|
rdf:type |
|
|
lifeskim:mentions |
umls-concept:C0023688,
umls-concept:C0038761,
umls-concept:C0087111,
umls-concept:C0205531,
umls-concept:C0226896,
umls-concept:C0243076,
umls-concept:C0289174,
umls-concept:C0442027,
umls-concept:C0682972,
umls-concept:C0851578,
umls-concept:C0935763,
umls-concept:C1367690,
umls-concept:C1426330,
umls-concept:C1428424,
umls-concept:C1527148,
umls-concept:C1527415,
umls-concept:C1880355
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|
pubmed:issue |
12
|
|
pubmed:dateCreated |
2010-6-4
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|
pubmed:abstractText |
Scaffold hopping from a non-basic series of 5-HT(2A) receptor antagonists developed in-house that possessed reduced activity in vivo enabled the discovery of a novel series of diaryl sulfones that gave excellent occupancy on oral dosing. Not only does this work further demonstrate that oral bioavailability of a given series can be enhanced by improving physicochemical parameters such as log P, but it corroborates the growing evidence that a protonated amine is not essential for affinity at aminergic GPCRs.
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pubmed:language |
eng
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pubmed:journal |
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|
pubmed:citationSubset |
IM
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pubmed:chemical |
|
|
pubmed:status |
MEDLINE
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pubmed:month |
Jun
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:copyrightInfo |
Copyright 2010 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
|
|
pubmed:volume |
20
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
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pubmed:pagination |
3708-12
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:20493697-Administration, Oral,
pubmed-meshheading:20493697-Amines,
pubmed-meshheading:20493697-Animals,
pubmed-meshheading:20493697-Biological Availability,
pubmed-meshheading:20493697-Drug Discovery,
pubmed-meshheading:20493697-Humans,
pubmed-meshheading:20493697-Ligands,
pubmed-meshheading:20493697-Receptors, G-Protein-Coupled,
pubmed-meshheading:20493697-Serotonin 5-HT2 Receptor Antagonists,
pubmed-meshheading:20493697-Serotonin Receptor Agonists,
pubmed-meshheading:20493697-Sleep Disorders,
pubmed-meshheading:20493697-Sulfones
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|
pubmed:year |
2010
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pubmed:articleTitle |
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.
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|
pubmed:affiliation |
Merck Sharp & Dohme, Eastwick Road, Harlow, Essex CM20 2QR, UK. Tammy.Ladduwahetty@glpg.com
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pubmed:publicationType |
Journal Article
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