(Q28304842)

English

Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia

scientific article

Discovery of 5′′-Chloro- N -[(5,6-dimethoxypyridin-2-yl)methyl]-2,2′:5′,3′′-terpyridine-3′-carboxamide (MK-1064): A Selective Orexin 2 Receptor Antagonist (2-SORA) for the Treatment of Insomnia

In more languages

Statements

scholarly article

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia (English)

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

0 references

Christopher Winrow

21

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

author name string

Anthony J Roecker

1

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Swati P Mercer

2

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

John D Schreier

3

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Christopher D Cox

4

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Mark E Fraley

5

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Justin T Steen

6

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Wei Lemaire

7

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Joseph G Bruno

8

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

C Meacham Harrell

9

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Susan L Garson

10

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Anthony L Gotter

11

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Steven V Fox

12

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Joanne Stevens

13

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Pamela L Tannenbaum

14

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Thomayant Prueksaritanont

15

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Tamara D Cabalu

16

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Donghui Cui

17

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Joyce Stellabott

18

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

George D Hartman

19

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Steven D Young

20

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

John J Renger

22

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Paul J Coleman

23

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

language of work or name

0 references

publication date

27 December 2013

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

9

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

2

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

311-322

2 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

Diagnosis and treatment of insomnia

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Zolpidem-induced sleep-related behavioural disorders

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Overview of experimental and conventional pharmacological approaches in the treatment of sleep and wake disorders

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Zolpidem and driving impairment--identifying persons at risk

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Narcolepsy in orexin knockout mice: molecular genetics of sleep regulation

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Distinct narcolepsy syndromes in Orexin receptor-2 and Orexin null mice: molecular genetic dissection of Non-REM and REM sleep regulatory processes

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

The sleep disorder canine narcolepsy is caused by a mutation in the hypocretin (orexin) receptor 2 gene

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Reduced number of hypocretin neurons in human narcolepsy

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Concomitant loss of dynorphin, NARP, and orexin in narcolepsy

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Narp immunostaining of human hypocretin (orexin) neurons: loss in narcolepsy

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

International Union of Basic and Clinical Pharmacology. LXXXVI. Orexin receptor function, nomenclature and pharmacology

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexin receptors as therapeutic drug targets

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexin receptors: pharmacology and therapeutic opportunities

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Connectomics of orexin-producing neurons: interface of systems of emotion, energy homeostasis and arousal

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Hypocretin antagonists in insomnia treatment and beyond

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

The brain hypocretins and their receptors: mediators of allostatic arousal.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexins/hypocretins: pain regulation and cellular actions

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Hypocretin and its emerging role as a target for treatment of sleep disorders

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Selective stimulation of orexin receptor type 2 promotes wakefulness in freely behaving rats.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Proline bis-amides as potent dual orexin receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexin receptor antagonists differ from standard sleep drugs by promoting sleep at doses that do not disrupt cognition

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Promotion of sleep by targeting the orexin system in rats, dogs and humans

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexin receptor antagonism, a new sleep-enabling paradigm: a proof-of-concept clinical trial.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Elucidation of the metabolic pathways and the resulting multiple metabolites of almorexant, a dual orexin receptor antagonist, in humans

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Pharmacokinetic interactions of almorexant with midazolam and simvastatin, two CYP3A4 model substrates, in healthy male subjects

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Disposition and metabolism of [14C]SB-649868, an orexin 1 and 2 receptor antagonist, in humans

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexin receptor antagonists: a new concept in CNS disorders?

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexin receptor antagonists: a review of promising compounds patented since 2006.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexin receptor antagonists: medicinal chemistry and therapeutic potential

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Discovery of dual orexin receptor antagonists (DORAs) for the treatment of insomnia

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

The First Large-Scale Synthesis of MK-4305: A Dual Orexin Receptor Antagonist for the Treatment of Sleep Disorder

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Orexin receptor antagonism for treatment of insomnia: a randomized clinical trial of suvorexant

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

ACS chemical neuroscience molecule spotlight on Suvorexant

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Update on emerging drugs for insomnia

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Hydrolytic instability of the important orexin 1 receptor antagonist SB-334867: possible confounding effects on in vivo and in vitro studies.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Blockade of orexin-1 receptors attenuates orexin-2 receptor antagonism-induced sleep promotion in the rat.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Identification of a novel series of orexin receptor antagonists with a distinct effect on sleep architecture for the treatment of insomnia

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Dual hypocretin receptor antagonism is more effective for sleep promotion than antagonism of either receptor alone

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Discovery of 2,5-diarylnicotinamides as selective orexin-2 receptor antagonists (2-SORAs).

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Evaluation of drug interactions with P-glycoprotein in drug discovery: in vitro assessment of the potential for drug-drug interactions with P-glycoprotein

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Clinical relevance of P-glycoprotein in drug therapy

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

The generation, detection, and effects of reactive drug metabolites

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Structural alert/reactive metabolite concept as applied in medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical examination of trends in the top 200 drugs marketed in the United States

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Demystifying brain penetration in central nervous system drug discovery. Miniperspective

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

NADPH-dependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

The current status of time dependent CYP inhibition assay and in silico drug-drug interaction predictions

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Development of an intact cell reporter gene beta-lactamase assay for G protein-coupled receptors for high-throughput screening

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

The duration of sleep promoting efficacy by dual orexin receptor antagonists is dependent upon receptor occupancy threshold

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

Quantitative electroencephalography within sleep/wake states differentiates GABAA modulators eszopiclone and zolpidem from dual orexin receptor antagonists in rats

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

21 January 2018

The dual orexin receptor antagonist almorexant induces sleep and decreases orexin-induced locomotion by blocking orexin 2 receptors

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

7 January 2021

based on heuristic

inferred from DOI database lookup

Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

7 January 2021

based on heuristic

inferred from DOI database lookup

The effect of plasma protein binding on in vivo efficacy: misconceptions in drug discovery

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

7 January 2021

based on heuristic

inferred from DOI database lookup

Pharmacokinetic benefits of 3,4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201300447

7 January 2021

based on heuristic

inferred from DOI database lookup

Identifiers

10.1002/CMDC.201300447

3 references

DOI.org query endpoint

https://doi.org/10.1002%2FCMDC.201300447

27 March 2017

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

OpenCitations bibliographic resource ID

1 reference

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

PubMed publication ID

2 references

Consolidated OpenCitations Corpus – April 2017

OpenCitations bibliographic resource ID

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:24376006%20AND%20SRC:MED&resulttype=core&format=json

3 March 2020

ResearchGate publication ID

0 references

Sitelinks

Wikipedia(0 entries)

Wikibooks(0 entries)

Wikinews(0 entries)

Wikiquote(0 entries)

Wikisource(0 entries)

Wikiversity(0 entries)

Wikivoyage(0 entries)

Wiktionary(0 entries)

Multilingual sites(0 entries)

Retrieved from "https://www.wikidata.org/w/index.php?title=Q28304842&oldid=1424149714"