Linked Life Data

12171573

Source:http://linkedlifedata.com/resource/pubmed/id/12171573

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
2002-8-12
pubmed:abstractText
The GABA(A) receptor system is implicated in a number of neurological diseases, making GABA(A) receptor ligands interesting as potential therapeutic agents. Only a few different classes of structures are currently known as ligands for the GABA recognition site on the GABA(A) receptor complex, reflecting the very strict structural requirements for GABA(A) receptor recognition and activation. Within the series of compounds showing agonist activity at the GABA(A) receptor site that have been developed, most of the ligands are structurally derived from the GABA(A) agonists muscimol, THIP or isoguvacine. Using recombinant GABA(A) receptors, functional selectivity has been shown for a number of compounds such as the GABA(A)agonists imidazole-4-acetic acid and THIP, showing highly subunit-dependent potency and maximal response. In the light of the interest in partial GABA(A) receptor agonists as potential therapeutics, structure-activity studies of a number of analogues of 4-PIOL, a low-efficacy partial GABA(A) agonist, have been performed. In this connection, a series of GABA(A) ligands has been developed showing pharmacological profiles from moderately potent low-efficacy partial GABA(A) agonist activity to potent and selective antagonist effect. Only little information about direct acting GABA(A) receptor agonists in clinical studies is available. Results from clinical studies on the effect of the GABA(A) agonist THIP on human sleep pattern shows that the functional consequences of a direct acting agonist are different from those seen after administration of GABA(A) receptor modulators.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/4,5,6,7-tetrahydroisoxazolo(5,4-c)py..., http://linkedlifedata.com/resource/pubmed/chemical/5-(4-piperidyl)isoxazol-3-ol, http://linkedlifedata.com/resource/pubmed/chemical/GABA Agents, http://linkedlifedata.com/resource/pubmed/chemical/GABA Agonists, http://linkedlifedata.com/resource/pubmed/chemical/GABA Antagonists, http://linkedlifedata.com/resource/pubmed/chemical/Isonicotinic Acids, http://linkedlifedata.com/resource/pubmed/chemical/Isoxazoles, http://linkedlifedata.com/resource/pubmed/chemical/Ligands, http://linkedlifedata.com/resource/pubmed/chemical/Muscimol, http://linkedlifedata.com/resource/pubmed/chemical/Piperidines, http://linkedlifedata.com/resource/pubmed/chemical/Protein Subunits, http://linkedlifedata.com/resource/pubmed/chemical/Receptors, GABA-A, http://linkedlifedata.com/resource/pubmed/chemical/isoguvacine
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
1568-0266
pubmed:author
pubmed:issnType
Print
pubmed:volume
2
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
817-32
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2002
pubmed:articleTitle
GABA(A) receptor ligands and their therapeutic potentials.
pubmed:affiliation
Departments of Medicinal Chemistry, The Royal Danish School of Pharmacy, Copenhagen, DK 2100, Denmark. bfr@dfh.dk
pubmed:publicationType
Journal Article, Review, Research Support, Non-U.S. Gov't