin-A-induced inhibition of KCl-provoked increases in relative fluorescence intensity. suvorexant 36-43 hypocretin neuropeptide precursor Rattus norvegicus 143-151 30810914-2 2019 As suvorexant is metabolized primarily by Cytochrome P450 3A (CYP3A), and its pharmacokinetics may be affected by CYP3A modulators, the effects of CYP3A inhibitors (ketoconazole or diltiazem) or an inducer (rifampin [rifampicin]) on the pharmacokinetics, safety, and tolerability of suvorexant were investigated. suvorexant 3-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-67 30810914-2 2019 As suvorexant is metabolized primarily by Cytochrome P450 3A (CYP3A), and its pharmacokinetics may be affected by CYP3A modulators, the effects of CYP3A inhibitors (ketoconazole or diltiazem) or an inducer (rifampin [rifampicin]) on the pharmacokinetics, safety, and tolerability of suvorexant were investigated. suvorexant 3-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-119 30810914-2 2019 As suvorexant is metabolized primarily by Cytochrome P450 3A (CYP3A), and its pharmacokinetics may be affected by CYP3A modulators, the effects of CYP3A inhibitors (ketoconazole or diltiazem) or an inducer (rifampin [rifampicin]) on the pharmacokinetics, safety, and tolerability of suvorexant were investigated. suvorexant 3-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-119 30905886-3 2019 The orexin receptor antagonist suvorexant, which specifically block the endogenous waking system, has been approved as a new drug to treat insomnia. suvorexant 31-41 hypocretin Mus musculus 4-10 30895461-0 2019 Correction to: Effect of CYP3A Inhibition and Induction on the Pharmacokinetics of Suvorexant: Two Phase I, Open-Label, Fixed-Sequence Trials in Healthy Subjects. suvorexant 83-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 25-30 28419646-0 2018 Suvorexant, an orexin/hypocretin receptor antagonist, attenuates motivational and hedonic properties of cocaine. suvorexant 0-10 hypocretin neuropeptide precursor Rattus norvegicus 15-21 30619717-2 2019 We investigated suvorexant (an anti-insomnia drug that targets the orexin system) effects on sleep architecture and glucose metabolism in T2DM patients with insomnia. suvorexant 16-26 hypocretin neuropeptide precursor Homo sapiens 67-73 29289556-8 2018 Hyper-activation of the orexin system also causes sleep disturbances, such as insomnia, and hence, suvorexant, an orexin receptor antagonist, has been clinically used to treat insomnia. suvorexant 99-109 hypocretin neuropeptide precursor Homo sapiens 24-30 29289556-8 2018 Hyper-activation of the orexin system also causes sleep disturbances, such as insomnia, and hence, suvorexant, an orexin receptor antagonist, has been clinically used to treat insomnia. suvorexant 99-109 hypocretin neuropeptide precursor Homo sapiens 114-120 29450984-4 2018 By comparison with the wild type of OX2 R, the results show the 1,2,3-triazole and p-toluamide groups of suvorexant are changed in the N324A mutant of OX2 R during 200 ns MD simulations. suvorexant 105-115 hypocretin receptor 2 Homo sapiens 36-41 29450984-4 2018 By comparison with the wild type of OX2 R, the results show the 1,2,3-triazole and p-toluamide groups of suvorexant are changed in the N324A mutant of OX2 R during 200 ns MD simulations. suvorexant 105-115 hypocretin receptor 2 Homo sapiens 151-156 29450984-5 2018 The QM/MM and weak interaction analysis are employed to calculate the non-covalent bonds interaction between suvorexant and key residues in the wild type and N324A mutant of OX2 R. suvorexant 109-119 hypocretin receptor 2 Homo sapiens 174-179 28741623-0 2018 Effects of Suvorexant, a Dual Orexin/Hypocretin Receptor Antagonist, on Impulsive Behavior Associated with Cocaine. suvorexant 11-21 hypocretin neuropeptide precursor Rattus norvegicus 30-36 28741623-7 2018 Suvorexant, a dual (OX1/2R) orexin receptor antagonist, reduced