|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
14
|
|
pubmed:dateCreated |
1996-9-10
|
|
pubmed:abstractText |
A series of potent, selective 5HT2B receptor antagonists has been identified based upon yohimbine, with SAR studies resulting in a 1000-fold increase in 5HT2B receptor affinity relative to the starting structure (-log KBS > 10.0 have been obtained). These high-affinity tetrahydro-beta-carboline antagonists are able to discriminate among the 5HT2 family of serotonin receptors, with members of the series showing selectivities of more than 100-fold versus both the 5HT2A and 5HT2C receptors based upon radioligand binding and functional assays. As the first compounds reported with such selectivity and enhanced receptor affinity, these tetrahydro-beta-carboline antagonists are useful tools for elucidating the role of serotonin acting at the 5HT2B receptor in normal and disease physiology.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Carbolines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2A,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2B,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Serotonin, 5-HT2C,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin,
http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/Yohimbine,
http://linkedlifedata.com/resource/pubmed/chemical/tryptoline
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Jul
|
|
pubmed:issn |
0022-2623
|
|
pubmed:author |
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
5
|
|
pubmed:volume |
39
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
2773-80
|
|
pubmed:dateRevised |
2006-11-15
|
|
pubmed:meshHeading |
pubmed-meshheading:8709108-Animals,
pubmed-meshheading:8709108-Carbolines,
pubmed-meshheading:8709108-Cell Line,
pubmed-meshheading:8709108-Cricetinae,
pubmed-meshheading:8709108-Gastric Fundus,
pubmed-meshheading:8709108-Male,
pubmed-meshheading:8709108-Mesocricetus,
pubmed-meshheading:8709108-Mice,
pubmed-meshheading:8709108-Molecular Structure,
pubmed-meshheading:8709108-Muscle, Smooth,
pubmed-meshheading:8709108-Muscle Contraction,
pubmed-meshheading:8709108-Rats,
pubmed-meshheading:8709108-Rats, Wistar,
pubmed-meshheading:8709108-Receptor, Serotonin, 5-HT2A,
pubmed-meshheading:8709108-Receptor, Serotonin, 5-HT2B,
pubmed-meshheading:8709108-Receptor, Serotonin, 5-HT2C,
pubmed-meshheading:8709108-Receptors, Serotonin,
pubmed-meshheading:8709108-Serotonin Antagonists,
pubmed-meshheading:8709108-Structure-Activity Relationship,
pubmed-meshheading:8709108-Yohimbine
|
|
pubmed:year |
1996
|
|
pubmed:articleTitle |
Potent, selective tetrahydro-beta-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus.
|
|
pubmed:affiliation |
Lilly Research Laboratories, Division of Eli Lilly & Company, Indianapolis, Indiana 46285, USA.
|
|
pubmed:publicationType |
Journal Article,
In Vitro
|
