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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
5
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pubmed:dateCreated |
2010-5-3
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pubmed:abstractText |
A series of chiral 2,3-dichlorophenoxy and 1-naphthyloxy alkylamines were synthesized, and their binding affinities towards 5-HT(1D) and h5-HT(1B) receptors were evaluated. In the naphthyloxy series, the (R)-prolinol derivative was the most selective 5-HT(1D) ligand, while (S)-N-methyl-2-(1-naphthyloxy)propan-1-amine showed the highest selectivity for h5-HT(1B). Both compounds performed as 5-HT(1D) agonists in the isolated guinea pig assay and showed higher analgesic activity than both sumatriptan and the achiral analogue 20 b in the mouse hot-plate test. Neither ligand displayed any affinity for nicotinic ACh receptors present in mouse brain membranes, thus indicating that their analgesic activity does not arise through interaction with these receptors.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
May
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pubmed:issn |
1860-7187
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pubmed:author |
pubmed-author:BrunoClaudioC,
pubmed-author:CarocciAlessiaA,
pubmed-author:CatalanoAlessiaA,
pubmed-author:CavalluzziMaria MaddalenaMM,
pubmed-author:ColabufoNicola AntonioNA,
pubmed-author:CorboFilomenaF,
pubmed-author:FranchiniCarloC,
pubmed-author:GaleottiNicolettaN,
pubmed-author:GhelardiniCarlaC,
pubmed-author:LentiniGiovanniG,
pubmed-author:MatucciRosannaR,
pubmed-author:MuragliaMarilenaM
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pubmed:issnType |
Electronic
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pubmed:day |
3
|
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pubmed:volume |
5
|
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pubmed:owner |
NLM
|
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pubmed:authorsComplete |
Y
|
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pubmed:pagination |
696-704
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:20235265-Amines,
pubmed-meshheading:20235265-Analgesics,
pubmed-meshheading:20235265-Animals,
pubmed-meshheading:20235265-Mice,
pubmed-meshheading:20235265-Receptor, Serotonin, 5-HT1B,
pubmed-meshheading:20235265-Receptor, Serotonin, 5-HT1D,
pubmed-meshheading:20235265-Serotonin 5-HT1 Receptor Agonists,
pubmed-meshheading:20235265-Stereoisomerism,
pubmed-meshheading:20235265-Tryptamines
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pubmed:year |
2010
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pubmed:articleTitle |
Chiral aryloxyalkylamines: Selective 5-HT(1B/1D) activation and analgesic activity.
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pubmed:affiliation |
Dipartimento Farmaco-Chimico, Università degli Studi di Bari, Italy. glentini@farmchim.uniba.it <glentini@farmchim.uniba.it>
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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