cocaine-evoked premature responses in 5-CSRTT when administered systemically or directly into VTA. suvorexant 0-10 hypocretin neuropeptide precursor Rattus norvegicus 28-34 28741623-9 2018 Finally, suvorexant did not alter Fos-immunoreactivity within tyrosine hydroxylase-immunolabeled neurons of VTA, but did attenuate cocaine- and orexin-induced increases in calcium transient amplitude within neurons of VTA. suvorexant 9-19 hypocretin neuropeptide precursor Rattus norvegicus 144-150 28419646-3 2018 Suvorexant, a dual orexin receptor antagonist, recently received approval from the US Food and Drug Administration to treat insomnia. suvorexant 0-10 hypocretin neuropeptide precursor Rattus norvegicus 19-25 28993579-9 2017 The OX1 and OX2 receptor antagonist MK-4305, but not the OX1 receptor antagonist SB334867, counteracted the effects of orexin-A on the KCl-induced increase in F/F0. suvorexant 36-43 CD200 receptor 1 Rattus norvegicus 12-24 28993579-9 2017 The OX1 and OX2 receptor antagonist MK-4305, but not the OX1 receptor antagonist SB334867, counteracted the effects of orexin-A on the KCl-induced increase in F/F0. suvorexant 36-43 hypocretin neuropeptide precursor Rattus norvegicus 119-127 28212694-0 2017 Suvorexant-Induced Dream Enactment Behavior in Parkinson Disease: A Case Report. suvorexant 0-10 potassium voltage-gated channel interacting protein 3 Homo sapiens 19-24 28447885-9 2017 Last, administration of the dual orexin receptor antagonist, suvorexant, during the initial 24 h post-resuscitation, led to sustained neurological deficits. suvorexant 61-71 hypocretin neuropeptide precursor Rattus norvegicus 33-39 28994603-4 2017 By blocking orexin receptors, suvorexant induces sleep. suvorexant 30-40 hypocretin neuropeptide precursor Homo sapiens 12-18 28945327-0 2017 Suvorexant as an orexin antagonist may regulate serum glucose levels in psychiatric patients with insomnia. suvorexant 0-10 hypocretin neuropeptide precursor Homo sapiens 17-23 28778226-3 2017 Although hypocretin receptor antagonists have been developed as sleep-inducing drugs, a high dose of suvorexant, a hypocretin receptor antagonist, inhibits gene expression of prepro-hypocretin to induce narcoleptic attack in wild-type mice. suvorexant 101-111 hypocretin Mus musculus 9-19 28778226-3 2017 Although hypocretin receptor antagonists have been developed as sleep-inducing drugs, a high dose of suvorexant, a hypocretin receptor antagonist, inhibits gene expression of prepro-hypocretin to induce narcoleptic attack in wild-type mice. suvorexant 101-111 hypocretin Mus musculus 115-125 28778226-3 2017 Although hypocretin receptor antagonists have been developed as sleep-inducing drugs, a high dose of suvorexant, a hypocretin receptor antagonist, inhibits gene expression of prepro-hypocretin to induce narcoleptic attack in wild-type mice. suvorexant 101-111 hypocretin Mus musculus 115-125 28584695-0 2017 Neuroendocrine, Autonomic, and Metabolic Responses to an Orexin Antagonist, Suvorexant, in Psychiatric Patients with Insomnia. suvorexant 76-86 hypocretin neuropeptide precursor Homo sapiens 57-63 27860547-0 2017 The Discovery of Suvorexant, the First Orexin Receptor Drug for Insomnia. suvorexant 17-27 hypocretin neuropeptide precursor Homo sapiens 39-45 27909991-6 2017 The orexin (hypocretin) neuropeptide system is an attractive target, given the recent FDA and PMDA approval of suvorexant for the treatment of insomnia. suvorexant 111-121 hypocretin neuropeptide precursor Homo sapiens 4-10 26864332-2 2016 Suvorexant (MK-4305, Belsomra ) is a first-in-class dual orexin receptor antagonist approved in the USA and Japan for the treatment of insomnia. suvorexant 0-10 hypocretin neuropeptide precursor Homo sapiens 57-63 27631554-2 2016 To investigate this possibility, we here examined the effects of suvorexant, an antiinsomnia drug targeting the orexin system, on sleep and glucose metabolism in