http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1073334-A4
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f8c0982b0f02b1ed6d20a315370a3a3a |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-164 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-165 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-164 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-165 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-336 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 |
filingDate | 1999-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dbd7c5642c47bff82bff2e229466d394 |
publicationDate | 2004-04-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | EP-1073334-A4 |
titleOfInvention | POTENTIALIZATION OF SEROTONIN BY OLEAMIDE ANALOGS |
abstract | Analogs related to oleamide are employed for potentiating the 5-HT2A and 5-HT1A responses to serotonin (5-HT). With respect to the potentiation of the 5-HT2A receptor response, it is disclosed that, of the naturally occurring fatty acids, the primary amide of oleic acid (oleamide) is the most effective potentiating agent of serotonin and that the potentiating activity of oleamide analogs is highly dependent upon their structural features. In particular, the presence, position, and stereochemistry of the 9- cis double bond is required and even subtle structural variations reduce or eliminate activity. Secondary or tertiary amides may replace the primary amide but follow a well-defined relationship requiring small amide substituents suggesting that the carboxamide serves as a hydrogen bond acceptor but not donor. Alternative modifications at the carboxamide as well as modifications of the methyl terminus of the hydrocarbon region spanning the carboxamide and double bond typically eliminate activity. With respect to the potentiation of the 5-HT1A receptor response, it is disclosed that the potentiation activity of oleamide analogs is more tolerant and accommodates a wider range of structural modifications. One genus of analogs is disclosed that inhibits rather than potentiates the 5-HT2A, but not the 5-HT1A, receptor response. Such analogs permit the selective modulation of serotonin receptor subtypes and have opposing effects on the different subtypes. |
priorityDate | 1998-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 381.