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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
12
|
| pubmed:dateCreated |
1999-2-1
|
| pubmed:abstractText |
A series of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamide derivatives were prepared and evaluated for their binding to 5-HT3 and dopamine D2 receptors. Among them, the 5-bromo-2-methoxy-6-methylaminonicotinamide 16 and its (R)-isomer were found to have potent affinities for both receptors. The affinities of (R)-16 for 5-HT3 and dopamine D2 receptors are approximately 3-fold higher than those of the corresponding benzamide (R)-1 (IC50: 1.1 and 12 nM vs. 2.9 and 35 nM, respectively).
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jun
|
| pubmed:issn |
0960-894X
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
16
|
| pubmed:volume |
8
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1551-4
|
| pubmed:dateRevised |
2003-11-14
|
| pubmed:meshHeading |
pubmed-meshheading:9873388-Animals,
pubmed-meshheading:9873388-Niacinamide,
pubmed-meshheading:9873388-Rats,
pubmed-meshheading:9873388-Receptors, Dopamine D2,
pubmed-meshheading:9873388-Receptors, Serotonin,
pubmed-meshheading:9873388-Receptors, Serotonin, 5-HT3,
pubmed-meshheading:9873388-Structure-Activity Relationship
|
| pubmed:year |
1998
|
| pubmed:articleTitle |
Synthesis of N-(1-ethyl-4-methylhexahydro-1,4-diazepin-6-yl)nicotinamides and their affinities for 5-HT3 and dopamine D2 receptors.
|
| pubmed:affiliation |
Discovery Research Laboratory I, Dainippon Pharmaceutical Co., Ltd., Osaka, Japan.
|
| pubmed:publicationType |
Journal Article
|