|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
4
|
|
pubmed:dateCreated |
2007-2-5
|
|
pubmed:abstractText |
The incorporation of constrained tertiary amines into an existing class of N-benzyl-4-aminopiperidinyl chromone-based MCHr1 antagonists led to the identification of a series of chiral racemic compounds that displayed good to excellent functional potency, binding affinity, and selectivity over the hERG channel. Further separation of two distinct chiral racemic compounds into their corresponding pairs of enantiomers revealed a considerable selectivity for MCHr1 for one configuration, in addition to a striking difference in oral exposure between one pair of enantiomers in diet-induced obese mice. Oral administration of the most potent compound in this class in the same animal model led to significant reduction of fat mass in a semi-chronic model for weight loss.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Anti-Obesity Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Appetite Depressants,
http://linkedlifedata.com/resource/pubmed/chemical/Chromones,
http://linkedlifedata.com/resource/pubmed/chemical/Dietary Fats,
http://linkedlifedata.com/resource/pubmed/chemical/Ether-A-Go-Go Potassium Channels,
http://linkedlifedata.com/resource/pubmed/chemical/Fenfluramine,
http://linkedlifedata.com/resource/pubmed/chemical/Indicators and Reagents,
http://linkedlifedata.com/resource/pubmed/chemical/Mch1r protein, mouse,
http://linkedlifedata.com/resource/pubmed/chemical/Piperidines,
http://linkedlifedata.com/resource/pubmed/chemical/Potassium Channel Blockers,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Somatostatin
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Feb
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:BenoDavid W ADW,
pubmed-author:BrodjianSevanS,
pubmed-author:BruneMichael EME,
pubmed-author:BushEugene NEN,
pubmed-author:ChenChong JCJ,
pubmed-author:CollinsChristine ACA,
pubmed-author:DaytonBrian DBD,
pubmed-author:DiazGilbert JGJ,
pubmed-author:DrozBrian ABA,
pubmed-author:FallsH DougHD,
pubmed-author:FreemanJennifer CJC,
pubmed-author:HernandezLisa ELE,
pubmed-author:IyengarRajesh RRR,
pubmed-author:JOBCC,
pubmed-author:JuddAndrew SAS,
pubmed-author:Knourek-SegelVictoriaV,
pubmed-author:KymPhilip RPR,
pubmed-author:LynchJohn KJK,
pubmed-author:MarshKennan CKC,
pubmed-author:MulhernMathew MMM,
pubmed-author:NapierJames JJJ,
pubmed-author:ReillyRegina MRM,
pubmed-author:ShamHing LHL,
pubmed-author:ShapiroRobinR,
pubmed-author:SouersAndrew JAJ,
pubmed-author:WodkaDariuszD,
pubmed-author:ZhaoGangG
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
15
|
|
pubmed:volume |
17
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
884-9
|
|
pubmed:meshHeading |
pubmed-meshheading:17188866-Animals,
pubmed-meshheading:17188866-Anti-Obesity Agents,
pubmed-meshheading:17188866-Appetite Depressants,
pubmed-meshheading:17188866-Body Weight,
pubmed-meshheading:17188866-Brain,
pubmed-meshheading:17188866-Cell Line,
pubmed-meshheading:17188866-Chromones,
pubmed-meshheading:17188866-Diet,
pubmed-meshheading:17188866-Dietary Fats,
pubmed-meshheading:17188866-Ether-A-Go-Go Potassium Channels,
pubmed-meshheading:17188866-Fenfluramine,
pubmed-meshheading:17188866-Indicators and Reagents,
pubmed-meshheading:17188866-Mice,
pubmed-meshheading:17188866-Molecular Conformation,
pubmed-meshheading:17188866-Piperidines,
pubmed-meshheading:17188866-Potassium Channel Blockers,
pubmed-meshheading:17188866-Receptors, Somatostatin,
pubmed-meshheading:17188866-Structure-Activity Relationship
|
|
pubmed:year |
2007
|
|
pubmed:articleTitle |
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
|
|
pubmed:affiliation |
Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, IL 60064, USA. andrew.souers@abbott.com
|
|
pubmed:publicationType |
Journal Article,
Comparative Study
|