type 2 diabetic mice. suvorexant 65-75 hypocretin Mus musculus 112-118 27390287-1 2016 Starting from suvorexant (trade name Belsomra), we successfully identified interesting templates leading to potent dual orexin receptor antagonists (DORAs) via a scaffold-hopping approach. suvorexant 14-24 hypocretin neuropeptide precursor Homo sapiens 120-126 26864332-2 2016 Suvorexant (MK-4305, Belsomra ) is a first-in-class dual orexin receptor antagonist approved in the USA and Japan for the treatment of insomnia. suvorexant 12-19 hypocretin neuropeptide precursor Homo sapiens 57-63 26864332-12 2016 In vitro, suvorexant demonstrated reversible inhibition of CYP3A4 and 2C19 (IC50 ~ 4-5 muM), and weak time-dependent inhibition of CYP3A4 (KI = 12 muM, kinact = 0.14 min(-1)). suvorexant 10-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-74 26864332-12 2016 In vitro, suvorexant demonstrated reversible inhibition of CYP3A4 and 2C19 (IC50 ~ 4-5 muM), and weak time-dependent inhibition of CYP3A4 (KI = 12 muM, kinact = 0.14 min(-1)). suvorexant 10-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-65 26864332-13 2016 Suvorexant was also a weak inducer of CYP3A4, 1A2 and 2B6. suvorexant 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 27191770-8 2016 DISCUSSION: Because suvorexant is metabolized by CYP3A4, next-day somnolence could have occurred as a result of increased plasma suvorexant concentration due to CYP3A4 inhibition by diltiazem. suvorexant 20-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-55 27191770-8 2016 DISCUSSION: Because suvorexant is metabolized by CYP3A4, next-day somnolence could have occurred as a result of increased plasma suvorexant concentration due to CYP3A4 inhibition by diltiazem. suvorexant 20-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-167 27191770-8 2016 DISCUSSION: Because suvorexant is metabolized by CYP3A4, next-day somnolence could have occurred as a result of increased plasma suvorexant concentration due to CYP3A4 inhibition by diltiazem. suvorexant 129-139 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-167 26648692-5 2015 Suvorexant is metabolized by the hepatic CYP3A system and should be avoided in combination with strong CYP3A inhibitors. suvorexant 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-46 26317591-5 2016 The work described herein culminated in the 2014 FDA approval of suvorexant as a first-in-class dual orexin receptor antagonist for the treatment of insomnia. suvorexant 65-75 hypocretin neuropeptide precursor Homo sapiens 101-107 27253658-0 2016 Assessment of the Abuse Potential of the Orexin Receptor Antagonist, Suvorexant, Compared With Zolpidem in a Randomized Crossover Study. suvorexant 69-79 hypocretin neuropeptide precursor Homo sapiens 41-47 27253658-1 2016 Suvorexant is a dual orexin receptor antagonist approved in the United States and Japan for the treatment of insomnia at a maximum dose of 20 mg. suvorexant 0-10 hypocretin neuropeptide precursor Homo sapiens 21-27 26950369-3 2016 We determined structures of hOX1R bound to the OX1R-selective antagonist SB-674042 and the dual antagonist suvorexant at 2.8-A and 2.75-A resolution, respectively, and used molecular modeling to illuminate mechanisms of antagonist subtype selectivity between hOX1R and hOX2R. suvorexant 107-117 hypocretin receptor 1 Homo sapiens 28-33 26950369-3 2016 We determined structures of hOX1R bound to the OX1R-selective antagonist SB-674042 and the dual antagonist suvorexant at 2.8-A and 2.75-A resolution, respectively, and used molecular modeling to illuminate mechanisms of antagonist subtype selectivity between hOX1R and hOX2R. suvorexant 107-117 hypocretin receptor 1 Homo sapiens 29-33 26648692-5 2015 Suvorexant is metabolized by the hepatic CYP3A system and should be avoided in combination with strong CYP3A inhibitors. suvorexant 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-108